685 results match your criteria Pharmaceutics [Journal]


A Review on (Hydro)Porphyrin-Loaded Polymer Micelles: Interesting and Valuable Platforms for Enhanced Cancer Nanotheranostics.

Pharmaceutics 2019 Feb 15;11(2). Epub 2019 Feb 15.

CQC and Department of Chemistry, University of Coimbra, Rua Larga, 3004-535 Coimbra, Portugal.

Porphyrins are known therapeutic agents for photodynamic therapy of cancer and also imaging agents for NIR fluorescence imaging, MRI, or PET. A combination of interesting features makes tetrapyrrolic macrocycles suitable for use as theranostic agents whose full potential can be achieved using nanocarriers. This review provides an overview on nanotheranostic agents based on polymeric micelles and porphyrins developed so far. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020081DOI Listing
February 2019

Polymer Distribution and Mechanism Conversion in Multiple Media of Phase-Separated Controlled-Release Film-Coating.

Pharmaceutics 2019 Feb 14;11(2). Epub 2019 Feb 14.

State key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.

Phase-separated films of water-insoluble ethyl cellulose (EC) and water-soluble hydroxypropyl cellulose (HPC) can be utilized to tailor drug release from coated pellets. In the present study, the effects of HPC levels and the pH, type, ionic strength and osmolarity of the media on the release profiles of soluble metoprolol succinates from the EC/HPC-coated pellets were investigated, and the differences in drug-release kinetics in multiple media were further elucidated through the HPC leaching and swelling kinetics of the pellets, morphology (SEM) and water uptake of the free films and the interaction between the coating polymers and the media compositions. Interestingly, the drug release rate from the pellets in different media was not in agreement with the drug solubility which have a positive correlation with the drug dissolution rate based on Noyes⁻Whitney equation law. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020080DOI Listing
February 2019

Improved Morphine-Loaded Hydrogels for Wound-Related Pain Relief.

Pharmaceutics 2019 Feb 12;11(2). Epub 2019 Feb 12.

Research Medicine Research Institute (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisboa, Portugal.

The use of morphine applied topically to painful wounds has potential advantages, such as dose reduction, fewer side effects and compound formulations, have been proposed for this purpose. Given the potential high impact of drug product quality on a patient's health, the aim of the present study was to develop two stable sterile hydrogels containing morphine hydrochloride, intended for topical application on painful wounds. Two carboxymethylcellulose sodium-based hydrogels were prepared containing 0. Read More

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http://www.mdpi.com/1999-4923/11/2/76
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http://dx.doi.org/10.3390/pharmaceutics11020076DOI Listing
February 2019
5 Reads

Investigation of the Quantity of Exhaled Aerosols Released into the Environment during Nebulisation.

Pharmaceutics 2019 Feb 12;11(2). Epub 2019 Feb 12.

Aerogen, IDA Business Park, Dangan, Galway, H91 HE94, Ireland.

Background: Secondary inhalation of medical aerosols is a significant occupational hazard in both clinical and homecare settings. Exposure to fugitive emissions generated during aerosol therapy increases the risk of the unnecessary inhalation of medication, as well as toxic side effects.

Methods: This study examines fugitively-emitted aerosol emissions when nebulising albuterol sulphate, as a tracer aerosol, using two commercially available nebulisers in combination with an open or valved facemask or using a mouthpiece with and without a filter on the exhalation port. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020075DOI Listing
February 2019

Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide⁻Solid Dispersion.

Pharmaceutics 2019 Feb 10;11(2). Epub 2019 Feb 10.

Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.

Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)⁻SD. The SDs of AG and the carrier materials, polyethylene glycol (PEG) and PEG grafted with carbon chains of different length (grafted PEG), have been prepared by spray-drying and vacuum-drying methods. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020074DOI Listing
February 2019

Dual Action of the PN159/KLAL/MAP Peptide: Increase of Drug Penetration across Caco-2 Intestinal Barrier Model by Modulation of Tight Junctions and Plasma Membrane Permeability.

Pharmaceutics 2019 Feb 10;11(2). Epub 2019 Feb 10.

Institute of Biophysics, Biological Research Centre, Hungarian Academy of Sciences, H-6726, Szeged, Hungary.

The absorption of drugs is limited by the epithelial barriers of the gastrointestinal tract. One of the strategies to improve drug delivery is the modulation of barrier function by the targeted opening of epithelial tight junctions. In our previous study the 18-mer amphiphilic PN159 peptide was found to be an effective tight junction modulator on intestinal epithelial and blood⁻brain barrier models. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020073DOI Listing
February 2019
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Chitosan Plus Compound 48/80: Formulation and Preliminary Evaluation as a Hepatitis B Vaccine Adjuvant.

Pharmaceutics 2019 Feb 9;11(2). Epub 2019 Feb 9.

CNC-Center for Neuroscience and Cell Biology, University of Coimbra, 3004-0504 Coimbra, Portugal.

Current vaccine research is mostly based on subunit antigens. Despite the better toxicity profile of these antigens they are often poorly immunogenic, so adjuvant association has been explored as a strategy to obtain a potent vaccine formulation. Recently, mast cell activators were recognized as a new class of vaccine adjuvants capable of potentiating mucosal and systemic immune responses. Read More

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http://www.mdpi.com/1999-4923/11/2/72
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http://dx.doi.org/10.3390/pharmaceutics11020072DOI Listing
February 2019
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Hybrid Nanogels: Stealth and Biocompatible Structures for Drug Delivery Applications.

Pharmaceutics 2019 Feb 7;11(2). Epub 2019 Feb 7.

Colorobbia Research Center (CERICOL), via Pietramarina 53, 50053 Sovigliana Vinci, Italy.

Considering nanogels, we have focused our attention on hybrid nanosystems for drug delivery and biomedical purposes. The distinctive strength of these structures is the capability to join the properties of nanosystems with the polymeric structures, where versatility is strongly demanded for biomedical applications. Alongside with the therapeutic effect, a non-secondary requirement of the nanosystem is indeed its biocompatibility. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020071DOI Listing
February 2019

Applicability of a Modified Rat Model of Acute Arthritis for Long-Term Testing of Drug Delivery Systems.

Pharmaceutics 2019 Feb 7;11(2). Epub 2019 Feb 7.

Department of Orthopedics, University Medical Center Utrecht, Heidelberglaan 100, 3508 GA Utrecht, The Netherlands.

Episodes of inflammation and pain are predominant features of arthritic joint diseases. Drug delivery systems (DDS) could reduce inflammation and pain long-term without chances of infection upon multiple injections. To allow for long-term evaluation of DDS, we modified a previously published acute arthritis model by extending follow-up periods between flare-ups. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020070DOI Listing
February 2019

Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes.

Pharmaceutics 2019 Feb 6;11(2). Epub 2019 Feb 6.

Department of Physical Chemistry, University of Seville, 41012 Seville, Spain.

Cefepime is an antibiotic with a broad spectrum of antimicrobial activity. However, this antibiotic has several side effects and a high degradation rate. For this reason, the preparation and characterization of new liposomes that are able to encapsulate this antibiotic seem to be an important research line in the pharmaceutical industry. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020069DOI Listing
February 2019

Amorphisation of Free Acid Ibuprofen and Other Profens in Mixtures with Nanocellulose: Dry Powder Formulation Strategy for Enhanced Solubility.

Pharmaceutics 2019 Feb 6;11(2). Epub 2019 Feb 6.

Nanotechnology and Functional Materials, Department of Engineering Sciences, Box 534, Uppsala University, 75121 Uppsala, Sweden.

The formulation of arylpropionic acid derivatives (profens), which are poorly soluble Biopharmaceutical Classification System (BCS) Type II drugs, has a strong impact on their therapeutic action. This article shows that heat-treated powder mixtures of free acid profens with high surface area Cladophora cellulose induces drug amorphization and results in enhanced solubility and bioavailability. Similar mixtures produced using conventional low surface area cellulose, i. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020068DOI Listing
February 2019

Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability.

Pharmaceutics 2019 Feb 3;11(2). Epub 2019 Feb 3.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.

In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The PXRD and DSC results suggested that the amorphous form of IBU was maintained in the solid dispersions. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020067DOI Listing
February 2019

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery.

Pharmaceutics 2019 Feb 2;11(2). Epub 2019 Feb 2.

Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain.

Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020066DOI Listing
February 2019

Methotrexate-Loaded Solid Lipid Nanoparticles: Protein Functionalization to Improve Brain Biodistribution.

Pharmaceutics 2019 Feb 2;11(2). Epub 2019 Feb 2.

Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, 10124 Torino, Italy.

Glioblastoma is the most common and invasive primary tumor of the central nervous system and normally has a negative prognosis. Biodistribution in healthy animal models is an important preliminary study aimed at investigating the efficacy of chemotherapy, as it is mainly addressed towards residual cells after surgery in a region with an intact blood⁻brain barrier. Nanoparticles have emerged as versatile vectors that can overcome the blood⁻brain barrier. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020065DOI Listing
February 2019

Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil.

Pharmaceutics 2019 Feb 1;11(2). Epub 2019 Feb 1.

Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain.

Donepezil (DPZ) is widely used in the treatment of Alzheimer's disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood⁻brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020064DOI Listing
February 2019
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Transferrin-Conjugated Polymeric Nanoparticle for Receptor-Mediated Delivery of Doxorubicin in Doxorubicin-Resistant Breast Cancer Cells.

Pharmaceutics 2019 Feb 1;11(2). Epub 2019 Feb 1.

College of Pharmacy, Yeungnam University, 214-1, Dae-dong, Gyeongsan 712-749, Korea.

In this study, a transferrin (T)-conjugated polymeric nanoparticle was developed for the targeted delivery of the chemotherapeutic agent doxorubicin (Dox) in order to overcome multi-drug resistance in cancer treatment. Our objective was to improve Dox delivery for producing significant antitumor efficacy in Dox-resistant (R) breast cancer cell lines with minimum toxicity to healthy cells. The results of our experiments revealed that Dox was successfully loaded inside a transferrin (T)-conjugated polymeric nanoparticle composed of poloxamer 407 (F127) and 123 (P123) (Dox/F127P123-T), which produced nanosized particles (~90 nm) with a low polydispersity index (~0. Read More

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http://www.mdpi.com/1999-4923/11/2/63
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http://dx.doi.org/10.3390/pharmaceutics11020063DOI Listing
February 2019
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Long-Lasting, Antinociceptive Effects of pH-Sensitive Niosomes Loaded with Ibuprofen in Acute and Chronic Models of Pain.

Pharmaceutics 2019 Feb 1;11(2). Epub 2019 Feb 1.

Istituto Superiore di Sanità, National Center for Drug Research and Evaluation, 00161 Rome, Italy.

Ibuprofen is one of the non-steroidal anti-inflammatory drugs (NSAIDs) widely used to treat pain conditions. NSAIDs encounter several obstacles to passing across biological membranes. To overcome these constraints, we decided to study the effects of a new pH-sensitive formulation of niosomes containing Polysorbate 20 derivatized by Glycine and loaded with ibuprofen (NioIbu) in several animal models of pain in mice. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020062DOI Listing
February 2019
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In Vitro Anticancer Activity of Extracellular Vesicles (EVs) Secreted by Gingival Mesenchymal Stromal Cells Primed with Paclitaxel.

Pharmaceutics 2019 Feb 1;11(2). Epub 2019 Feb 1.

CRC StaMeTec, Department of Biomedical, Surgical and Dental Sciences, University of Milan, 20133 Milan, Italy.

Interdental papilla are an interesting source of mesenchymal stromal cells (GinPaMSCs), which are easy to isolate and expand in vitro. In our laboratory, GinPaMSCs were isolated, expanded, and characterized by studying their secretome before and after priming with paclitaxel (PTX). The secretome of GinPaMSCs did not affect the growth of cancer cell lines tested in vitro, whereas the secretome of GinPaMSCs primed with paclitaxel (GinPaMSCs/PTX) exerted a significant anticancer effect. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020061DOI Listing
February 2019

Gold Nanocage-Incorporated Poly(ε-Caprolactone) (PCL) Fibers for Chemophotothermal Synergistic Cancer Therapy.

Pharmaceutics 2019 Feb 1;11(2). Epub 2019 Feb 1.

Department of Polymer Science and Engineering, Kyungpook National University, Daegu 41566, Korea.

This paper introduces a new fibrous system for synergistic cancer therapy, which consists of gold nanocage (AuNC)-loaded poly(ε-caprolactone) (PCL) fibers with encapsulation of a chemotherapeutic anticancer drug in their core and loading of a phase-changeable fatty acid in their sheath. Under on⁻off switching of near-infrared (NIR) light irradiation, the excellent photothermal ability and photostability of AuNCs allows repeated, significant heating of the fibers to a temperature available to hyperthermia. Simultaneously, the NIR light-induced heat generation enables the melting out of the loaded fatty acid, leading to a rapid release of the drug molecules from the fibers. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020060DOI Listing
February 2019
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Chlorambucil Conjugated Ugi Dendrimers with PAMAM-NH₂ Core and Evaluation of Their Anticancer Activity.

Pharmaceutics 2019 Feb 1;11(2). Epub 2019 Feb 1.

Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, 06120, Halle (Saale), Germany.

Herein, a new Ugi multicomponent reaction strategy is described to enhance activity and solubility of the chemotherapeutic drug chlorambucil through its conjugation to poly(amidoamine) (PAMAM-NH₂) dendrimers with the simultaneous introduction of lipidic (-Pr) and cationic (⁻NH₂) or anionic (⁻COOH) groups. Standard viability assays were used to evaluate the anticancer potential of the water-soluble dendrimers against PC-3 prostate and HT-29 colon cancer cell lines, as well as non-cancerous mouse NIH3T3 fibroblasts. It could be demonstrated that the anticancer activity against PC-3 cells was considerably improved when both chlorambucil and ⁻NH₂ (cationic) groups were present on the dendrimer surface (). Read More

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http://dx.doi.org/10.3390/pharmaceutics11020059DOI Listing
February 2019

Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire 44/14.

Pharmaceutics 2019 Jan 31;11(2). Epub 2019 Jan 31.

College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Korea.

To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of Capmul MCM (oil), Tween 80 (surfactant), Transcutol P (cosurfactant), and Poloxamer 407 (precipitation inhibitor) but encountered a stability problem (Transcutol P-induced weight loss in storage) after solidification. In the present study, replacing Transcutol P with Gelucire 44/14 resulted in a novel SuSMED formulation, wherein the total amount of surfactant/cosurfactant was less than that of the previous formulation. Solidified SuSMED (S-SuSMED) granules were prepared by blending VST-containing SuSMED with selective solid carriers, L-HPC and Florite PS-10, wherein VST existed in an amorphous state. Read More

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http://www.mdpi.com/1999-4923/11/2/58
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http://dx.doi.org/10.3390/pharmaceutics11020058DOI Listing
January 2019
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Optimized Preparation of Levofloxacin Loaded Polymeric Nanoparticles.

Pharmaceutics 2019 Jan 30;11(2). Epub 2019 Jan 30.

Department of Physical Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain.

In this work, poly(lactic--glycolic acid) (PLGA) and chitosan (CS) nanoparticles were synthesized with the purpose of encapsulating levofloxacin (LEV). A thorough study has been carried out in order to optimize the preparation of LEV-loaded polymeric nanoparticles (NPs) suitable for parenteral administration. Changes in the preparation method, in the organic solvent nature, in the pH of the aqueous phase, or in the temperature were investigated. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020057DOI Listing
January 2019

Co-Crystal Formation of Antibiotic Nitrofurantoin Drug and Melamine Co-Former Based on a Vibrational Spectroscopic Study.

Pharmaceutics 2019 Jan 30;11(2). Epub 2019 Jan 30.

Centre for THz Research, China Jiliang University, Hangzhou 310018, China.

The co-crystallization of active pharmaceutical ingredients (APIs) has received increasing attention due to the modulation of the relative physicochemical properties of APIs such as low solubility, weak permeability and relatively inferior oral bioavailability. Crystal engineering plays a decisive role in the systematic design and synthesis of co-crystals by means of exerting control on the inter-molecular interactions. The characterization and detection of such co-crystal formations plays an essential role in the field of pharmaceutical research and development. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020056DOI Listing
January 2019

Advances of Non-Ionic Surfactant Vesicles (Niosomes) and Their Application in Drug Delivery.

Pharmaceutics 2019 Jan 29;11(2). Epub 2019 Jan 29.

Engineering Research Center of Cell & Therapeutic Antibody, Ministry of Education, and School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.

Non-Ionic surfactant based vesicles, also known as niosomes, have attracted much attention in pharmaceutical fields due to their excellent behavior in encapsulating both hydrophilic and hydrophobic agents. In recent years, it has been discovered that these vesicles can improve the bioavailability of drugs, and may function as a new strategy for delivering several typical of therapeutic agents, such as chemical drugs, protein drugs and gene materials with low toxicity and desired targeting efficiency. Compared with liposomes, niosomes are much more stable during the formulation process and storage. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020055DOI Listing
January 2019

Dendritic Cell-Targeted pH-Responsive Extracellular Vesicles for Anticancer Vaccination.

Pharmaceutics 2019 Jan 27;11(2). Epub 2019 Jan 27.

Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Bucheon-si, Gyeonggi-do 14662, Korea.

Immunotherapy can potentially treat cancers on a patient-dependent manner. Most of the efforts expended on anticancer vaccination parallel the efforts expended on prototypical immunization in infectious diseases. In this study, we designed and synthesized pH-responsive extracellular vesicles (EVs) coupled with hyaluronic acid (HA), 3-(diethylamino)propylamine (DEAP), monophosphoryl lipid A (MPLA), and mucin 1 peptide (MUC1), referred to as HDEA@EVAT. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020054DOI Listing
January 2019

Localized Therapy of Vaginal Infections and Inflammation: Liposomes-In-Hydrogel Delivery System for Polyphenols.

Pharmaceutics 2019 Jan 27;11(2). Epub 2019 Jan 27.

Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Universitetsveien 57, 9037 Tromsø, Norway.

Natural polyphenols, such as resveratrol (RES) or epicatechin (EPI), are attractive for treatments of various diseases, including vaginal infections and inflammation, because of their strong anti-oxidative and anti-inflammatory properties. However, their low solubility and consequent poor bioavailability limit their therapeutic uses. To overcome these limitations, a vaginal delivery system comprising either RES or EPI liposomes-in-hydrogel was developed. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020053DOI Listing
January 2019
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Syringeable Self-Organizing Gels that Trigger Gold Nanoparticle Formation for Localized Thermal Ablation.

Pharmaceutics 2019 Jan 26;11(2). Epub 2019 Jan 26.

Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, R+D Pharma Group (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

Block copolymer dispersions that form gels at body temperature and that additionally are able to reduce a gold salt to nanoparticles (AuNPs) directly in the final formulation under mild conditions were designed as hybrid depots for photothermal therapy. The in situ gelling systems may retain AuNPs in the application zone for a long time so that localized elevations of temperature can be achieved each time the zone is irradiated. To carry out the work, dispersions were prepared covering a wide range of poloxamine Tetronic 1307:gold salt molar ratios in NaCl media (also varying from pure water to hypertonic solution). Read More

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http://dx.doi.org/10.3390/pharmaceutics11020052DOI Listing
January 2019

Improved Pharmacokinetics of Icariin (ICA) within Formulation of PEG-PLLA/PDLA-PNIPAM Polymeric Micelles.

Pharmaceutics 2019 Jan 25;11(2). Epub 2019 Jan 25.

College of Pharmacy, Jiamusi University, 148 Xuefu Road, Heilongjiang, Jiamusi 154007, China.

Icariin (ICA) is a major flavonoid that contains the active compound . However, ICA's pharmacokinetic characteristics remain unsatisfactory due to its low bioavailability, and hence limited drugability. In order to improve its pharmacokinetics and achieve prolonged blood circulation time, a novel polymeric micelle, made of the self-assembled micelle between poly (ethylene glycol)-poly (-lactic acid) (PEG-PLLA) and poly (-lactic acid)-poly(N-isopropylacrylamide) (PDLA-PNIPAM), was designed to encapsulate ICA. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020051DOI Listing
January 2019
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Cationic Niosomes as Non-Viral Vehicles for Nucleic Acids: Challenges and Opportunities in Gene Delivery.

Pharmaceutics 2019 Jan 22;11(2). Epub 2019 Jan 22.

Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Jordi Girona 18-26, E-08034 Barcelona, Spain.

Cationic niosomes have become important non-viral vehicles for transporting a good number of small drug molecules and macromolecules. Growing interest shown by these colloidal nanoparticles in therapy is determined by their structural similarities to liposomes. Cationic niosomes are usually obtained from the self-assembly of non-ionic surfactant molecules. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020050DOI Listing
January 2019
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Pharmacodynamics and Pharmacokinetics of a New Type of Compound Lansoprazole Capsule in Gastric Ulcer Rats and Beagle Dogs: Importance of Adjusting Oxidative Stress and Inflammation.

Pharmaceutics 2019 Jan 22;11(2). Epub 2019 Jan 22.

School of Pharmacy, China Medical University, Shenyang 110021, China.

The aim of this study was to investigate the pharmacodynamics and pharmacokinetics of a new type of compound lansoprazole capsule in gastric ulcer rats and beagle dogs in order to confirm whether it is more effective in treating gastric ulcers and its rapid absorption. A rat model of gastric ulcers was used to evaluate the anti-ulcerogenic effect of the compound lansoprazole capsule. A fast and sensitive UPLC-MS/MS method was developed to detect lansoprazole in dog plasma. Read More

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http://dx.doi.org/10.3390/pharmaceutics11020049DOI Listing
January 2019
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Advances in Drug Delivery and Biomaterials: Facts and Vision.

Pharmaceutics 2019 Jan 21;11(1). Epub 2019 Jan 21.

Department of Drug Chemistry and Technologies, Sapienza University of Roma, P.le Aldo Moro 5, 00185 Roma, Italy.

Drug delivery and biomaterials are different fields of science but, at the same time, are tightly related and intertwined. The 2018 CRS Italy Chapter Annual Workshop aims to explore recent advances in design and development in these areas. Many colleagues from Europe participated to the Workshop, stimulating the discussion. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010048DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359636PMC
January 2019
1 Read

Targeted Transfection Using PEGylated Cationic Liposomes Directed Towards P-Selectin Increases siRNA Delivery into Activated Endothelial Cells.

Pharmaceutics 2019 Jan 21;11(1). Epub 2019 Jan 21.

Institute of Cellular Biology and Pathology "Nicolae Simionescu," 050568 Bucharest, Romania.

The progress in small-interfering RNA (siRNA) therapeutics depends on the development of suitable nanocarriers to perform specific and effective delivery to dysfunctional cells. In this paper, we questioned whether P-selectin, a cell adhesion molecule specifically expressed on the surface of activated endothelial cells (EC) could be employed as a target for nanotherapeutic intervention. To this purpose, we developed and characterized P-selectin targeted PEGylated cationic liposomes able to efficiently pack siRNA and to function as efficient vectors for siRNA delivery to tumour necrosis factor-α (TNF-α) activated EC. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010047DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359248PMC
January 2019
1 Read

Human Olfactory Bulb Neural Stem Cells (Hu-OBNSCs) Can Be Loaded with Paclitaxel and Used to Inhibit Glioblastoma Cell Growth.

Pharmaceutics 2019 Jan 21;11(1). Epub 2019 Jan 21.

CRC StaMeTec, Department of Biomedical, Surgical and Dental Sciences, University of Milan, 20133 Milan, Italy.

Exploitation of the potential ability of human olfactory bulb (hOB) cells to carry, release, and deliver an effective, targeted anticancer therapy within the central nervous system (CNS) milieu remains elusive. Previous studies have demonstrated the marked ability of several types of stem cells (such as mesenchymal stem cells (MSCs) to carry and release different anti-cancer agents such as paclitaxel (PTX). Herein we investigate the ability of human olfactory bulb neural stem cells (Hu-OBNSCs) to carry and release paclitaxel, producing effective cytotoxic effects against cancer cells. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010045DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358986PMC
January 2019
1 Read

Behaviour of Tetrabenazine in Acid Medium: Reassessment and Impact on Formulation.

Pharmaceutics 2019 Jan 20;11(1). Epub 2019 Jan 20.

LAGEP UMR 5007, CNRS, Université Claude Bernard Lyon 1, Université de Lyon, 43 bd du 11 novembre, F-69622 Villeurbanne, France.

Thorough studies of previous analytical stress data of tetrabenazine, a dopamine depleting agent, showed a potential susceptibility to acidic conditions. Hence, the behavior of tetrabenazine acidic solutions was studied by LC-MS and NMR spectroscopy. Reverse-phase LC-MS analysis of tetrabenazine acidic aqueous solutions consistently showed a main lipophilic impurity in a proportion of 15 to 20%. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010044DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359103PMC
January 2019
2 Reads

Interactions of Self-Assembled S Polysaccharide Nanoparticles with Bovine Serum Albumin and Biodistribution of Its Docetaxel-Loaded Nanoparticles.

Pharmaceutics 2019 Jan 19;11(1). Epub 2019 Jan 19.

Department of Pharmaceutics, School of Pharmacy, Jilin University, Changchun 130012, China.

Amphiphilic copolymers of stearic acid (SA)-modified s polysaccharides (BSPs-SA) with three different degrees of substitution (DSs) were synthesized. The effects of DS values on the properties of BSPs-SA nanoparticles were evaluated. Drug state, cytotoxicity, and histological studies were carried out. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010043DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358745PMC
January 2019
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Magnetic Mixed Micelles Composed of a Non-Ionic Surfactant and Nitroxide Radicals Containing a D-Glucosamine Unit: Preparation, Stability, and Biomedical Application.

Pharmaceutics 2019 Jan 19;11(1). Epub 2019 Jan 19.

Graduate School of Human and Environmental Studies, Kyoto University, Kyoto 606-8501, Japan.

Metal-free magnetic mixed micelles (mean diameter: < 20 nm) were prepared by mixing the biocompatible non-ionic surfactant Tween 80 and the non-toxic, hydrophobic pyrrolidine--oxyl radicals bearing a D-glucosamine unit in pH 7.4 phosphate-buffered saline (PBS). The time-course stability and magnetic resonance imaging (MRI) contrast ability of the mixed micelles was found to depend on the length of the alkyl chain in the nitroxide radicals. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359449PMC
January 2019
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Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update.

Pharmaceutics 2019 Jan 19;11(1). Epub 2019 Jan 19.

IDentity, 19 Cavendish Crescent North, The Park, Nottingham NG7 1BA, UK.

The application of permeation enhancers (PEs) to improve transport of poorly absorbed active pharmaceutical ingredients across the intestinal epithelium is a widely tested approach. Several hundred compounds have been shown to alter the epithelial barrier, and although the research emphasis has broadened to encompass a role for nanoparticle approaches, PEs represent a key constituent of conventional oral formulations that have progressed to clinical testing. In this review, we highlight promising PEs in early development, summarize the current state of the art, and highlight challenges to the translation of PE-based delivery systems into safe and effective oral dosage forms for patients. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010041DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359609PMC
January 2019
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Formulation and Characterization of Eplerenone Nanoemulsion Liquisolids, An Oral Delivery System with Higher Release Rate and Improved Bioavailability.

Authors:
Ahmed Khames

Pharmaceutics 2019 Jan 18;11(1). Epub 2019 Jan 18.

Department of pharmaceutics and industrial pharmacy, Beni-suef University, Beni-Suef 62514, Egypt.

Because Eplerenone (EPL) is a Biopharmaceutical Classification System (BCS) class-II drug and is prone to extensive liver degradation, it suffers from poor bioavailability after oral administration. This work aimed to prepare liquisolids loaded with EPL-nanoemulsions (EPL-NEs) that have a higher drug release rate and improved bioavailability by the oral route. Based on solubility studies, mixtures of Triacetin (oil) and Kolliphor EL/PEG 400 surfactant/co-surfactant (S) in different ratios were used to prepare EPL-NE systems, which were characterized and optimized for droplet size, zeta potential, polydispersity index (PDI), and drug content. Read More

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http://www.mdpi.com/1999-4923/11/1/40
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http://dx.doi.org/10.3390/pharmaceutics11010040DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358907PMC
January 2019
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Comparative Analysis of Protein Quantification Methods for the Rapid Determination of Protein Loading in Liposomal Formulations.

Pharmaceutics 2019 Jan 18;11(1). Epub 2019 Jan 18.

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, UK.

Advances in manufacturing processes provide the ability for the high throughput production of liposomes containing a range of moieties, from small molecules to large biologicals (including proteins and nucleic acids for prophylactic and therapeutic applications). Whilst rapid quantification methods for small molecules are generally well established, the ability to rapidly quantify liposomal entrapment of proteins is limited. Indeed, most standard protein quantification techniques (including the BCA assay and Reverse phase-high performance liquid chromatography (RP-HPLC)) measure protein encapsulation indirectly, by measuring the amount of non-incorporated drug, and subtracting from the initial amount of protein added. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010039DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358724PMC
January 2019
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Simultaneous Quantitation of a Novel α₁/β₁-Blocker TJ0711 and Its Two Metabolites in Dog Plasma Using LC-MS/MS and Its Application to a Pharmacokinetic Study after Intravenous Infusion.

Pharmaceutics 2019 Jan 18;11(1). Epub 2019 Jan 18.

School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.

TJ0711∙HCl, which is a novel α₁/β₁ adrenoceptor blocking agent with a ratio of 1:1 for α₁/β₁, is designed to treat and prevent perioperative hypertension. M1 and M3 were identified as important metabolites in vitro for either antihypertension activity or the major metabolite production. In order to obtain a pharmacokinetic profile of both TJ0711 and its metabolites, a rapid, selective, and reliable LC-MS/MS method was developed and validated for simultaneous determination of TJ0711 and two metabolites in beagle dog plasma via efficiently separating two interferential metabolites M16 and M4 from M1 and M3, respectively. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010038DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359546PMC
January 2019
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Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate.

Pharmaceutics 2019 Jan 18;11(1). Epub 2019 Jan 18.

Nanotechnology and Functional Materials, Department of Engineering Sciences, Uppsala University, 75121 Uppsala, Sweden.

Nifedipine (NIF) is a 1,4-dihydropyridine-based calcium channel blocker with poor solubility, whose bioavailability is highly dependent on the type of formulation. Dry powder mixtures of 20% / NIF with microcrystalline cellulose (MCC) and its high surface area nanocellulose analogue, which is namely Cladophora (CLAD) cellulose, were produced by heating at the melting temperature of the drug for 1 h. Non-heated samples were used as a reference. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010037DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359467PMC
January 2019
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Intestinal Drug Absorption Enhancement by Gel and Whole Leaf Extract: In Vitro Investigations into the Mechanisms of Action.

Pharmaceutics 2019 Jan 18;11(1). Epub 2019 Jan 18.

Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), Potchefstroom Campus, North West University, Potchefstroom 2520, South Africa.

The co-administration of absorption enhancing agents with macromolecular drugs (e.g., protein and peptide drugs) has been identified as a means to improve the oral bioavailability of these drugs. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010036DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359586PMC
January 2019
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Enhanced In Situ Availability of Constituents Entrapped in Buccal Films for the Treatment of Oxidative Stress-Related Oral Diseases: Biomechanical Characterization and In Vitro/Ex Vivo Evaluation.

Pharmaceutics 2019 Jan 17;11(1). Epub 2019 Jan 17.

Department of Surgical, Oncological and Oral Sciences, University of Palermo, 90127 Palermo, Italy.

In recent years, the key role of oxidative stress in pathogenesis of oral diseases has been emphasized and the use of antioxidant agents has been encouraged. (AFA) is a unicellular blue-green alga with antioxidant and anti-inflammatory properties. The aim of this study was the formulation and characterization of mucoadhesive thin layer films loaded with AFA, finalized to the treatment of oxidative stress (OS)-related oral diseases. Read More

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http://www.mdpi.com/1999-4923/11/1/35
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http://dx.doi.org/10.3390/pharmaceutics11010035DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359436PMC
January 2019
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Stable, Monodisperse, and Highly Cell-Permeating Nanocochleates from Natural Soy Lecithin Liposomes.

Pharmaceutics 2019 Jan 16;11(1). Epub 2019 Jan 16.

Department of Chemistry, University of Florence, Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.

(1) Background: Andrographolide (AN), the main diterpenoid constituent of , has a wide spectrum of biological activities. The aim of this study was the development of nanocochleates (NCs) loaded with AN and based on phosphatidylserine (PS) or phosphatidylcholine (PC), cholesterol and calcium ions in order to overcome AN low water solubility, its instability under alkaline conditions and its rapid metabolism in the intestine. (2) Methods: The AN-loaded NCs (AN⁻NCs) were physically and chemically characterised. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010034DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359122PMC
January 2019
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Drug Bioavailability Enhancing Agents of Natural Origin (Bioenhancers) that Modulate Drug Membrane Permeation and Pre-Systemic Metabolism.

Pharmaceutics 2019 Jan 16;11(1). Epub 2019 Jan 16.

Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom 2520, South Africa.

Many new chemical entities are discovered with high therapeutic potential, however, many of these compounds exhibit unfavorable pharmacokinetic properties due to poor solubility and/or poor membrane permeation characteristics. The latter is mainly due to the lipid-like barrier imposed by epithelial mucosal layers, which have to be crossed by drug molecules in order to exert a therapeutic effect. Another barrier is the pre-systemic metabolic degradation of drug molecules, mainly by cytochrome P450 enzymes located in the intestinal enterocytes and liver hepatocytes. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010033DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359194PMC
January 2019
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Loading of Porous Functionalized Calcium Carbonate Microparticles: Distribution Analysis with Focused Ion Beam Electron Microscopy and Mercury Porosimetry.

Pharmaceutics 2019 Jan 15;11(1). Epub 2019 Jan 15.

Division of Pharmaceutical Technology, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.

Accurate analysis of intraparticle distribution of substances within porous drug carriers is important to optimize loading and subsequent processing. Mercury intrusion porosimetry, a common technique used for characterization of porous materials, assumes cylindrical pore geometry, which may lead to misinterpretation. Therefore, imaging techniques such as focused ion beam scanning electron microscopy (FIB-SEM) help to better interpret these results. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010032DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358859PMC
January 2019
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Protein Corona Fingerprints of Liposomes: New Opportunities for Targeted Drug Delivery and Early Detection in Pancreatic Cancer.

Pharmaceutics 2019 Jan 15;11(1). Epub 2019 Jan 15.

Department of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 291, 00161 Rome, Italy.

Pancreatic ductal adenocarcinoma (PDAC) is the fourth cause of cancer-related mortality in the Western world and is envisaged to become the second cause by 2030. Although our knowledge about the molecular biology of PDAC is continuously increasing, this progress has not been translated into better patients' outcome. Liposomes have been used to circumvent concerns associated with the low efficiency of anticancer drugs such as severe side effects and damage of healthy tissues, but they have not resulted in improved efficacy as yet. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010031DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358751PMC
January 2019
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Preparation and Study of the Antibacterial Applications and Oxidative Stress Induction of Copper Maleamate-Functionalized Mesoporous Silica Nanoparticles.

Pharmaceutics 2019 Jan 14;11(1). Epub 2019 Jan 14.

Departamento de Biología y Geología, Física y Química Inorgánica, ESCET, Universidad Rey Juan Carlos, Calle Tulipán s/n, E-28933 Móstoles (Madrid), Spain.

Mesoporous silica nanoparticles (MSNs) are an interesting class of nanomaterials with potential applications in different therapeutic areas and that have been extensively used as drug carriers in different fields of medicine. The present work is focused on the synthesis of MSNs containing a maleamato ligand (MSN-maleamic) and the subsequent coordination of copper(II) ions (MSN-maleamic-Cu) for the exploration of their potential application as antibacterial agents. The Cu-containing nanomaterials have been characterized by different techniques and the preliminary antibacterial effect of the supported maleamato-copper(II) complexes has been tested against two types of bacteria (Gram positive and Gram negative) in different assays to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Read More

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http://dx.doi.org/10.3390/pharmaceutics11010030DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359009PMC
January 2019
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Transungual Delivery of Ciclopirox Is Increased 3⁻4-Fold by Mechanical Fenestration of Human Nail Plate in an In Vitro Model.

Pharmaceutics 2019 Jan 14;11(1). Epub 2019 Jan 14.

Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain.

Onychomycosis is a fungal infection of nails that is widespread and difficult to treat because of the impermeable nature of human nails. Topically applied anti-fungal agents cannot penetrate this structure, and treatment regimens often resort to systemic antifungals with concomitant side effects. One recent clinical study suggested that mechanical fenestration of the nail using an intelligent nail drill might be a possible solution to this problem. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010029DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358885PMC
January 2019
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A New Generation of Dihydropyridine Calcium Channel Blockers: Photostabilization of Liquid Formulations Using Nonionic Surfactants.

Pharmaceutics 2019 Jan 11;11(1). Epub 2019 Jan 11.

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.

The stability profile of a new 1,4-dihydropyridine derivative (DHP), representative of a series with a hexahydroquinoline ring, was studied to design light-stable liquid formulations. This molecule, named M3, has been shown among the analogs to have a high capacity to block both L- and T-type calcium channels. The ethanol solution of the drug was subjected to a photodegradation test, in accordance with standard rules. Read More

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http://dx.doi.org/10.3390/pharmaceutics11010028DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359235PMC
January 2019
1 Read