2,838 results match your criteria AAPS PharmSciTech[Journal]


Delivery Technologies for Orally Inhaled Products: an Update.

AAPS PharmSciTech 2019 Feb 19;20(3):117. Epub 2019 Feb 19.

College of Pharmacy, The University of Texas at Austin, 2409 West University Avenue, PHR 4.214, Austin, Texas, 78712, USA.

Orally inhaled products have well-known benefits. They allow for effective local administration of many drugs for the treatment of pulmonary disease, and they allow for rapid absorption and avoidance of first-pass metabolism of several systemically acting drugs. Several challenges remain, however, such as dosing limitations, low and variable deposition of the drug in the lungs, and high drug deposition in the oropharynx region. Read More

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http://dx.doi.org/10.1208/s12249-019-1314-2DOI Listing
February 2019

Delivery Systems as Vital Tools in Drug Repurposing.

AAPS PharmSciTech 2019 Feb 15;20(3):116. Epub 2019 Feb 15.

Advanced Drug Delivery Laboratory, Department of Pharmaceutical Sciences, College of Pharmacy, Northeast Ohio Medical University, 4209 State Route 44, Rootstown, Ohio, 44272, USA.

The process of developing an old drug for new indications is now a widely accepted strategy of shortening drug development time, reducing drug costs, and improving drug availability, especially for rare and neglected diseases. In this mini-review, we highlighted the impact of drug delivery systems in the fulfillment of crucial aspects of drug repurposing such as (i) maximizing the repurposed drug effects on a new target, (ii) minimizing off-target effects, (iii) modulating the release profiles of drug at the site of absorption, (iv) modulating the pharmacokinetics/in vivo biodistribution of the repurposed drug, (v) targeting/modulating drug retention at the sites of action, and (vi) providing a suitable platform for therapeutic application of combination drugs. Read More

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http://dx.doi.org/10.1208/s12249-019-1333-zDOI Listing
February 2019

Naringenin Cocrystals Prepared by Solution Crystallization Method for Improving Bioavailability and Anti-hyperlipidemia Effects.

AAPS PharmSciTech 2019 Feb 15;20(3):115. Epub 2019 Feb 15.

Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.

Naringenin exerts anti-inflammatory, hypolipidemic, and hepatoprotective effects; however, it shows low oral bioavailability because of poor water solubility. In this work, cocrystals of naringenin were formed to address these issues. Using the solution crystallization method, various naringenin cocrystals were prepared with different cocrystal coformers, including naringenin-nicotinamide, naringenin-isonicotinamide, naringenin-caffeine, naringenin-betaine, and naringenin-L-proline. Read More

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http://dx.doi.org/10.1208/s12249-019-1324-0DOI Listing
February 2019
1.776 Impact Factor

Xylan from Pineapple Stem Waste: a Potential Biopolymer for Colonic Targeting of Anti-inflammatory Agent Mesalamine.

AAPS PharmSciTech 2019 Feb 13;20(3):112. Epub 2019 Feb 13.

School of Pharmacy, Research Center for Nanosciences and Nanotechnology, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia.

We have successfully conjugated mesalamine (5-aminosalicylic acid, 5-ASA) with xylan, a biopolymer isolated from pineapple stem waste, to form xylan-5-ASA conjugate. The biopolymer was used to provide colon-targeting properties for 5-ASA, a golden standard anti-inflammatory agent commonly used for ulcerative colitis treatment. A series of data from FTIR spectroscopy, UV-Vis spectrophotometry, and HPLC confirmed the xylan-5-ASA conjugate formation. Read More

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http://dx.doi.org/10.1208/s12249-018-1205-yDOI Listing
February 2019
1.776 Impact Factor

Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation.

AAPS PharmSciTech 2019 Feb 13;20(3):113. Epub 2019 Feb 13.

Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK.

The aim of this study is to investigate the dissolution properties of poorly soluble drugs from their pure form and their amorphous formulation under physiological relevant conditions for oral administration based on surface dissolution ultraviolet (UV) imaging. Dissolution of two poorly soluble drugs (cefuroxime axetil and itraconazole) and their amorphous formulations (Zinnat and Sporanox) was studied with the Sirius Surface Dissolution Imager (SDI). Media simulating the fasted state conditions (compendial and biorelevant) with sequential media/flow rate change were used. Read More

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http://dx.doi.org/10.1208/s12249-019-1317-zDOI Listing
February 2019
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Investigating the Mechanism of L-Valine in Improving the Stability of Gabapentin Combining Chemical Analysis Experiments with Computational Pharmacy.

AAPS PharmSciTech 2019 Feb 13;20(3):114. Epub 2019 Feb 13.

Department of Nuclear Medicine, Shanghai Tenth People's Hospital, Shanghai, China.

The mechanism of L-Val on how to improve the stability of gabapentin (GBP) was described by the combination of chemical analysis experiments and computer simulations. Scanning electron microscope (SEM), powder X-ray diffraction (PXRD), and differential scanning calorimeter (DSC), coupled with attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR), were used to identify β-GBP prepared by rapid solvent removal method. The reaction barriers on crystal planes, β-GBP (100) and β-GBP (10-1), are smaller than α-GBP and γ-GBP, reaching 276. Read More

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http://dx.doi.org/10.1208/s12249-019-1312-4DOI Listing
February 2019

Design, Synthesis, and In Vitro Evaluation of Low Molecular Weight Protamine (LMWP)-Based Amphiphilic Conjugates as Gene Delivery Carriers.

AAPS PharmSciTech 2019 Feb 12;20(3):111. Epub 2019 Feb 12.

Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, P.O. Box: 91775-1365, Mashhad, Iran.

Development of efficient non-viral carriers is one of the major challenges of gene delivery. In the current study, we designed, synthesized, and evaluated the in vitro gene delivery efficiency of novel amphiphilic constructs composed of cholesterol and low molecular weight protamine (LMWP: VSRRRRRRGGRRRR) peptide. Vectors having both hydrophobic and hydrophilic moieties were evaluated in terms of particle size and charge, DNA condensation ability, cytotoxicity, and gene transfection efficiency. Read More

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http://dx.doi.org/10.1208/s12249-018-1235-5DOI Listing
February 2019

Nanofiber-Mediated Sustained Delivery of Triiodothyronine: Role in Angiogenesis.

AAPS PharmSciTech 2019 Feb 12;20(3):110. Epub 2019 Feb 12.

Biological Materials Laboratory, CSIR - Central Leather Research Institute, Chennai, 600020, India.

Angiogenesis is a vital component of the orchestrated wound healing cascade and tissue regeneration process, which has a therapeutic prominence in treatment of ischemic vascular diseases and certain cardiac conditions. Based on its eminence, several strategies using growth factors have been studied to initiate angiogenesis. However, growth factors are expensive and have short half-life. Read More

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http://dx.doi.org/10.1208/s12249-019-1326-yDOI Listing
February 2019

Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment.

AAPS PharmSciTech 2019 Feb 11;20(3):106. Epub 2019 Feb 11.

Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752-607, Porto Alegre, RS, 90610-000, Brazil.

Kaempferol (KPF), an important flavonoid, has been reported to exert antioxidant, anti-inflammatory, and anticancer activity. However, this compound has low water solubility and hence poor oral bioavailability. This work aims to prepare a solid dispersion (SD) of KPF using Poloxamer 407 in order to improve the water solubility, dissolution rate, and pharmacokinetic properties KPF. Read More

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http://dx.doi.org/10.1208/s12249-019-1318-yDOI Listing
February 2019
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Brillouin Light Scattering: Development of a Near Century-Old Technique for Characterizing the Mechanical Properties of Materials.

AAPS PharmSciTech 2019 Feb 11;20(3):109. Epub 2019 Feb 11.

Division of Pharmaceutics and Translational Therapeutics, College of Pharmacy, The University of Iowa, Iowa City, Iowa, 52242, United States of America.

Brillouin light scattering (BLS), a technique theoretically described nearly a century back by the French physicist Léon Brillouin in 1922, is a light-scattering method for determining the mechanical properties of materials. This inelastic scattering method is described by the Bragg diffraction of light from a propagating fluctuation in the local dielectric. These fluctuations arise spontaneously from thermally populated sound waves intrinsic to all materials, and thus BLS may be broadly applied to transparent samples of any phase. Read More

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http://dx.doi.org/10.1208/s12249-019-1311-5DOI Listing
February 2019

Lipopolysaccharide Polyelectrolyte Complex for Oral Delivery of an Anti-tubercular Drug.

AAPS PharmSciTech 2019 Feb 11;20(3):107. Epub 2019 Feb 11.

Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 2193, South Africa.

Anti-tuberculosis drug delivery has remained a challenge due to inconsistent bioavailability and inadequate sustained-release properties leading to treatment failure. To resolve these drawbacks, a lipopolysaccharide polyelectrolyte complex (PEC) encapsulated with rifampicin (RIF) (as the model drug) was fabricated, using the solvent injection technique (SIT), with soy lecithin (SLCT), and low-molecular-weight chitosan (LWCT). The average particle size and surface charge of RIF-loaded PEC particulates was 151. Read More

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http://dx.doi.org/10.1208/s12249-019-1310-6DOI Listing
February 2019
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Application of the SeDeM Expert System in Studies for Direct Compression Suitability on Mixture of Rhodiola Extract and an Excipient.

AAPS PharmSciTech 2019 Feb 11;20(3):105. Epub 2019 Feb 11.

Chongqing University of Science and Technology, No. 20, University City East Road, Chongqing, 401331, China.

The SeDeM expert system is used to reveal direct compression (DC) suitability of the active ingredients and excipients in preformulation. In this study, the system was used to predict compressibility of rhodiola extract (RhE) and its mixture with excipients. The parameter index (IP), parameter profile index (IPP), and good compressibility index (IGC) of RhE mixtures with different fillers were investigated. Read More

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http://dx.doi.org/10.1208/s12249-019-1320-4DOI Listing
February 2019

Enhanced Solubility of Alkaloids by Complexation with Polycarboxylic Materials for Controlled Release Formulations: Case of Peschiera fuchsiaefolia.

AAPS PharmSciTech 2019 Feb 11;20(3):108. Epub 2019 Feb 11.

Department of Chemistry, Research Chair on Enteric Dysfunctions "Allerdys", Pharmaqam and CERMO-FC Centers, Université du Québec à Montréal, C.P. 8888, Branch A, Montréal, Québec, H3C 3P8, Canada.

Malaria is a major public health problem with hundreds of thousands of deaths yearly. Extracts of Peschiera fuchsiaefolia (Pf), an Apocynaceae family plant, are used as malaria treatment by several populations. Artemisinin is another effective largely used antimalarial agent but susceptible to generate resistant forms of Plasmodium. Read More

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http://dx.doi.org/10.1208/s12249-019-1315-1DOI Listing
February 2019

Risedronate-Loaded Macroporous Gel Foam Enriched with Nanohydroxyapatite: Preparation, Characterization, and Osteogenic Activity Evaluation Using Saos-2 Cells.

AAPS PharmSciTech 2019 Feb 8;20(3):104. Epub 2019 Feb 8.

Department of Microbiology of Supplementary General Science, Faculty of Oral and Dental Medicine, Future University in Egypt, Cairo, Egypt.

The application of minimally invasive surgical techniques in the field of orthopedic surgery has created a growing need for new injectable synthetic materials that can be used for bone grafting. In this work, novel injectable thermosensitive foam was developed by mixing nHAP powder with a thermosensitive polymer with foaming power (Pluronic F-127) and loaded with a water-soluble bisphosphonate drug (risedronate) to promote osteogenesis. The foam was able to retain the porous structure after injection and set through temperature change of PF-127 solution to form gel inside the body. Read More

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http://dx.doi.org/10.1208/s12249-019-1292-4DOI Listing
February 2019

Spray-Dried PulmoSphere™ Formulations for Inhalation Comprising Crystalline Drug Particles.

AAPS PharmSciTech 2019 Feb 7;20(3):103. Epub 2019 Feb 7.

Respira Therapeutics, Inc., 155 Bovet Road #303, San Mateo, California, 94402, USA.

Over the past 20 years, solution-based spray dried powders have transformed inhaled product development, enabling aerosol delivery of a wider variety of molecules as dry powders. These include inhaled proteins for systemic action (e.g. Read More

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http://dx.doi.org/10.1208/s12249-018-1280-0DOI Listing
February 2019
1.776 Impact Factor

Effects of Polymer/Surfactant as Carriers on the Solubility and Dissolution of Fenofibrate Solid Dispersion.

AAPS PharmSciTech 2019 Feb 5;20(3):102. Epub 2019 Feb 5.

School of Pharmacy, China Medical University, 77 Puhe Road, Shenyang North New Area, Shenyang, 110122, Liaoning, China.

The purpose of this work is to investigate the effects of polymer/surfactant as carriers on the solubility and dissolution of fenofibrate solid dispersions (FF SDs) with the aid of systematic research on the physicochemical properties of the polymer/surfactant system and further highlight the importance of studying polymer/surfactant interaction in the preformulation. The critical micelle concentration (CMC) of sodium lauryl sulfate (SLS) and critical aggregation concentration (CAC) of polymer/SLS solutions were obtained through conductivity measurement. Meanwhile, surface tension, viscosity, morphology, and wettability of polymer/SLS with different weight ratios of SLS were analyzed to screen out the suitable content of SLS (weight%, 5% in carriers) incorporated in SDs. Read More

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http://dx.doi.org/10.1208/s12249-018-1273-zDOI Listing
February 2019
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Development and In Vivo Evaluation of Ziyuglycoside I-Loaded Self-Microemulsifying Formulation for Activity of Increasing Leukocyte.

AAPS PharmSciTech 2019 Feb 5;20(3):101. Epub 2019 Feb 5.

School of Pharmacy, Zunyi Medical University, West No. 6 Xuefu Road, Xinpu District, Zunyi, 563000, Guizhou, People's Republic of China.

Ziyuglycoside I (ZgI), a major effective ingredient of Sanguisorba officinalis L, has shown good activity in increasing leukocyte of myelosuppression mice. However, oral ZgI therapy has been deterred by poor bioavailability because of its low aqueous solubility and permeability. Our study was to develop ZgI-loaded self-microemulsifying drug delivery system (SMEDDS) and evaluate its intestinal absorption, and pharmacokinetic and pharmacodynamic activity for increasing leukocyte. Read More

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http://dx.doi.org/10.1208/s12249-019-1313-3DOI Listing
February 2019

Beta-carotene-Encapsulated Solid Lipid Nanoparticles (BC-SLNs) as Promising Vehicle for Cancer: an Investigative Assessment.

AAPS PharmSciTech 2019 Feb 5;20(3):100. Epub 2019 Feb 5.

University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Chandigarh, 160 014, India.

Beta-carotene (BC), a red-colored pigment found in plants and animals, is one of the most extensively investigated carotenoids due to its provitamin-A, antioxidant, and anticancer properties. The anticancer activity of BC through oral administration is severely affected due to its low bioavailability and oxidative degradation. The present study aimed to formulate and characterize solid lipid nanoparticles (SLNs) of BC for enhanced bioavailability and therapeutic efficacy. Read More

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http://dx.doi.org/10.1208/s12249-019-1301-7DOI Listing
February 2019
1 Read
1.776 Impact Factor

Preparation and Characterization of Syringic Acid-Loaded TPGS Liposome with Enhanced Oral Bioavailability and In Vivo Antioxidant Efficiency.

AAPS PharmSciTech 2019 Feb 4;20(3):98. Epub 2019 Feb 4.

Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang, 212013, China.

In this study, syringic acid-loaded TPGS liposome (SA-TPGS-Ls) was successfully prepared to improve oral bioavailability of syringic acid (SA). SA is a natural and notable antioxidant activity compound with its limited bioavailability ascribable to its poor aqueous solubility and fast elimination. Recently, TPGS has become a perfect molecular biomaterial in developing several carrier systems with sustained, controlled, and targeted the drug delivery. Read More

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http://dx.doi.org/10.1208/s12249-019-1290-6DOI Listing
February 2019
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Co-delivery of Doxorubicin and Ceramide in a Liposomal Formulation Enhances Cytotoxicity in Murine B16BL6 Melanoma Cell Lines.

AAPS PharmSciTech 2019 Feb 4;20(3):99. Epub 2019 Feb 4.

Department of Drug Discovery and Development, Harrison School of Pharmacy, Auburn University, Auburn, Alabama, 36849, USA.

This study reports co-delivery of doxorubicin (DOX) and ceramide in a liposomal system in B16BL6 melanoma cell lines for enhanced cytotoxic effects. Different types of ceramides (C6-ceramide, C8-ceramide, and C8-glucosylceramide) and lipids (1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE)) were considered in the preparation of liposomes. DOX was encapsulated within liposome, and ceramide was used as the component of the lipid bilayer. Read More

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http://dx.doi.org/10.1208/s12249-019-1316-0DOI Listing
February 2019
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Ultrasound-Assisted Facile Synthesis of Nanostructured Hybrid Vesicle for the Nasal Delivery of Indomethacin: Response Surface Optimization, Microstructure, and Stability.

AAPS PharmSciTech 2019 Jan 29;20(3):97. Epub 2019 Jan 29.

Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), New Delhi, India.

This work is devoted to design a novel nanostructured hybrid vesicle (NHV) made of lecithin and an acrylate/C10-C30 alkyl acrylate for the nasal delivery of a model active indomethacin (IND), and further to probe its microstructure, intermolecular interactions, drug release behavior, ex vivo permeation, and stability. NHVs were prepared by cavitation technology employing RSM-based central composite design (CCD). Amount of lecithin (X), power of ultrasound (X), and sonication time (X) were selected as three independent variables while the studied response included Z-Avg (nm), polydispersity index (PDI), and zeta potential (mV). Read More

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http://dx.doi.org/10.1208/s12249-018-1247-1DOI Listing
January 2019

Enhancement of Transdermal Delivery of Haloperidol via Spanlastic Dispersions: Entrapment Efficiency vs. Particle Size.

AAPS PharmSciTech 2019 Jan 29;20(3):95. Epub 2019 Jan 29.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Eini Street, Cairo, 11562, Egypt.

Haloperidol (Hal) is a well-known typical antipsychotic. Hepatic first pass metabolism leads to its limited oral bioavailability. This study aimed at enhancing transdermal delivery of Hal via spanlastic formulae. Read More

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http://dx.doi.org/10.1208/s12249-019-1306-2DOI Listing
January 2019

Enhanced Transdermal Drug Delivery by Sonophoresis and Simultaneous Application of Sonophoresis and Iontophoresis.

AAPS PharmSciTech 2019 Jan 29;20(3):96. Epub 2019 Jan 29.

Department of Chemical and Biomolecular Engineering, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea.

Transdermal drug delivery has advantages of topical drug administration compared to the other conventional administration methods. However, the skin penetration of drugs is limited by the barrier properties of stratum corneum. The combinational strategy has been investigated to improve the skin permeability of the drug. Read More

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http://dx.doi.org/10.1208/s12249-019-1309-zDOI Listing
January 2019
1 Read
1.776 Impact Factor

Assessing Aerosol Performance of a Dry Powder Carrier Formulation with Increasing Doses Using a Novel Inhaler.

AAPS PharmSciTech 2019 Jan 28;20(3):94. Epub 2019 Jan 28.

Respiratory Technology, the Woolcock Institute for Medical Research and Discipline of Pharmacology, Faculty of Medicine and Health, University of Sydney, Sydney, NSW, 2006, Australia.

This study aims to investigate the implications of loaded formulation mass on aerosol performance using a reservoir novel dry powder inhaler containing a custom dosing cup to deliver carrier-based formulation to the lungs. A 3D printed dosing cup with volume size of 133.04 mm was manufactured to allow for the progressive loading of different carrier formulation masses of 1% beclomethasone dipropionate BDP (w/w) formulation (10 to 60 mg, with increments of 10 mg), in a novel customizable DPI device. Read More

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http://dx.doi.org/10.1208/s12249-019-1302-6DOI Listing
January 2019
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Recent Perspectives in Hot Melt Extrusion-Based Polymeric Formulations for Drug Delivery: Applications and Innovations.

AAPS PharmSciTech 2019 Jan 28;20(3):92. Epub 2019 Jan 28.

State Key Laboratory of Biotherapy and Cancer Center, and Department of Neurosurgery, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, No. 17, Block 3, Southern Renmin Road, Chengdu, 610041, People's Republic of China.

Hot melt extrusion (HME), a technology which mixing the advantages of solid dispersion technology and mechanical preparation, is accepted in varied applications in pharmaceutical formulations. When combined with other techniques, such as nanotechnique, three-dimensional printing, and co-extrusion, HME becomes much more multifunctional in the application of drug delivery. While in most cases, polymers employed in HME are responsible for the final property of products. Read More

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http://dx.doi.org/10.1208/s12249-019-1300-8DOI Listing
January 2019

Effects of Drug-Polymer Interactions on Tablet Properties During the Development of Abuse-Deterrent Dosage Forms.

AAPS PharmSciTech 2019 Jan 28;20(3):93. Epub 2019 Jan 28.

Division of Pharmaceutics, College of Pharmacy, The University of Iowa, 115 S Grand Avenue, Iowa City, Iowa, 52242-1112, USA.

The objective of the present study is to understand the effects of drug-PEO interactions during the thermal treatment of polyethylene oxide (PEO)-based, directly compressed, abuse-deterrent formulations (ADFs). The drugs studied were dextromethorphan HBr monohydrate, ketoprofen, promethazine HCl, and anhydrous theophylline. Thermal treatment above the melting point of PEO resulted in tablets with higher crushing strength (> 500 N). Read More

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http://link.springer.com/10.1208/s12249-018-1221-y
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http://dx.doi.org/10.1208/s12249-018-1221-yDOI Listing
January 2019
7 Reads

Preparation, Pre-clinical and Clinical Evaluation of a Novel Rapidly Absorbed Celecoxib Formulation.

AAPS PharmSciTech 2019 Jan 25;20(2):90. Epub 2019 Jan 25.

NanGenex Inc., 47-49 Madarász Viktor str, Budapest, 1138, Hungary.

Celecoxib (Celebrex®) is the only widely used NSAID that selectively inhibits the COX-2 isoenzyme. Celebrex® is absorbed slowly in the fasted state and food intake further delays absorption. In this work, an amorphous water dispersible granule formulation of celecoxib is described with in vitro characterization, preclinical and clinical data. Read More

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http://dx.doi.org/10.1208/s12249-018-1270-2DOI Listing
January 2019

Matrix Tablets for Controlled Release of Drugs Incorporated Using Capillary Absorption.

AAPS PharmSciTech 2019 Jan 25;20(2):91. Epub 2019 Jan 25.

Faculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, SI-1000, Ljubljana, Slovenia.

Cost and time effectiveness make direct tableting still the favored method for tablet production. Among its most noticeable limitations in application is the non-uniformity (and/or inhomogeneities) in the contents of the resulting tablets, possibly leading to inconsistencies in required tablet properties. The efficiency of direct tableting is mostly affected by surface properties of the components to be tableted, which govern the final tablet mechanical and chemical properties and can influence the liquid capillary rise that the tablets exhibit after ingestion. Read More

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http://dx.doi.org/10.1208/s12249-019-1303-5DOI Listing
January 2019
2 Reads

Investigation of the Compatibility of the Skin PAMPA Model with Topical Formulation and Acceptor Media Additives Using Different Assay Setups.

AAPS PharmSciTech 2019 Jan 24;20(2):89. Epub 2019 Jan 24.

Almirall Hermal, R&D Dermatology, Scholtzstrasse 3, 21465, Reinbek, Germany.

The Skin Parallel Artificial Membrane Permeability Assay (PAMPA) is a 96-well plate-based skin model with an artificial membrane containing free fatty acid, cholesterol, and synthetic ceramide analogs to mimic the stratum corneum (SC) barrier. The current study evaluates the compatibility of lipophilic solvents/penetration enhancer, topical emulsions containing different emulsifier systems, and organic acceptor media additives with the artificial membrane of the assay. Additionally, different assay setups (standard setup: donor in bottom plate versus modified setup: donor in top plate) were compared. Read More

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http://dx.doi.org/10.1208/s12249-019-1305-3DOI Listing
January 2019

Paclitaxel-loaded Nanolipidic Carriers with Improved Oral Bioavailability and Anticancer Activity against Human Liver Carcinoma.

AAPS PharmSciTech 2019 Jan 23;20(2):87. Epub 2019 Jan 23.

Nanomedicine Research Lab, Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062, India.

The poorly water-soluble chemotherapeutic agents, paclitaxel (PTX), exhibit serious clinical side effects upon oral administration due to poor aqueous solubility and a high degree of toxic effects due to non-specific distribution to healthy tissues. In our efforts, we formulated biocompatible dietary lipid-based nanostructured lipidic carriers (NLCs) to enhance the oral bioavailability of PTX for treatment of the liver cancer. A three-factor, three-level Box-Behnken design was employed for formulation and optimization of PTX-loaded NLC formulations. Read More

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http://link.springer.com/10.1208/s12249-019-1304-4
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http://dx.doi.org/10.1208/s12249-019-1304-4DOI Listing
January 2019
4 Reads

In Vitro Cytotoxicity and Bioavailability of Ginsenoside-Modified Nanostructured Lipid Carrier Containing Curcumin.

AAPS PharmSciTech 2019 Jan 23;20(2):88. Epub 2019 Jan 23.

College of Pharmacy, Gachon University, 191 Hambakmoero, Yeonsu-gu, Incheon, 21936, South Korea.

Our aim was to investigate the cellular uptake, in vitro cytotoxicity and bioavailability of ginsenoside-modified nanostructured lipid carrier loaded with curcumin (G-NLC). The formulation was prepared by melt emulsification technique, in which water was added to the melted lipids and homogenized to give a uniform suspension of NLC (without ginsenoside) and G-NLC. Cellular uptake of curcumin in two colon cancer cell lines (HCT116 and HT29) was increased when administered using both NLC and G-NLC compared to control (curcumin dissolved into DMSO) as measured by fluorescence microscopy. Read More

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http://link.springer.com/10.1208/s12249-019-1295-1
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http://dx.doi.org/10.1208/s12249-019-1295-1DOI Listing
January 2019
6 Reads

Sustained Release Bilayer Tablet of Ibuprofen and Phenylephrine Hydrochloride: Preparation and Pharmacokinetics in Beagle Dogs.

AAPS PharmSciTech 2019 Jan 23;20(2):86. Epub 2019 Jan 23.

School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China.

Cold is a global common infectious disease accompanied by symptoms such as headache and stuffy nose. Ibuprofen (IBU) and phenylephrine hydrochloride (PE) were commonly used for common cold due to their different effects in relieving fever and the main symptoms such as nasal congestion and high sinus pressure. However, the commercial tablets of IBU and PE have to be administered 2 to 3 times per day due to their short half-life, with inconvenience for patient and fluctuations of plasma concentration. Read More

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http://dx.doi.org/10.1208/s12249-018-1271-1DOI Listing
January 2019
7 Reads
1.776 Impact Factor

Novel Inhalable Ciprofloxacin Dry Powders for Bronchiectasis Therapy: Mannitol-Silk Fibroin Binary Microparticles with High-Payload and Improved Aerosolized Properties.

AAPS PharmSciTech 2019 Jan 23;20(2):85. Epub 2019 Jan 23.

School of Pharmaceutical Sciences, Sun Yat-Sen University, No.132 Waihuandong Road, University Town, Guangzhou, 510006, People's Republic of China.

Non-cystic fibrosis bronchiectasis (NCFB) is a chronic respiratory disease associated with the high morbidity and mortality. Long-term intermittent therapy by inhalable antibiotics has recently emerged as an effective approach for NCFB treatment. However, the effective delivery of antibiotics to the lung requires administering a high dose to the site of infection. Read More

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http://link.springer.com/10.1208/s12249-019-1291-5
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http://dx.doi.org/10.1208/s12249-019-1291-5DOI Listing
January 2019
5 Reads

Lipid-Based Nanocarriers for Lymphatic Transportation.

AAPS PharmSciTech 2019 Jan 23;20(2):83. Epub 2019 Jan 23.

Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Vishwavidyalaya, Sagar, M.P., 470003, India.

The effectiveness of any drug is dependent on to various factors like drug solubility, bioavailability, selection of appropriate delivery system, and proper route of administration. The oral route for the delivery of drugs is undoubtedly the most convenient, safest and has been widely used from past few decades for the effective delivery of drugs. However, despite of the numerous advantages that oral route offers, it often suffers certain limitations like low bioavailability due to poor water solubility as well as poor permeability of drugs, degradation of the drug in the physiological pH of the stomach, hepatic first-pass metabolism, etc. Read More

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http://link.springer.com/10.1208/s12249-019-1293-3
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http://dx.doi.org/10.1208/s12249-019-1293-3DOI Listing
January 2019
3 Reads
1.776 Impact Factor

Methods to Assess Mixing of Pharmaceutical Powders.

AAPS PharmSciTech 2019 Jan 23;20(2):84. Epub 2019 Jan 23.

Faculty of Engineering, Western University, London, Ontario, N6A 5B9, Canada.

The pharmaceutical manufacturing process consists of several steps, each of which must be monitored and controlled to ensure quality standards are met. The level of blending has an impact on the final product quality; therefore, it is important to be able to monitor blending progress and identify an end-point. Currently, the pharmaceutical industry assesses blend content and uniformity through the extraction of samples using thief probes followed by analytical methods, such as spectroscopy, to determine the sample composition. Read More

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http://dx.doi.org/10.1208/s12249-018-1286-7DOI Listing
January 2019

Enhanced Oral Absorption of Amisulpride Via a Nanostructured Lipid Carrier-Based Capsules: Development, Optimization Applying the Desirability Function Approach and In Vivo Pharmacokinetic Study.

AAPS PharmSciTech 2019 Jan 16;20(2):82. Epub 2019 Jan 16.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El Aini, Cairo, 12411, Egypt.

Amisulpride (AMS), a second generation antipsychotic, suffers from low oral bioavailability (48%). This might be due to its pH-dependent solubility or being a substrate of P-glycoprotein efflux pump. Nanostructured lipid carriers (NLCs) were proposed in this study to enhance the oral absorption of AMS. Read More

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http://dx.doi.org/10.1208/s12249-018-1283-xDOI Listing
January 2019
1 Read

Folate-Functionalized Thiomeric Nanoparticles for Enhanced Docetaxel Cytotoxicity and Improved Oral Bioavailability.

AAPS PharmSciTech 2019 Jan 15;20(2):81. Epub 2019 Jan 15.

Riphah Institute of Pharmaceutical Sciences, Riphah International University, Lahore Campus, Lahore, Pakistan.

To achieve remotely directed delivery of anticancer drugs, surface-decorated nanoparticles with ligands are reported. In this study, folic acid- and thiol-decorated chitosan nanoparticles loaded with docetaxel (DTX-NPs) were prepared for enhanced cellular internalization in cancer cells and improved oral absorption. The DTX-NPs were explored through in vitro and in vivo parameters for various parameters. Read More

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http://dx.doi.org/10.1208/s12249-019-1297-zDOI Listing
January 2019
2 Reads

Abuse Deterrent Immediate Release Egg-Shaped Tablet (Egglets) Using 3D Printing Technology: Quality by Design to Optimize Drug Release and Extraction.

AAPS PharmSciTech 2019 Jan 15;20(2):80. Epub 2019 Jan 15.

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, St. Albert Hall, B18B, 8000 Utopia Parkway, Queens, New York, 11439, USA.

Opioid abuse is a growing problem and has become a national health crisis over the past decade in the USA. Oral ingestion, snorting, and injection are the most commonly employed routes of abuse for an immediate release product. To circumvent these issues, we have developed an egg-shaped tablet (egglet) using fused deposition modeling (FDM) 3D printing technology. Read More

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http://dx.doi.org/10.1208/s12249-019-1298-yDOI Listing
January 2019
9 Reads

Effect of Mild Hyperthermia on Transdermal Absorption of Nicotine from Patches.

AAPS PharmSciTech 2019 Jan 11;20(2):77. Epub 2019 Jan 11.

Department of Pharmaceutics and Drug Delivery, University of Mississippi, Oxford, Mississippi, 38677, USA.

Application of heat (hyperthermic conditions) on skin is known to enhance drug transfer and facilitate skin penetration of molecules. The aim of this work was to study the effect of hyperthermia on the drug release and skin permeation from nicotine transdermal patches. The drug release and skin permeation were characterized by in vitro release test and in vitro permeation test. Read More

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http://dx.doi.org/10.1208/s12249-019-1299-xDOI Listing
January 2019
2 Reads

Development and Characterization of a Self-Nanoemulsifying Drug Delivery System Comprised of Rice Bran Oil for Poorly Soluble Drugs.

AAPS PharmSciTech 2019 Jan 11;20(2):78. Epub 2019 Jan 11.

Laboratory of Pharmaceutical Technology, Department of Pharmacy, Aristotle University of Thessaloniki, 54124, Thessaloniki, Greece.

Poor aqueous solubility and low bioavailability are limiting factors in the oral delivery of lipophilic drugs. In a formulation approach to overcome these limitations, rice bran (RB) oil was evaluated as drug carrier in the development of self-nanoemulsifying drug delivery systems (SNEDDS). The performance of RB in formulations incorporating Kolliphor RH40 or Kolliphor EL as surfactants and Transcutol HP as cosolvent was compared to a common oil vehicle, corn oil (CO). Read More

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http://link.springer.com/10.1208/s12249-018-1274-y
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http://dx.doi.org/10.1208/s12249-018-1274-yDOI Listing
January 2019
8 Reads
1.776 Impact Factor

Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery.

AAPS PharmSciTech 2019 Jan 11;20(2):79. Epub 2019 Jan 11.

Laboratoire de Chimie Agro-industrielle (LCA), INRA, INPT, Université de Toulouse, Toulouse, France.

The potential value of succinylated soy protein (SPS) as a wall material for the encapsulation of ibuprofen (IBU), a model hydrophobic drug, by spray-drying was investigated. A succinylation rate of 93% was obtained for soy protein isolate, with a molar ratio of 1/1.5 (NH/succinic anhydride). Read More

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http://dx.doi.org/10.1208/s12249-018-1250-6DOI Listing
January 2019
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Optimal Selection of Incoming Materials from the Inventory for Achieving the Target Drug Release Profile of High Drug Load Sustained-Release Matrix Tablet.

AAPS PharmSciTech 2019 Jan 11;20(2):76. Epub 2019 Jan 11.

Research Center of TCM Information Engineering, Beijing University of Chinese Medicine, Beijing, 100029, China.

In the pharmaceutical process, raw material (including APIs and excipients) variability can be delivered to the final product, and lead to batch-to-batch and lot-to-lot variances in its quality, finally impacting the efficacy of the drug. In this paper, the Panax notoginseng saponins (PNS) sustained-release matrix tablet was taken as the model formulation. Hydroxypropyl methylcellulose with the viscosity of 4000 mPa·s (HPMCK4M) from different vendors and batches were collected and their physical properties were characterized by the SeDeM methodology. Read More

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http://dx.doi.org/10.1208/s12249-018-1268-9DOI Listing
January 2019
2 Reads
1.776 Impact Factor

An Evaluation of Curcumin-Encapsulated Chitosan Nanoparticles for Transdermal Delivery.

AAPS PharmSciTech 2019 Jan 10;20(2):69. Epub 2019 Jan 10.

Center for Cancer and Stem Cell Research, International Medical University, No.126, Jalan Jalil Perkasa 19, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.

Curcumin-loaded chitosan nanoparticles were synthesised and evaluated in vitro for enhanced transdermal delivery. Zetasizer® characterisation of three different formulations of curcumin nanoparticles (Cu-NPs) showed the size ranged from 167.3 ± 3. Read More

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http://link.springer.com/10.1208/s12249-018-1279-6
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http://dx.doi.org/10.1208/s12249-018-1279-6DOI Listing
January 2019
12 Reads
1.776 Impact Factor

Oral Delivery of Methylthioadenosine to the Brain Employing Solid Lipid Nanoparticles: Pharmacokinetic, Behavioral, and Histopathological Evidences.

AAPS PharmSciTech 2019 Jan 10;20(2):74. Epub 2019 Jan 10.

Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt., Ajmer, Rajasthan, 305817, India.

The present study aimed to orally deliver methylthioadenosine (MTA) to the brain employing solid lipid nanoparticles (SLNs) for the management of neurological conditions like multiple sclerosis. The stearic acid-based SLNs were below 100 nm with almost neutral zeta potential and offered higher drug entrapment and drug loading. Cuprizone-induced demyelination model in mice was employed to mimic the multiple sclerosis-like conditions. Read More

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http://dx.doi.org/10.1208/s12249-019-1296-0DOI Listing
January 2019
3 Reads
1.776 Impact Factor

Application of Texture Analysis Technique in Formulation Development of Lyophilized Orally Disintegrating Tablets Containing Mannitol, Polyvinylpyrrolidone and Amino Acids.

AAPS PharmSciTech 2019 Jan 10;20(2):71. Epub 2019 Jan 10.

Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, Leicester, UK.

Orally disintegrating tablets (ODTs) attract a great attention as this easy swallowing dosage form often improves patient compliance. In the current work, orally disintegrating tablets comprising mannitol, polyvinylpyrrolidone (PVP) and an amino acid (alanine, glycine or serine) with various PVP-to-amino acid ratios were formulated. The combination of mannitol and an amino acid was aimed to use the advantages of mannitol, the matrix-supporting and disintegration agent, and to reduce the total amount of sugar/polyol in tablets. Read More

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http://dx.doi.org/10.1208/s12249-018-1269-8DOI Listing
January 2019
1 Read

Formulation and Evaluation of a Novel Oral Oil-Based Suspension Using Micro-environmental pH-Modifying Solid Dispersion.

AAPS PharmSciTech 2019 Jan 10;20(2):75. Epub 2019 Jan 10.

The Department of Veterinary Parasitology, College of Veterinary Medicine, China Agricultural University, Hai Dian District, Beijing, 100193, China.

Drugs with pH-dependent solubility that have poor water solubility can be identified in the drug discovery pipeline. Some of them have poor oral absorption, which can result in insufficient efficacy. Micro-environmental pH-modifying solid dispersion (micro pHm SD) is a promising approach to overcome the poor oral absorption of these drugs. Read More

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http://dx.doi.org/10.1208/s12249-018-1222-xDOI Listing
January 2019
3 Reads

Detailed Morphological Characterization of Nanocrystalline Active Ingredients in Solid Oral Dosage Forms Using Atomic Force Microscopy.

AAPS PharmSciTech 2019 Jan 10;20(2):70. Epub 2019 Jan 10.

Division of Drugs, National Institute of Health Sciences, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki, Kanagawa, 210-9501, Japan.

The characterization of nanocrystalline active ingredients in multicomponent formulations for the design and manufacture of products with increased bioavailability is often challenging. The purpose of this study is to develop an atomic force microscopy (AFM) imaging method for the detailed morphological characterization of nanocrystalline active ingredients in multicomponent oral formulations. The AFM images of aprepitant and sirolimus nanoparticles in aqueous suspension show that their sizes are comparable with those measured using dynamic light scattering (DLS) analysis. Read More

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http://dx.doi.org/10.1208/s12249-018-1259-xDOI Listing
January 2019
1 Read

Pediatric Formulations: Knowledge Gaps Limiting the Expedited Preclinical to Clinical Translation in Children.

AAPS PharmSciTech 2019 Jan 10;20(2):73. Epub 2019 Jan 10.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

Traditionally, drug discovery and development research have been primarily focused on the mitigation of disease treatment for the general adult population, often overlooking the medical needs of pediatric patients. While remarkable progress toward the discovery of better medicines has been made, the pharmacological differences between children and adults are often neglected as part of the translation process. In fact, until recently, children have been considered therapeutic orphans due to the lack of significant drug discovery, formulation development, and dosage form design specifically tailored for pediatric patients. Read More

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http://link.springer.com/10.1208/s12249-018-1253-3
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http://dx.doi.org/10.1208/s12249-018-1253-3DOI Listing
January 2019
7 Reads

Distribution of Protein Content and Number of Aggregates in Monoclonal Antibody Formulation After Large-Scale Freezing.

AAPS PharmSciTech 2019 Jan 10;20(2):72. Epub 2019 Jan 10.

Institute of Physical Chemistry, University Innsbruck, Innrain 52c, 6020, Innsbruck, Austria.

Cryoconcentration of an in-house IgG and number of aggregates in a formulation containing trehalose were determined in dependence on freezing protocol and volume. Morphology changes of ice crystals depending on cooling rates were captured by optical cryomicroscopy (OCM) images. UV-Vis and affinity chromatography (ALC) was used to determine protein content and size-exclusion chromatography (SEC) for detection of aggregates. Read More

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http://dx.doi.org/10.1208/s12249-018-1281-zDOI Listing
January 2019
2 Reads

Aggregation Behavior of Medium Chain Fatty Acids Studied by Coarse-Grained Molecular Dynamics Simulation.

AAPS PharmSciTech 2019 Jan 9;20(2):61. Epub 2019 Jan 9.

Dept of Pharmacy and the Swedish Drug Delivery Forum (SDDF), Uppsala University, Uppsala Biomedical Center, P.O. Box 580, SE-751 23, Uppsala, Sweden.

Medium chain fatty acids (MCFA) are digestion products of lipid-rich food and lipid-based formulations, and they are used as transient permeability enhancers in formulation of poorly permeable compounds. These molecules may promote drug absorption by several different processes, including solubilization, increased membrane fluidity, and increased paracellular transport through opening of the tight junctions. Therefore, understanding the aggregation behavior of MCFAs is important. Read More

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http://link.springer.com/10.1208/s12249-018-1289-4
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http://dx.doi.org/10.1208/s12249-018-1289-4DOI Listing
January 2019
11 Reads