802 results match your criteria Pharmaceutics [Journal]


In Vivo Biocompatibility of Electrospun Biodegradable Dual Carrier (Antibiotic + Growth Factor) in a Mouse Model-Implications for Rapid Wound Healing.

Pharmaceutics 2019 Apr 14;11(4). Epub 2019 Apr 14.

Department of Chemical and Product Safety, German Federal Institute for Risk Assessment (BfR), Max-Dohrn-Strasse 8-10, 10589 Berlin, Germany.

Tissue engineering technologies involving growth factors have produced one of the most advanced generations of diabetic wound healing solutions. Using this approach, a nanocomposite carrier was designed using Poly(d,l-lactide--glycolide) (PLGA)/Gelatin polymer solutions for the simultaneous release of recombinant human epidermal growth factor (rhEGF) and gentamicin sulfate at the wound site to hasten the process of diabetic wound healing and inactivation of bacterial growth. The physicochemical characterization of the fabricated scaffolds was carried out using scanning electron microscopy (SEM) and X-ay diffraction (XRD). Read More

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https://www.mdpi.com/1999-4923/11/4/180
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http://dx.doi.org/10.3390/pharmaceutics11040180DOI Listing
April 2019
1 Read

Biodistribution and Physiologically-Based Pharmacokinetic Modeling of Gold Nanoparticles in Mice with Interspecies Extrapolation.

Pharmaceutics 2019 Apr 12;11(4). Epub 2019 Apr 12.

School of Pharmacy, University of Waterloo, Kitchener, ON N2G 1C5, Canada.

Gold nanoparticles (AuNPs) are a focus of growing medical research applications due to their unique chemical, electrical and optical properties. Because of uncertain toxicity, "green" synthesis methods are emerging, using plant extracts to improve biological and environmental compatibility. Here we explore the biodistribution of green AuNPs in mice and prepare a physiologically-based pharmacokinetic (PBPK) model to guide interspecies extrapolation. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040179DOI Listing

Characteristics of Skin Deposition of Itraconazole Solubilized in Cream Formulation.

Pharmaceutics 2019 Apr 22;11(4). Epub 2019 Apr 22.

College of Pharmacy, Chung-Ang University, Seoul 06974, Korea.

Itraconazole (ITZ) is an anti-fungal agent generally used to treat cutaneous mycoses. For efficient delivery of ITZ to the skin tissues, an oil-in-water (O/W) cream formulation was developed. The O/W cream base was designed based on the solubility measurement of ITZ in various excipients. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040195DOI Listing

Influence of High, Disperse API Load on Properties along the Fused-Layer Modeling Process Chain of Solid Dosage Forms.

Pharmaceutics 2019 Apr 22;11(4). Epub 2019 Apr 22.

Institute for Particle Technology, TU Braunschweig, Volkmaroder Str. 5, 38104 Braunschweig, Germany.

In order to cope with the increasing number of multimorbid patients due to demographic changes, individualized polypill solutions must be developed. One promising tool is fused layer modeling (FLM) of dosage forms with patient-specific dose combinations and release individualization. As there are few approaches reported that systematically investigate the influence of high disperse active pharmaceutical ingredient (API) loads in filaments needed for FLM, this was the focus for the present study. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040194DOI Listing

Comparison of Salbutamol Delivery Efficiency for Jet versus Mesh Nebulizer Using Mice.

Pharmaceutics 2019 Apr 19;11(4). Epub 2019 Apr 19.

Department of Medical Engineering, Dongguk University College of Medicine, Goyang-si, Gyeonggi-do 10326, Korea.

Recent reports using a breathing simulator system have suggested that mesh nebulizers provide more effective medication delivery than jet nebulizers. In this study, the performances of jet and mesh nebulizers were evaluated by comparing their aerosol drug delivery efficiencies in mice. We compared four home nebulizers: two jet nebulizers (PARI BOY SX with red and blue nozzles), a static mesh nebulizer (NE-U22), and a vibrating mesh nebulizer (NE-SM1). Read More

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http://dx.doi.org/10.3390/pharmaceutics11040192DOI Listing

Current State and Future Perspectives on Gastroretentive Drug Delivery Systems.

Pharmaceutics 2019 Apr 20;11(4). Epub 2019 Apr 20.

College of Pharmacy, Dongguk University-Seoul, 32 Donggukro, Ilsandonggu, Goyang, Gyeonggi 10326, Korea.

In recent years, many attempts have been made to enhance the drug bioavailability and therapeutic effectiveness of oral dosage forms. In this context, various gastroretentive drug delivery systems (GRDDS) have been used to improve the therapeutic efficacy of drugs that have a narrow absorption window, are unstable at alkaline pH, are soluble in acidic conditions, and are active locally in the stomach. In this review, we discuss the physiological state of the stomach and various factors that affect GRDDS. Read More

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https://www.mdpi.com/1999-4923/11/4/193
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http://dx.doi.org/10.3390/pharmaceutics11040193DOI Listing
April 2019
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An In Vitro Study of the Influence of Extracts on the Microbiota Modulation Process, In Patients with Hypertension.

Pharmaceutics 2019 Apr 18;11(4). Epub 2019 Apr 18.

Department of Genetics, ICUB-Research Institute of the University of Bucharest, 36-46 Bd. M. Kogalniceanu, 5th District, 050107 Bucharest, Romania.

The multiple causes of cardiovascular diseases signify a major incidence and developmental risk of this pathology. One of the processes accountable for this pathologic development is the instauration of dysbiosis and its connection with an inflammatory process. Low antioxidant colonic protection encourages the progression of inflammation, with cardiovascular dysfunctions being a secondary consequence of the dysbiosis. Read More

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https://www.mdpi.com/1999-4923/11/4/191
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http://dx.doi.org/10.3390/pharmaceutics11040191DOI Listing
April 2019
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Preparation and Physicochemical Stability of Liquid Oral Dosage Forms Free of Potentially Harmful Excipient Designed for Pediatric Patients.

Pharmaceutics 2019 Apr 18;11(4). Epub 2019 Apr 18.

Health-Endocrine Disruptors-EXposome (HEDEX), CIC Inserm 1402, University Hospital of Poitiers, Poitiers 86021, France.

Dexamethasone, hydrochlorothiazide, spironolactone, and phenytoin are commonly used in neonates, but no age-appropriate formulation containing these active pharmaceutical ingredients (APIs) is commercially available. Thus, pharmaceutical compounding of the liquid oral dosage form is required to enable newborn administration. A problem common to the compounded preparations described in the literature is that they include potentially harmful excipients (PHEs). Read More

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https://www.mdpi.com/1999-4923/11/4/190
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http://dx.doi.org/10.3390/pharmaceutics11040190DOI Listing
April 2019
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Enhanced Intestinal Permeability and Plasma Concentration of Metformin in Rats by the Repeated Administration of Red Ginseng Extract.

Pharmaceutics 2019 Apr 18;11(4). Epub 2019 Apr 18.

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea.

We aimed to assess the potential herb-drug interactions between Korean red ginseng extract (RGE) and metformin in rats in terms of the modulation of metformin transporters, such as organic cation transporter (Oct), multiple toxin and extrusion protein (Mate), and plasma membrane monoamine transporter (Pmat). Single treatment of RGE did not inhibit the in vitro transport activity of OCT1/2 up to 500 µg/mL and inhibited MATE1/2-K with high IC value (more than 147.8 µg/mL), suggesting that concomitant used of RGE did not directly inhibit OCT- and MATE-mediated metformin uptake. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040189DOI Listing
April 2019
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Co-Delivery of M2e Virus-Like Particles with Influenza Split Vaccine to the Skin Using Microneedles Enhances the Efficacy of Cross Protection.

Pharmaceutics 2019 Apr 18;11(4). Epub 2019 Apr 18.

Institute for Biomedical Sciences, Georgia State University, Atlanta, GA 30303, USA.

It is a high priority to develop a simple and effective delivery method for a cross-protective influenza vaccine. We investigated skin immunization by microneedle (MN) patch with human influenza split vaccine and virus-like particles containing heterologous M2 extracellular (M2e) domains (M2e5x virus-like particles (VLP)) as a cross-protective influenza vaccine candidate. Co-delivery of influenza split vaccine and M2e5x VLP to the skin by MN patch was found to confer effective protection against heterosubtypic influenza virus by preventing weight loss and reducing lung viral loads. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040188DOI Listing

Gellan Gum/Laponite Beads for the Modified Release of Drugs: Experimental and Modeling Study of Gastrointestinal Release.

Pharmaceutics 2019 Apr 17;11(4). Epub 2019 Apr 17.

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, Italy.

In this study, gellan gum (GG), a natural polysaccharide, was used to fabricate spherical porous beads suitable as sustained drug delivery systems for oral administration. GG was cross-linked with calcium ions to prepare polymeric beads. Rheological studies and preliminary experiments of beads preparation allowed to identify the GG and the CaCl concentrations suitable for obtaining stable and spherical particles. Read More

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https://www.mdpi.com/1999-4923/11/4/187
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http://dx.doi.org/10.3390/pharmaceutics11040187DOI Listing
April 2019
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Phospholipid-Based Prodrugs for Colon-Targeted Drug Delivery: Experimental Study and In-Silico Simulations.

Pharmaceutics 2019 Apr 16;11(4). Epub 2019 Apr 16.

Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

In ulcerative colitis (UC), the inflammation is localized in the colon, and one of the successful strategies for colon-targeting drug delivery is the prodrug approach. In this work, we present a novel phospholipid (PL)-based prodrug approach, as a tool for colonic drug targeting in UC. We aim to use the phospholipase A (PLA), an enzyme that is overexpressed in the inflamed colonic tissues of UC patients, as the PL-prodrug activating enzyme, to accomplish the liberation of the parent drug from the prodrug complex at the specific diseased tissue(s). Read More

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http://dx.doi.org/10.3390/pharmaceutics11040186DOI Listing

Development and Characterization of Liposomal Formulations Containing Phytosterols Extracted from Canola Oil Deodorizer Distillate along with Tocopherols as Food Additives.

Pharmaceutics 2019 Apr 16;11(4). Epub 2019 Apr 16.

Drug Design and Discovery Group, College of Pharmacy and Nutrition, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5, Canada.

Phytosterols are plant sterols recommended as adjuvant therapy for hypercholesterolemia and tocopherols are well-established anti-oxidants. However, thermo-sensitivity, lipophilicity and formulation-dependent efficacy bring challenges in the development of functional foods, enriched with phytosterols and tocopherols. To address this, we developed liposomes containing brassicasterol, campesterol and β-sitosterol obtained from canola oil deodorizer distillate, along with alpha, gamma and delta tocopherol. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040185DOI Listing

Design of Poly(lactic--glycolic Acid) (PLGA) Nanoparticles for Vaginal Co-Delivery of Griffithsin and Dapivirine and Their Synergistic Effect for HIV Prophylaxis.

Pharmaceutics 2019 Apr 16;11(4). Epub 2019 Apr 16.

Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15261, USA.

Long-acting topical products for pre-exposure prophylaxis (PrEP) that combine antiretrovirals (ARVs) inhibiting initial stages of infection are highly promising for prevention of HIV sexual transmission. We fabricated core-shell poly(lactide--glycolide) (PLGA) nanoparticles, loaded with two potent ARVs, griffithsin (GRFT) and dapivirine (DPV), having different physicochemical properties and specifically targeting the fusion and reverse transcription steps of HIV replication, as a potential long-acting microbicide product. The nanoparticles were evaluated for particle size and zeta potential, drug release, cytotoxicity, cellular uptake and in vitro bioactivity. Read More

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https://www.mdpi.com/1999-4923/11/4/184
Publisher Site
http://dx.doi.org/10.3390/pharmaceutics11040184DOI Listing
April 2019
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Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis.

Pharmaceutics 2019 Apr 15;11(4). Epub 2019 Apr 15.

Department of Pharmaceutics, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.

Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, and ¹H-nuclear magnetic resonance spectroscopy analyses. Moreover, advantages of using SH as an excipient were investigated by comparing physiological properties and pharmacokinetic behaviors of SH-containing AZI eye drops with that of hydroxypropyl methylcellulose (HPMC)-containing formulation. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040183DOI Listing
April 2019
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Electrospun Nanofibers for Tissue Engineering with Drug Loading and Release.

Pharmaceutics 2019 Apr 15;11(4). Epub 2019 Apr 15.

State Key Laboratory for Modification of Chemical Fibers and Polymer Materials, College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, China.

Electrospinning technologies have been applied in the field of tissue engineering as materials, with nanoscale-structures and high porosity, can be easily prepared via this method to bio-mimic the natural extracellular matrix (ECM). Tissue engineering aims to fabricate functional biomaterials for the repairment and regeneration of defective tissue. In addition to the structural simulation for accelerating the repair process and achieving a high-quality regeneration, the combination of biomaterials and bioactive molecules is required for an ideal tissue-engineering scaffold. Read More

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https://www.mdpi.com/1999-4923/11/4/182
Publisher Site
http://dx.doi.org/10.3390/pharmaceutics11040182DOI Listing
April 2019
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Effect of Cationic Lipid Type in Folate-PEG-Modified Cationic Liposomes on Folate Receptor-Mediated siRNA Transfection in Tumor Cells.

Pharmaceutics 2019 Apr 15;11(4). Epub 2019 Apr 15.

Department of Drug Delivery Research, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan.

In this study, we examined the effect of cationic lipid type in folate (FA)-polyethylene glycol (PEG)-modified cationic liposomes on gene-silencing effects in tumor cells using cationic liposomes/siRNA complexes (siRNA lipoplexes). We used three types of cationic cholesterol derivatives, cholesteryl (3-((2-hydroxyethyl)amino)propyl)carbamate hydroiodide (HAPC-Chol), -(2-(2-hydroxyethylamino)ethyl)cholesteryl-3-carboxamide (OH-Chol), and cholesteryl (2-((2-hydroxyethyl)amino)ethyl)carbamate (OH-C-Chol), and we prepared three types of FA-PEG-modified siRNA lipoplexes. The modification of cationic liposomes with 1-2 mol % PEG-lipid abolished the gene-silencing effect in human nasopharyngeal tumor KB cells, which overexpress the FA receptor (FR). Read More

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https://www.mdpi.com/1999-4923/11/4/181
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http://dx.doi.org/10.3390/pharmaceutics11040181DOI Listing
April 2019
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Tuning the Transdermal Delivery of Hydroquinone upon Formulation with Novel Permeation Enhancers.

Pharmaceutics 2019 Apr 4;11(4). Epub 2019 Apr 4.

Department of Pharmaceutics and Food Technology, School of Pharmacy, Complutense University of Madrid, Ramón y Cajal square, 28040 Madrid, Spain.

Hydroquinone (HQ) is an anti-hyperpigmentation agent with poor physicochemical stability. HQ formulations are currently elaborated by compounding in local pharmacies. Variability in the characteristics of HQ topical formulations can lead to remarkable differences in terms of their stability, efficacy, and toxicity. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040167DOI Listing
April 2019
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A New Hope: Self-Assembling Peptides with Antimicrobial Activity.

Pharmaceutics 2019 Apr 4;11(4). Epub 2019 Apr 4.

Department of Pharmacy, University of Naples Federico II, Via Mezzocannone 16, 80134 Naples, Italy.

Peptide drugs hold great promise for the treatment of infectious diseases thanks to their novel mechanisms of action, low toxicity, high specificity, and ease of synthesis and modification. Naturally developing self-assembly in nature has inspired remarkable interest in self-assembly of peptides to functional nanomaterials. As a matter of fact, their structural, mechanical, and functional advantages, plus their high bio-compatibility and bio-degradability make them excellent candidates for facilitating biomedical applications. Read More

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https://www.mdpi.com/1999-4923/11/4/166
Publisher Site
http://dx.doi.org/10.3390/pharmaceutics11040166DOI Listing
April 2019
3 Reads

Antioxidant PLA Composites Containing Lignin for 3D Printing Applications: A Potential Material for Healthcare Applications.

Pharmaceutics 2019 Apr 4;11(4). Epub 2019 Apr 4.

School of Pharmacy, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK.

Lignin (LIG) is a natural biopolymer with well-known antioxidant capabilities. Accordingly, in the present work, a method to combine LIG with poly(lactic acid) (PLA) for fused filament fabrication applications (FFF) is proposed. For this purpose, PLA pellets were successfully coated with LIG powder and a biocompatible oil (castor oil). Read More

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http://dx.doi.org/10.3390/pharmaceutics11040165DOI Listing

Development of a New Ex Vivo Lipolysis-Absorption Model for Nanoemulsions.

Pharmaceutics 2019 Apr 4;11(4). Epub 2019 Apr 4.

School of Health Sciences, Macao Polytechnic Institute, Macau 999078, China.

The use of lipid-based formulations (LBFs) in improving the absorption of poorly water-soluble drugs has now well established. Because the in vivo evaluation of LBFs is labor-intensive, in vitro or ex vivo approaches could provide advantages. In this study, a new ex vivo lipolysis-absorption model (LAM) composed of an intestinal digestion system and an intestinal tissue system was developed to evaluate and predict the in vivo absorption performances of LBFs. Read More

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https://www.mdpi.com/1999-4923/11/4/164
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http://dx.doi.org/10.3390/pharmaceutics11040164DOI Listing
April 2019
3 Reads

Co-Delivery of Eugenol and Dacarbazine by Hyaluronic Acid-Coated Liposomes for Targeted Inhibition of Survivin in Treatment of Resistant Metastatic Melanoma.

Pharmaceutics 2019 Apr 3;11(4). Epub 2019 Apr 3.

Departmant of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.

While melanoma remains a challenge for oncologists, possibilities are being continuously explored to fight resistant metastatic melanoma more effectively. Eugenol is reported to inhibit survivin protein in breast cancer cells. Survivin is also overexpressed by melanoma cells, and is known to impart resistance to them against chemotherapy-induced apoptosis. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040163DOI Listing

Pharmacokinetics and Metabolism of Acetyl Triethyl Citrate, a Water-Soluble Plasticizer for Pharmaceutical Polymers in Rats.

Pharmaceutics 2019 Apr 3;11(4). Epub 2019 Apr 3.

Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 15588, Korea.

Acetyl triethyl citrate (ATEC) is a water-soluble plasticizer used in pharmaceutical plasticized polymers. In this study, the pharmacokinetics and metabolism of ATEC were investigated using liquid chromatography-tandem mass spectrometry (LC-MS/MS) in rats. Plasma protein precipitation with methanol was used for sample preparation. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040162DOI Listing

Release Profile of Gentamicin Sulfate from Polylactide--Polycaprolactone Electrospun Nanofiber Matrices.

Pharmaceutics 2019 Apr 3;11(4). Epub 2019 Apr 3.

Department of Drug Sciences, University of Pavia, Viale Taramelli 12/14, 27100 Pavia, Italy.

The advent and growth of resistance phenomena to antibiotics has reached critical levels, invalidating the action of a majority of antibiotic drugs currently used in the clinical field. Several innovative techniques, such as the nanotechnology, can be applied for creating innovative drug delivery systems designed to modify drug release itself and/or drug administration route; moreover, they have proved suitable for overcoming the phenomenon of antibiotic resistance. Electrospun nanofibers, due to their useful structural properties, are showing promising results as antibiotic release devices for preventing bacteria biofilm formation after surgical operation and for limiting resistance phenomena. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040161DOI Listing
April 2019
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Relating Advanced Electrospun Fiber Architectures to the Temporal Release of Active Agents to Meet the Needs of Next-Generation Intravaginal Delivery Applications.

Pharmaceutics 2019 Apr 3;11(4). Epub 2019 Apr 3.

Department of Pharmacology and Toxicology, School of Medicine, University of Louisville, Louisville, KY 40202, USA.

Electrospun fibers have emerged as a relatively new delivery platform to improve active agent retention and delivery for intravaginal applications. While uniaxial fibers have been explored in a variety of applications including intravaginal delivery, the consideration of more advanced fiber architectures may offer new options to improve delivery to the female reproductive tract. In this review, we summarize the advancements of electrospun coaxial, multilayered, and nanoparticle-fiber architectures utilized in other applications and discuss how different material combinations within these architectures provide varied durations of release, here categorized as either transient (within 24 h), short-term (24 h to one week), or sustained (beyond one week). Read More

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https://www.mdpi.com/1999-4923/11/4/160
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http://dx.doi.org/10.3390/pharmaceutics11040160DOI Listing
April 2019
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Characterization of Amorphous Solid Dispersion of Pharmaceutical Compound with pH-Dependent Solubility Prepared by Continuous-Spray Granulator.

Pharmaceutics 2019 Apr 3;11(4). Epub 2019 Apr 3.

Graduate School of Pharmaceutical Sciences, Musashino University, 1-1-20 Shin-machi, Nishi-Tokyo, Tokyo 202-8585, Japan.

A continuous-spray granulator (CTS-SGR) is a one-step granulation technology capable of using solutions or suspensions. The present research objectives were, (1) to reduce the manufacturing operations for solid dosage formulations, (2) to make amorphous solid dispersion (ASD) granules without pre-preparation of amorphous solids of active pharmaceutical ingredients (API), and (3) to characterize the obtained SGR granules by comprehensive pharmaceutical analysis. Rebamipide (RBM), a biopharmaceutical classification system class IV drug, that has low solubility or permeability in the stomach, was selected as a model compound. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040159DOI Listing

Melt-Cast Films Significantly Enhance Triamcinolone Acetonide Delivery to the Deeper Ocular Tissues.

Pharmaceutics 2019 Apr 2;11(4). Epub 2019 Apr 2.

Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA.

Delivering an effective drug load to the posterior section of the ocular tissues, while using a non-invasive technique, has always been a challenge. In this regard, the goal of the present study was to develop sustained release triamcinolone acetonide (TA) loaded polymeric matrix films for ocular delivery. The TA-films were prepared in two different polymer matrices, with drug loadings of 10% and 20% /, and they were evaluated for ocular distribution in vivo in a conscious rabbit model. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040158DOI Listing

Achieving High Excipient Efficiency with Elastic Thermoplastic Polyurethane by Ultrasound Assisted Direct Compression.

Pharmaceutics 2019 Apr 2;11(4). Epub 2019 Apr 2.

Departamento de Farmacia y Tecnología Farmacéutica. Facultad de Farmacia, Universidad de Sevilla, 41012 Seville, Spain.

Ultrasound assisted compression (USAC) is a manufacturing technique which applies thermal and mechanical energy to the powder bed, producing tablets with improved characteristics compared to the direct compression process. This technology is ideal for thermoplastic materials, as polyurethanes, whose particles usually undergo a sintering process. Thermoplastic polyurethanes are widely used in sustained drug release systems but rarely seen in tablets due to their elastic properties. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040157DOI Listing

Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model.

Pharmaceutics 2019 Apr 2;11(4). Epub 2019 Apr 2.

School of Pharmacy, University of Waterloo, Waterloo, ON N2L3G1, Canada.

Phyto-phospholipid complexes have been developed as a common way of improving the oral bioavailability of poorly absorbable phyto-pharmaceuticals; however, the complexation with phospholipids can induce positive or negative effects on the bioaccessibility of such plant-derived active ingredients in different parts of the gastrointestinal tract (GIT). The purpose of this study was to investigate the effects of phospholipid complexation on the bioaccessibility of a rosmarinic acid-phospholipid complex (RA-PLC) using the TNO dynamic intestinal model-1 (TIM-1). Preparation of RA-PLC was confirmed using X-ray diffraction, Fourier-transform infrared spectroscopy, partition coefficient measurement, and Caco-2 monolayer permeation test. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040156DOI Listing

Short and Long-Term Effects of the Exposure of Breast Cancer Cell Lines to Different Ratios of Free or Co-Encapsulated Liposomal Paclitaxel and Doxorubicin.

Pharmaceutics 2019 Apr 11;11(4). Epub 2019 Apr 11.

Department of Pharmaceutical Products, Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, 31270-901, Belo Horizonte, Minas Gerais, Brazil.

Background: Associating paclitaxel (PTX) to doxorubicin (DXR) is one of the main chemotherapy strategies for breast cancer (BC) management. Protocols currently available consist in administering both drugs on their maximum tolerated dose, not taking into account the possible differences in efficacy due to their combination ratio. In the present study, the short and long-term cytotoxic effects as well as migratory effects of PTX, DXR, and its combinations at 10:1; 1:1 and 1:10 PTX:DXR molar ratios either free or co-encapsulated in liposomes were evaluated against three human BC cell lines (MDA-MB-231, MCF-7, and SKBR-3). Read More

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http://dx.doi.org/10.3390/pharmaceutics11040178DOI Listing

Cell Internalization in Fluidic Culture Conditions Is Improved When Microparticles Are Specifically Targeted to the Human Epidermal Growth Factor Receptor 2 (HER2).

Pharmaceutics 2019 Apr 11;11(4). Epub 2019 Apr 11.

Unitat de Biologia Cel·lular, Departament de Biologia Cel·lular, Fisiologia i Immunologia, Facultat de Biociències, Universitat Autònoma de Barcelona, Bellaterra, 08193 Barcelona, Spain.

Purpose: To determine if the specific targeting of microparticles improves their internalization by cells under fluidic conditions.

Methods: Two isogenic breast epithelial cell lines, one overexpressing the Human Epidermal Growth Factor Receptor 2 (HER2) oncogene (D492HER2) and highly tumorigenic and the other expressing HER2 at much lower levels and non-tumorigenic (D492), were cultured in the presence of polystyrene microparticles of 1 µm in diameter, biofunctionalized with either a specific anti-HER2 antibody or a non-specific secondary antibody. Mono- and cocultures of both cell lines in static and fluidic conditions were performed, and the cells with internalized microparticles were scored. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040177DOI Listing

Dual pH/Redox-Responsive Mixed Polymeric Micelles for Anticancer Drug Delivery and Controlled Release.

Pharmaceutics 2019 Apr 11;11(4). Epub 2019 Apr 11.

Advanced Research Institute for Multidisciplinary Science, Beijing Institute of Technology, Beijing 100081, China.

Stimuli-responsive polymeric micelles (PMs) have shown great potential in drug delivery and controlled release in cancer chemotherapy. Herein, inspired by the features of the tumor microenvironment, we developed dual pH/redox-responsive mixed PMs which are self-assembled from two kinds of amphiphilic diblock copolymers (poly(ethylene glycol) methyl ether-b-poly(β-amino esters) (mPEG-b-PAE) and poly(ethylene glycol) methyl ether-grafted disulfide-poly(β-amino esters) (PAE-ss-mPEG)) for anticancer drug delivery and controlled release. The co-micellization of two copolymers is evaluated by measurement of critical micelle concentration (CMC) values at different ratios of the two copolymers. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040176DOI Listing

Modulation of the Release of a Non-Interacting Low Solubility Drug from Chitosan Pellets Using Different Pellet Size, Composition and Numerical Optimization.

Pharmaceutics 2019 Apr 10;11(4). Epub 2019 Apr 10.

Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.

Two size classes of piroxicam (PXC) pellets (mini (380-550 μm) and conventional (700-1200 μm)) were prepared using extrusion/spheronization and medium viscosity chitosan (CHS). Mixture experimental design and numerical optimization were applied to distinguish formulations producing high sphericity pellets with fast or extended release. High CHS content required greater wetting liquid volume for pellet formation and the diameter decreased linearly with volume. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040175DOI Listing

Polyelectrolytes in Hot Melt Extrusion: A Combined Solvent-Based and Interacting Additive Technique for Solid Dispersions.

Pharmaceutics 2019 Apr 10;11(4). Epub 2019 Apr 10.

Institute of Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, Hofackerstr. 30, 4132 Muttenz, Switzerland.

Solid dispersions are important supersaturating formulations to orally deliver poorly water-soluble drugs. A most important process technique is hot melt extrusion but process requirements limit the choice of suitable polymers. One way around this limitation is to synthesize new polymers. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040174DOI Listing

Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV.

Pharmaceutics 2019 Apr 9;11(4). Epub 2019 Apr 9.

Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.

Tenofovir alafenamide (TAF) is an effective nucleotide reverse transcriptase inhibitor that is used in the treatment of HIV-1 and HBV. Currently, it is being investigated for HIV prophylaxis. Oral TAF regimens require daily intake, which hampers adherence and increases the possibility of viral resistance. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040173DOI Listing
April 2019
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Age-Related Medicine.

Pharmaceutics 2019 Apr 9;11(4). Epub 2019 Apr 9.

Medicines Evaluation Board in the Netherlands, Quality Department, Chemical Pharmaceutical Assessments, P.O. Box 8275, 3503 RG Utrecht, The Netherlands.

A meeting organised by the Academy of Pharmaceutical Sciences focussed on the challenges of developing medicines for older adults. International experts discussed the complexity introduced by polypharmacy and multiple morbidities and how the risk⁻benefit ratio of a medicine changes as an individual ages. The way in which regulatory authorities are encouraging the development of age-appropriate medicines was highlighted. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040172DOI Listing

A Low-Molecular-Weight Polyethylenimine/pDNA-VEGF Polyplex System Constructed in a One-Pot Manner for Hindlimb Ischemia Therapy.

Pharmaceutics 2019 Apr 8;11(4). Epub 2019 Apr 8.

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

Peripheral arterial disease (PAD) is often characterized by continued reduction in blood flow supply to limbs. Advanced therapeutic strategies like gene therapy could potentially be applied to limb ischemia therapy. However, developing a gene delivery system with low toxicity and high efficiency remains a great challenge. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040171DOI Listing
April 2019
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Mechanistic Studies on the Absorption-Enhancing Effects of Gemini Surfactant on the Intestinal Absorption of Poorly Absorbed Hydrophilic Drugs in Rats.

Pharmaceutics 2019 Apr 7;11(4). Epub 2019 Apr 7.

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto 607-8414, Japan.

Generally, the use of absorption enhancers might be the most effective approaches to ameliorate the enteric absorption of poorly absorbed substances. Among numerous absorption enhancers, we already reported that a gemini surfactant, sodium dilauramidoglutamide lysine (SLG-30) with two hydrophobic and two hydrophilic moieties, is a novel and promising adjuvant with a high potency in improving the absorption safely. Here, we examined and elucidated the absorption-improving mechanisms of SLG-30 in the enteric absorption of substances. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040170DOI Listing
April 2019
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Cytotoxic Effect of Paclitaxel and Lapatinib -Delivered in Polylactide--Poly(ethylene glycol) Micelles on HER-2-Negative Breast Cancer Cells.

Pharmaceutics 2019 Apr 6;11(4). Epub 2019 Apr 6.

School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia, Katowice, Poland, Department of Biopharmacy, Jedności 8, 41-200 Sosnowiec, Poland.

To find better strategies to enhance the cytotoxic effect of paclitaxel (PTX) and lapatinib (LAP) against breast cancer cells, we analyzed the efficacy of a novel delivery system containing polylactide-co-poly(ethylene glycol) (PLA-PEG) filomicelles of over 100 nm in length and spherical micelles of approximately 20 nm in diameter. The ¹H NMR measurements confirmed the incorporation of PTX and LAP into micelles. Analysis of the drug release mechanism revealed the diffusion-controlled release of LAP and anomalous transport of PTX. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040169DOI Listing
April 2019
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Interpretation of Non-Clinical Data for Prediction of Human Pharmacokinetic Parameters: In Vitro-In Vivo Extrapolation and Allometric Scaling.

Pharmaceutics 2019 Apr 5;11(4). Epub 2019 Apr 5.

College of Pharmacy, CHA University, 335 Pangyo-ro, Bundang-gu, Seongnam-si, Gyeonggi-do 13488, Korea.

Extrapolation of pharmacokinetic (PK) parameters from in vitro or in vivo animal to human is one of the main tasks in the drug development process. Translational approaches provide evidence for go or no-go decision-making during drug discovery and the development process, and the prediction of human PKs prior to the first-in-human clinical trials. In vitro-in vivo extrapolation and allometric scaling are the choice of method for projection to human situations. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040168DOI Listing

Enhanced Transepithelial Permeation of Gallic Acid and (-)-Epigallocatechin Gallate across Human Intestinal Caco-2 Cells Using Electrospun Xanthan Nanofibers.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

Nano-BioScience Research Group, DTU-Food, Technical University of Denmark, Kemitorvet, B202, 2800 Kgs. Lyngby, Denmark.

Electrospun xanthan polysaccharide nanofibers (X) were developed as an encapsulation and delivery system of the poorly absorbed polyphenol compounds, gallic acid (GA) and (-)-epigallocatechin gallate (EGCG). Scanning electron microscopy was used to characterize the electrospun nanofibers, and controlled release studies were performed at pH 6.5 and 7. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040155DOI Listing

Modelling the Effect of Process Parameters on the Wet Extrusion and Spheronisation of High-Loaded Nicotinamide Pellets Using a Quality by Design Approach.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

Leicester School of Pharmacy, De Montfort University, Leicester LE1 9BH, UK.

The aim of the present study was to develop an alternative process to spray granulation in order to prepare high loaded spherical nicotinamide (NAM) pellets by wet extrusion and spheronisation. Therefore, a quality by design approach was implemented to model the effect of the process parameters of the extrusion-spheronisation process on the roundness, roughness and useable yield of the obtained pellets. The obtained results were compared to spray granulated NAM particles regarding their characteristics and their release profile in vitro after the application of an ileocolon targeted shellac coating. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040154DOI Listing
April 2019
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Simulation of Airway Deposition of an Aerosol Drug in COPD Patients.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

Energy Institute, Faculty of Mechanical Engineering, Brno University of Technology, Technicka 2896/2, 616 69 Brno, Czech Republic.

Medical aerosols are key elements of current chronic obstructive pulmonary disease (COPD) therapy. Therapeutic effects are conditioned by the delivery of the right amount of medication to the right place within the airways, that is, to the drug receptors. Deposition of the inhaled drugs is sensitive to the breathing pattern of the patients which is also connected with the patient's disease severity. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040153DOI Listing
April 2019
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Translational PBPK Modeling of the Protein Therapeutic and CD95L Inhibitor Asunercept to Develop Dose Recommendations for Its First Use in Pediatric Glioblastoma Patients.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

Clinical Pharmacy, Saarland University, 66123 Saarbrücken, Germany.

The protein therapeutic and CD95L inhibitor asunercept is currently under clinical investigation for the treatment of glioblastoma and myelodysplastic syndrome. The purpose of this study was to predict the asunercept pharmacokinetics in children and to give dose recommendations for its first use in pediatric glioblastoma patients. A physiologically-based pharmacokinetic (PBPK) model of asunercept in healthy and diseased adults was successfully developed using the available clinical Phase I and Phase II study data. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040152DOI Listing

Synthesis and Biological Evaluation of RGD⁻Cryptophycin Conjugates for Targeted Drug Delivery.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

Organic and Bioorganic Chemistry, Department of Chemistry, Bielefeld University, Universitätsstraße 25, DE-33615 Bielefeld, Germany.

Cryptophycins are potent tubulin polymerization inhibitors with picomolar antiproliferative potency in vitro and activity against multidrug-resistant (MDR) cancer cells. Because of neurotoxic side effects and limited efficacy in vivo, cryptophycin-52 failed as a clinical candidate in cancer treatment. However, this class of compounds has emerged as attractive payloads for tumor-targeting applications. Read More

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https://www.mdpi.com/1999-4923/11/4/151
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http://dx.doi.org/10.3390/pharmaceutics11040151DOI Listing
April 2019
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Drop-On-Powder 3D Printing of Tablets with an Anti-Cancer Drug, 5-Fluorouracil.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

School of Life Sciences, University of Sussex, Falmer, Brighton BN1 9QJ, UK.

This study reports the first case of an innovative drop-on-powder (DoP) three-dimensional (3D) printing technology to produce oral tablets (diameters of 10 mm and 13 mm) loaded with an anticancer model drug, 5-fluorouracil (FLU). For this study, a composition of the powder carrier containing CaSO₄ hydrates, vinyl polymer, and carbohydrate was used as the matrix former, whereas 2-pyrrolidone with a viscosity like water was used as a binding liquid or inkjet ink. All tablets were printed using a commercial ZCorp 3D printer with modification. Read More

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https://www.mdpi.com/1999-4923/11/4/150
Publisher Site
http://dx.doi.org/10.3390/pharmaceutics11040150DOI Listing
April 2019
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Feasibility Study of Mesoporous Silica Particles for Pulmonary Drug Delivery: Therapeutic Treatment with Dexamethasone in a Mouse Model of Airway Inflammation.

Pharmaceutics 2019 Apr 1;11(4). Epub 2019 Apr 1.

Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, 20520 Turku, Finland.

Diseases in the respiratory tract rank among the leading causes of death in the world, and thus novel and optimized treatments are needed. The lungs offer a large surface for drug absorption, and the inhalation of aerosolized drugs are a well-established therapeutic modality for local treatment of lung conditions. Nanoparticle-based drug delivery platforms are gaining importance for use through the pulmonary route. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040149DOI Listing

3D Printed Pellets (Miniprintlets): A Novel, Multi-Drug, Controlled Release Platform Technology.

Pharmaceutics 2019 Mar 29;11(4). Epub 2019 Mar 29.

Department of Pharmaceutics, UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.

Selective laser sintering (SLS) is a single-step three-dimensional printing (3DP) process that can be leveraged to engineer a wide array of drug delivery systems. The aim of this work was to utilise SLS 3DP, for the first time, to produce small oral dosage forms with modified release properties. As such, paracetamol-loaded 3D printed multiparticulates, termed miniprintlets, were fabricated in 1 mm and 2 mm diameters. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040148DOI Listing
March 2019
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Smart Nanovesicles for Drug Targeting and Delivery.

Pharmaceutics 2019 Mar 29;11(4). Epub 2019 Mar 29.

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, 00185 Rome, Italy.

Nanovesicles are highly-promising and versatile systems for the delivery and/or targeting of drugs, biomolecules and contrast agents [... Read More

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http://dx.doi.org/10.3390/pharmaceutics11040147DOI Listing
March 2019
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MRI of the Colon in the Pharmaceutical Field: The Future before us.

Pharmaceutics 2019 Mar 27;11(4). Epub 2019 Mar 27.

Nottingham Digestive Diseases Centre and National Institute for Health Research (NIHR) Nottingham Biomedical Research Centre, Nottingham University Hospitals NHS Trust and University of Nottingham, Nottingham NG7 2UH, UK.

Oral solid drug formulation is the most common route for administration and it is vital to increase knowledge of the gastrointestinal physiological environment to understand dissolution and absorption processes and to develop reliable biorelevant in vitro tools. In particular, colon targeted drug formulations have raised the attention of pharmaceutical scientists because of the great potential of colonic drug delivery. However, the distal bowel is still a relatively understudied part of the gastrointestinal tract. Read More

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http://dx.doi.org/10.3390/pharmaceutics11040146DOI Listing
March 2019
4 Reads