3,210 results match your criteria AAPS PharmSciTech[Journal]


Relationship Between Geometric and Aerodynamic Particle Size Distributions in the Formulation of Solution and Suspension Metered-Dose Inhalers.

AAPS PharmSciTech 2020 May 26;21(5):158. Epub 2020 May 26.

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

The relationship between the geometric particle size distribution (GPSD) and the aerodynamic particle size distribution (APSD) of commercial solution and suspension metered-dose inhaler (MDI) formulations was assessed to clarify the use of GPSD to estimate the APSD. The size distribution of particles discharged from four suspension and four solution MDIs was measured using the Inas®100 light-scattering spectrometer and a Next Generation Impactor. The conversion factor was calculated by measuring the GPSD and APSD of MDIs. Read More

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http://dx.doi.org/10.1208/s12249-020-01675-3DOI Listing

Development of Dry Powder Inhaler Patient Interfaces for Improved Aerosol Delivery to Children.

AAPS PharmSciTech 2020 May 25;21(5):157. Epub 2020 May 25.

Department of Mechanical and Nuclear Engineering, Virginia Commonwealth University, 401 West Main Street, P.O. Box 843015, Richmond, Virginia, 23284-3015, USA.

The objective of this study was to explore different internal flow passages in the patient interface region of a new air-jet-based dry powder inhaler (DPI) in order to minimize device and extrathoracic aerosol depositional losses using computational fluid dynamics (CFD) simulations. The best-performing flow passages were used for oral and nose-to-lung (N2L) aerosol delivery in pediatric extrathoracic airway geometries consistent with a 5-year-old child. Aerosol delivery conditions were based on a previously developed and tested air-jet DPI device and included a base flow rate of 13. Read More

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http://dx.doi.org/10.1208/s12249-020-01667-3DOI Listing

Continuous Manufacturing of a Polymer Stabilized Emulsion Monitored with Process Analytical Technology.

AAPS PharmSciTech 2020 May 24;21(5):154. Epub 2020 May 24.

Laboratory of Pharmaceutical Process Analytical Technology, Ghent University, Ghent, Belgium.

Moving from batch to continuous manufacturing (CM) requires implementation of process analytical technology (PAT), as it is crucial to monitor and control these processes. CM of semi-solids has been demonstrated but implementation of a broader range of PAT tools with in- or on-line process interfacing at the end of the CM line has not been demonstrated. The goal of this work was to continuously manufacture creams and to investigate whether in- and on-line measurement of viscosity, changes in the concentration of active pharmaceutical ingredient (API), and pH could be used to support optimization of a model cream product. Read More

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http://dx.doi.org/10.1208/s12249-020-01704-1DOI Listing

Meloxicam Carrier Systems Having Enhanced Release and Aqueous Wettability Prepared Using Micro-suspensions in Different Liquid Media.

AAPS PharmSciTech 2020 May 24;21(5):155. Epub 2020 May 24.

Department of Organic Technology, University of Chemistry and Technology, Technická 5, 166 28, Prague 6, Czech Republic.

One of the conventional methods of alleviating the problem of poor drug solubility is the particle size reduction. The efficiency of this approach depends on successful formulation suppressing the drug agglomeration. The aim of this study was to circumvent the dissolution problems of model hydrophobic meloxicam drug (MLX) by using liquid media of different wetting capacity to comminute and formulate a rapidly dissolving carrier system without the use of surfactants. Read More

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http://dx.doi.org/10.1208/s12249-020-01701-4DOI Listing

Proniosomal Microcarriers: Impact of Constituents on the Physicochemical Properties of Proniosomes as a New Approach to Enhance Inhalation Efficiency of Dry Powder Inhalers.

AAPS PharmSciTech 2020 May 24;21(5):156. Epub 2020 May 24.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, El-Shahid/Shehata Ahmed Hijaz St., Beni-Suef, Egypt.

Proniosomes are free-flowing systems with coating carriers, which developed as a method for improving the drug flow and pulmonary delivery. Extensive research on proniosomes was done to enhance the dry powder inhalers (DPI)'s inhalation performance. This research aimed at studying the impact of lactose-mannitol mixture additives on the proniosome's physicochemical properties as a method for improving the inhalation efficiency of DPI. Read More

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http://dx.doi.org/10.1208/s12249-020-01705-0DOI Listing

In and Beyond COVID-19: US Academic Pharmaceutical Science and Engineering Community Must Engage to Meet Critical National Needs.

AAPS PharmSciTech 2020 May 24;21(5):153. Epub 2020 May 24.

The National Institute for Pharmaceutical Technology and Education (NIPTE), Inc., Minneapolis, Minnesota, 55414, USA.

The supply of affordable, high-quality pharmaceuticals to US patients has been on a critical path for decades. In and beyond the COVID-19 pandemic, this critical path has become tortuous. To regain reliability, reshoring of the pharmaceutical supply chain to the USA is now a vital national security need. Read More

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http://dx.doi.org/10.1208/s12249-020-01718-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7245992PMC

EGFR Targeted Paclitaxel and Piperine Co-loaded Liposomes for the Treatment of Triple Negative Breast Cancer.

AAPS PharmSciTech 2020 May 21;21(5):151. Epub 2020 May 21.

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (BHU), Varanasi, 221005, India.

Triple-negative breast (TNBC) cancer that is upregulated with epidermal growth factor receptor (EGFR), and devoid of both the hormonal receptors and epidermal growth factor receptor 2 (HER 2), has led to a concept of treating TNBC with EGFR-targeted therapeutics. The combination of paclitaxel (PTX) and piperine (PIP) may improve the bioavailability of paclitaxel for cancer therapy. TPGS (vit E-PEG 1000-succinate)-coated liposomes were prepared with PTX alone or in combination with PIP, and either with (targeted) or without (non-targeted) cetuximab (CTX) conjugation. Read More

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http://dx.doi.org/10.1208/s12249-020-01671-7DOI Listing

Understanding Concomitant Physical and Chemical Transformations of Simvastatin During Dry Ball Milling.

AAPS PharmSciTech 2020 May 21;21(5):152. Epub 2020 May 21.

Research Center Pharmaceutical Engineering (RCPE) GmbH, Inffeldgasse 13, 8010, Graz, Austria.

The present study investigates concomitant processes of solid-state disordering and oxidation of simvastatin during milling. The separate dry ball milling of crystalline and amorphous powders of simvastatin were conducted at ambient temperature for 10 and 60 min each. The relative crystallinity was determined using X-ray scattering and oxidative degradation was analyzed using liquid chromatography. Read More

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http://dx.doi.org/10.1208/s12249-020-01687-zDOI Listing

Robustness of Controlled Release Tablets Based on a Cross-linked Pregelatinized Potato Starch Matrix.

AAPS PharmSciTech 2020 May 20;21(5):148. Epub 2020 May 20.

University of Lille, Inserm, CHU Lille, U1008, 59000, Lille, France.

The aim of this study was to evaluate the potential of a cross-linked pregelatinized potato starch (PREGEFLO® PI10) as matrix former for controlled release tablets. Different types of tablets loaded with diprophylline, diltiazem HCl or theophylline were prepared by direct compression of binary drug/polymer blends. The drug content was varied from 20 to 50%. Read More

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http://dx.doi.org/10.1208/s12249-020-01674-4DOI Listing

The Effect of Enzymes and Sodium Lauryl Sulfate on the Surface Tension of Dissolution Media: Toward Understanding the Solubility and Dissolution of Carvedilol.

AAPS PharmSciTech 2020 May 20;21(5):146. Epub 2020 May 20.

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, P.O. Box 130, Amman, 11733, Jordan.

The objective of this work was to study the effect of the physiologically relevant enzymes pepsin, pancreatin, and the synthetic surfactant sodium lauryl sulfate (SLS) on the surface tension of the dissolution media and the solubility and dissolution of the weakly basic drug carvedilol. Compendial dissolution media and buffer solutions that simulate the gastrointestinal fluid, prepared with and without the addition of SLS, were used in this study. The surface tension of the dissolution media; critical micelle concentration (CMC) of SLS in buffer solutions; and size, polydispersity index, and zeta potential of SLS micelles loading carvedilol were determined. Read More

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http://dx.doi.org/10.1208/s12249-020-01683-3DOI Listing

Effect of Genotype and Sex of the Host on the Bioavailability of Novel Albendazole Microcrystals Based on Chitosan and Cellulose Derivatives.

AAPS PharmSciTech 2020 May 20;21(5):149. Epub 2020 May 20.

IQUIR-CONICET, Suipacha 570, S2002LRK, Rosario, Argentina.

Albendazole (ABZ), an anthelmintic compound widely used in the treatment of systemic nematode infections, is included in the list of class II drugs based on the Biopharmaceutical Classification System. ABZ has limited effectiveness due to its poor water solubility and consequent low bioavailability. Bioavailability of novel ABZ microcrystals based on hydroxyethylcellulose (S4A) or chitosan (S10A) was studied in male and female mice of two inbred lines, from the murine CBi-IGE model of trichinellosis, differing in susceptibility to this parasitosis (line CBi/L, resistant; line CBi+, susceptible). Read More

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http://dx.doi.org/10.1208/s12249-020-01692-2DOI Listing

Development of Morin-Loaded Nanoemulsions Containing Various Polymers; Role of Polymers in Formulation Properties and Bioavailability.

AAPS PharmSciTech 2020 May 20;21(5):150. Epub 2020 May 20.

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

Emulsions for oral delivery are not suitable for sustained drug absorption because such preparations diffuse rapidly in the gastrointestinal (GI) tract after oral administration. In order to generate sustained drug absorption and increase oral bioavailability, various polymers were added to a morin (MO) nanoemulsion to improve retention in the GI tract and alter the surface properties of oil droplets in the nanoemulsion. The influence of these polymers on the formulation properties was investigated. Read More

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http://dx.doi.org/10.1208/s12249-020-01670-8DOI Listing

Evaluation of the Sensitivity and Robustness of Modified Chi-Square Ratio Statistic for Cascade Impactor Equivalence Testing Through Monte Carlo Simulations.

AAPS PharmSciTech 2020 May 20;21(5):147. Epub 2020 May 20.

Department of Pharmaceutics, College of Pharmacy, University of Florida, Box 100494, Gainesville, Florida, 32610, USA.

The objective of this work was to study the performance of the modified chi-square ratio statistic (mCSRS test) proposed for cascade impactor (CI) profile equivalence testing. The test (T) and reference (R) CI profile datasets were generated from different typical CI profile patterns either with or without inter-site correlation (ISC) through Monte Carlo simulations. The mCSRS test pass rate outcome employing previously published critical values was compared with that of critical values derived from different types of datasets. Read More

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http://dx.doi.org/10.1208/s12249-020-01664-6DOI Listing

Stimulatory Effects of Soluplus® on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment.

AAPS PharmSciTech 2020 May 19;21(5):145. Epub 2020 May 19.

Pharmacy, Ministry of Defense, King Abdulaziz Air Base Hospital, Dhahran, Saudi Arabia.

The present study demonstrates the solubility and dissolution of flufenamic acid (FLF)/β-cyclodextrin (β-CD)/Soluplus® supramolecular ternary inclusion complex. The binary and ternary inclusion complexes were prepared using solvent evaporation and the microwave irradiation method. The prepared inclusion complexes were evaluated for physicochemical characterization and anti-inflammatory activity using a murine paw edema mol. Read More

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http://dx.doi.org/10.1208/s12249-020-01684-2DOI Listing

Correction to: Development of Nanocrystal Ziprasidone Orally Disintegrating Tablets: Optimization by Using Design of Experiment and In Vitro Evaluation.

AAPS PharmSciTech 2020 May 19;21(5):144. Epub 2020 May 19.

Department of Pharmaceutical Technology, Faculty of Pharmacy Gazi University, Ankara, Turkey.

Several typos occurred during the production process and captions were misplaced. The corrected captions for Picture 1, Fig. 6-9 are below. Read More

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http://dx.doi.org/10.1208/s12249-020-01703-2DOI Listing

Spray-Dried Proliposomes: an Innovative Method for Encapsulation of Rosmarinus officinalis L. Polyphenols.

AAPS PharmSciTech 2020 May 18;21(5):143. Epub 2020 May 18.

Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café s/n, Ribeirão Preto, SP, 14040-903, Brazil.

This work aims to improve the functionality of Rosmarinus officinalis L. (rosemary) polyphenols by encapsulation in an optimized proliposome formulation. A 2 Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture content (X); water activity (A); concentration and retention of rosemary polyphenols-rosmarinic acid (ROA), carnosol (CAR), and carnosic acid (CNA); and recovery of spray-dried proliposomes (SDP). Read More

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http://dx.doi.org/10.1208/s12249-020-01668-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7235052PMC

Optimization of Thymoquinone-Loaded Coconut Oil Nanostructured Lipid Carriers for the Management of Ethanol-Induced Ulcer.

AAPS PharmSciTech 2020 May 17;21(5):137. Epub 2020 May 17.

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, P.O.Box: 80260, Jeddah, 21589, Saudi Arabia.

In the global incidence of peptic ulcer, with the associated rates of hospitalizations and mortality are increasing, in the United States, peptic ulcer disease affects approximately 4.6 million people annually, with an estimated 10% of the US population having evidence of a duodenal ulcer. The present research aims to find a novel treatment for ethanol induced ulcer by loading thymoquinone (TQ) on a nanostructured lipid carrier (NLC), using Compritol® 888 and coconut oil. Read More

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http://dx.doi.org/10.1208/s12249-020-01693-1DOI Listing

An NMR Protocol for In Vitro Paclitaxel Release from an Albumin-Bound Nanoparticle Formulation.

AAPS PharmSciTech 2020 May 17;21(5):136. Epub 2020 May 17.

Division of Complex Drug Analysis, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, Maryland, 20993, USA.

The paclitaxel protein-bound particles for injectable suspension (marketed under the brand name Abraxane®) contains nanosized complexes of paclitaxel and albumin. The molecular interaction between paclitaxel and albumin within the higher-order nanostructure is analytically challenging to assess, as is any correlation of differences to differences in therapeutic effect. However, because the higher-order nanostructures may affect the paclitaxel release, a suitable in vitro assay to detect potential differences in paclitaxel release between comparator lots and products is desirable. Read More

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http://dx.doi.org/10.1208/s12249-020-01669-1DOI Listing

The Application of Coarse-Grained Molecular Dynamics to the Evaluation of Liposome Physical Stability.

AAPS PharmSciTech 2020 May 17;21(5):138. Epub 2020 May 17.

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 102488, China.

Physical stability is one of critical characteristics of liposome, especially to its clinical application. Vesicle fusion was one of the common physical stability phenomena that occurred during the long storage period. Because vesicle fusion could be easily checked by the change of vesicle size, it was widely applied in the evaluation of liposome physical stability. Read More

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http://dx.doi.org/10.1208/s12249-020-01680-6DOI Listing

Poloxamer-407-Co-Poly (2-Acrylamido-2-Methylpropane Sulfonic Acid) Cross-linked Nanogels for Solubility Enhancement of Olanzapine: Synthesis, Characterization, and Toxicity Evaluation.

AAPS PharmSciTech 2020 May 17;21(5):141. Epub 2020 May 17.

College of Pharmacy, University of Sargodha, University Road, Sargodha City, Punjab, Pakistan.

Current study is focused to enhance the solubility of poorly soluble drug olanzapine (OLZ) by nanogels drug delivery system, as improved solubility is one of the most important applications of nanosystems. Poor solubility is a major issue, and 40% of marketed and about 75% of new active pharmaceutical ingredients are poorly water soluble which significantly affect the bioavailability and therapeutic effects of these drugs. In this study, nanogels, a promising system for solubility enhancement, were developed by free-radical polymerization technique. Read More

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http://dx.doi.org/10.1208/s12249-020-01694-0DOI Listing

Self-Emulsifying Drug Delivery System of Celecoxib for Avoiding Delayed Oral Absorption in Rats with Impaired Gastric Motility.

AAPS PharmSciTech 2020 May 17;21(5):135. Epub 2020 May 17.

Laboratory of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka, 422-8526, Japan.

This study aimed to develop a self-emulsifying drug delivery system (SEDDS) of celecoxib (CEL) for suppressed delay in oral absorption under impaired gastric motility. A pseudo-ternary phase diagram was constructed for the determination of the optimal component ratio in SEDDS of CEL (SEDDS/CEL), and the SEDDS/CEL was physicochemically characterized. A pharmacokinetic study on orally dosed CEL samples (5-mg CEL/kg) was carried out in normal and propantheline (PPT)-treated rats to mimic impaired gastric motility. Read More

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http://dx.doi.org/10.1208/s12249-020-01686-0DOI Listing

MUCO-DIS: a New AFM-Based Nanoscale Dissolution Technique.

AAPS PharmSciTech 2020 May 17;21(5):142. Epub 2020 May 17.

Department of Pharmacy, School of Applied Sciences, University of Huddersfield, Huddersfield, HD1 3DH, UK.

Mucoadhesion-based drug delivery systems have recently gained interest because of their bio-adhesion capability, which results in enhanced residence time leading to prolonged duration of action with the mucosal surface, potentially improving compliance and convenience. Mucoadhesion testing of these formulations is widely reported; however, this is technically challenging due to the absence of any standard methods and difficulty in conducting mucoadhesion, formulation-mucosal surface interaction, mucosal surface topography and drug release in a single experiment. As these measurements are currently conducted separately, on replicate formulations, results can often be subjective and difficult to correlate. Read More

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http://dx.doi.org/10.1208/s12249-020-01697-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7231801PMC

Chewable Antacid Tablets: Are Disintegration Tests Relevant?

AAPS PharmSciTech 2020 May 17;21(5):139. Epub 2020 May 17.

Department of Pharmaceutical Chemistry, School of Pharmacy, College of Health Sciences, University of Nairobi, P.O. Box 19676-00202, Nairobi, Kenya.

A recently published FDA guidance on chewable tablets has addressed the quality attributes of this class of dosage forms. This study evaluated disintegration as a quality attribute for a number of commercially available chewable antacid tablets. Additionally, acid-neutralizing-capacity values were evaluated. Read More

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http://dx.doi.org/10.1208/s12249-020-01696-yDOI Listing

Formulation, Optimization and Evaluation of Novel Ultra-deformable Vesicular Drug Delivery System for an Anti-fungal Drug.

AAPS PharmSciTech 2020 May 17;21(5):140. Epub 2020 May 17.

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India.

The present study is aimed at enhancing the skin penetration of ketoconazole by formulating it as transethosome. Ketoconazole-loaded transethosome formulations were prepared by conventional thin film evaporation and hydration method and were optimized using concentration of edge activator (span 80), ethanol and sonication time as factors and particle size, polydispersity index and entrapment efficiency as responses. The optimized formulation was further evaluated for in vitro diffusion, anti-fungal activity, ex vivo penetration and in vivo pharmacodynamic activity. Read More

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http://dx.doi.org/10.1208/s12249-020-01681-5DOI Listing

The Stabilizing Excipients in Dry State Therapeutic Phage Formulations.

AAPS PharmSciTech 2020 May 15;21(4):133. Epub 2020 May 15.

Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, 2409 University Ave, Stop A1920, Austin, Texas, 78712, USA.

Phage therapy has gained prominence due to the increasing pathogenicity of "super bugs" and the rise of their multidrug resistance to conventional antibiotics. Dry state formulation of therapeutic phage is attractive to improve their "druggability" by increasing their shelf life, improving their ease of handling, and ultimately retaining their long-term potency. The use and selection of excipients are critical to stabilize phage in solid formulations and protect their viability from stresses encountered during the solidification process and long-term storage prior to use. Read More

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http://dx.doi.org/10.1208/s12249-020-01673-5DOI Listing

Cationic Polylactic Acid-Based Nanoparticles Improve BSA-FITC Transport Across M Cells and Engulfment by Porcine Alveolar Macrophages.

AAPS PharmSciTech 2020 May 15;21(4):134. Epub 2020 May 15.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, 10330, Thailand.

This work described the development of a cationic polylactic acid (PLA)-based nanoparticles (NPs) as an antigen delivery system using dimethyldioctadecylammonium bromide (DDA) to facilitate the engulfment of BSA-FITC by porcine alveolar macrophages (3D4/2 cells) and heat-labile enterotoxin subunit B (LTB) to enhance the transport of BSA-FITC across M cells. The experimental design methodology was employed to study the influence of PLA, polyvinyl alcohol (PVA), DDA, and LTB on the physical properties of the PLA-based NPs. The size of selected cationic PLA NPs comprising 5% PLA, 5% PVA, and 0. Read More

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http://dx.doi.org/10.1208/s12249-020-01689-xDOI Listing
May 2020
1.776 Impact Factor

Factors Influencing the Delivery Efficiency of Cancer Nanomedicines.

AAPS PharmSciTech 2020 May 14;21(4):132. Epub 2020 May 14.

Department of Clinical Pharmacy, School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, 211198, Jiangsu Province, People's Republic of China.

The superiority of nanomedicine over conventional medicines in the treatment of cancer has gained immediate recognition worldwide. As traditional cancer therapies are nonspecific and detrimental to healthy cells, the ability of nanomedicine to release drugs to target tumor cells specifically instead of healthy cells has brought new hope to cancer patients. This review focuses on the effects of various factors of nanoparticles such as transport, concentration in cells, tumor microenvironment, interaction with protein, penetration, uptake by tumor cells, cancer cell mutations, and intracellular trafficking of the nanoparticle. Read More

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http://dx.doi.org/10.1208/s12249-020-01691-3DOI Listing

Characterization, Optimization, In Vitro and In Vivo Evaluation of Simvastatin Proliposomes, as a Drug Delivery.

AAPS PharmSciTech 2020 May 13;21(4):129. Epub 2020 May 13.

Department of Pharmaceutics, College of Pharmacy, University of Hail, Hail, Kingdom of Saudi Arabia.

Simvastatin a cholesterol-lowering agent used to treat hypercholesterolemia, coronary heart disease, and dyslipidemia. However, simvastatin (SV) has shown low oral bioavailability in GIT. The main purpose of the work was to develop proliposomal formulations to increase the oral bioavailability of SV. Read More

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http://dx.doi.org/10.1208/s12249-020-01666-4DOI Listing

In Vitro Release of 5-Fluorouracil and Methotrexate from Different Thermosensitive Chitosan Hydrogel Systems.

AAPS PharmSciTech 2020 May 13;21(4):131. Epub 2020 May 13.

Department of Pharmaceutics and Industrial pharmacy, College of Pharmacy, Al-Azhar University, Cairo, Egypt.

5-Fluorouracil is a member of cytotoxic drugs with poor selectivity to cancer cells. Currently, systemic administration of this anti-cancer drug (oral or injection) exposes normal tissues to the drug-induced toxicity. Nowadays, attention has been greatly directed towards in situ gel-forming systems that can be injected into the affected tissues in its sol form with a minimally invasive technique. Read More

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http://dx.doi.org/10.1208/s12249-020-01672-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7220897PMC

Research Progress of Drug Treatment in Novel Coronavirus Pneumonia.

AAPS PharmSciTech 2020 May 13;21(4):130. Epub 2020 May 13.

Department of Pharmacy, The First Affiliated Hospital, College of Clinical Medicine of Henan University of Science and Technology, Luoyang, 471003, People's Republic of China.

As of March 10, 2020, more than 100,000 novel coronavirus pneumonia cases have been confirmed globally. With the continuous spread of the new coronavirus pneumonia epidemic in even the world, prevention and treatment of the disease have become urgent tasks. The drugs currently being developed are not adequate to deal with this critical situation. Read More

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http://dx.doi.org/10.1208/s12249-020-01679-zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7220569PMC

Evaluation of the Physico-mechanical Properties and Electrostatic Charging Behavior of Different Capsule Types for Inhalation Under Distinct Environmental Conditions.

AAPS PharmSciTech 2020 May 12;21(4):128. Epub 2020 May 12.

Research Center Pharmaceutical Engineering (RCPE) GmbH, Inffeldgasse 13, 8010, Graz, Austria.

Capsule-based dry powder inhaler (DPI) products can be influenced by a multitude of interacting factors, including electrostatic charging. Tribo-charging is a process of charge transfer impacted by various factors, i.e. Read More

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http://dx.doi.org/10.1208/s12249-020-01676-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7217808PMC

Quality Risk Management and Quality by Design for the Development of Diclofenac Sodium Intra-articular Gelatin Microspheres.

AAPS PharmSciTech 2020 May 10;21(4):127. Epub 2020 May 10.

NatPro-AUTH, Center for Interdisciplinary Research and Innovation (CIRI-AUTH), 57001, Thessaloniki, Greece.

The aim of the present study was to evaluate the development of an intra-articular nonsteroidal anti-inflammatory drug gelatin microsphere formulation based on quality risk management and quality by design approaches. Specifically, after setting the quality target product profile and the critical quality attributes, risk assessment was performed by constructing Ishikawa fishbone diagrams based on preliminary hazard analysis. A Plackett-Burman screening experimental design was applied in order to identify the factors (previously classified by risk assessment analysis as having high risk of failure) having a statistically significant impact on the formation of gelatin microspheres. Read More

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http://dx.doi.org/10.1208/s12249-020-01678-0DOI Listing

A Novel Technique to Improve Drug Loading Capacity of Fast/Extended Release Orally Dissolving Films with Potential for Paediatric and Geriatric Drug Delivery.

AAPS PharmSciTech 2020 May 7;21(4):126. Epub 2020 May 7.

School of Pharmacy, Aston University, Birmingham, UK.

Orally dissolving films (ODFs) have received much attention as potential oral drug delivery systems for paediatric and geriatric patients, particularly those suffering from dysphagia. With their unique properties and advantages, the technology offers improved patient compliance and wider acceptability, eliminates the fear of choking, enables ease of administration and offers dosing convenience, without the requirement of water. However, adequate drug loading remains a challenge. Read More

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http://dx.doi.org/10.1208/s12249-020-01665-5DOI Listing

Synthesis and Characterization of Nanostructured Lipid Nanocarriers for Enhanced Sun Protection Factor of Octyl p-methoxycinnamate.

AAPS PharmSciTech 2020 Apr 29;21(4):125. Epub 2020 Apr 29.

School of Pharmaceutical Sciences, UNESP-São Paulo State University, Rodovia Araraquara-Jau, km. 1, Araraquara, São Paulo, 14800-903, Brazil.

Sunlight is important to health, but higher exposure to radiation causes early aging of the skin and skin damage that can lead to skin cancers. This study aimed at producing a stable octyl p-methoxycinnamate (OMC)-loaded nanostructured lipid carrier (NLC) sunscreen, which can help in the photoprotective effect. NLC was produced by emulsification-sonication method and these systems were composed of myristyl myristate (MM), caprylic capric triglyceride (CCT), Tween® 80 (TW), and soybean phosphatidylcholine (SP) and characterized by dynamic light scattering (DLS), zeta potential (ZP) measurement, atomic force microscopy (AFM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and in vitro release studies. Read More

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http://dx.doi.org/10.1208/s12249-019-1547-0DOI Listing
April 2020
1.776 Impact Factor

SP94 Peptide-Functionalized PEG-PLGA Nanoparticle Loading with Cryptotanshinone for Targeting Therapy of Hepatocellular Carcinoma.

AAPS PharmSciTech 2020 Apr 27;21(4):124. Epub 2020 Apr 27.

School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, 510006, China.

To achieve improved drug delivery efficiency to hepatocellular carcinoma (HCC), biodegradable poly (ethylene glycol)-poly (lactic-co-glycolic acid) (PEG-PLGA) nanoparticles (NP), surface-modified with SP94 peptide, were designed for the efficient delivery of cryptotanshinone to the tumor for the treatment of HCC. Cryptotanshinone NP and SP94-NP were prepared by using nanoprecipitation. The physicochemical and pharmaceutical properties of the NP and SP94-NP were characterized, and the release kinetics suggested that both NP and SP94-NP provided continuous, slow release of cryptotanshinone for 48 h. Read More

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http://dx.doi.org/10.1208/s12249-020-01655-7DOI Listing

Evaluation of Mogroside V as a Promising Carrier in Drug Delivery: Improving the Bioavailability and Liver Distribution of Silybin.

AAPS PharmSciTech 2020 Apr 26;21(4):123. Epub 2020 Apr 26.

Department of TCMs Pharmaceuticals, China Pharmaceutical University, Nanjing, 210009, Jiangsu, China.

The objective of this work was to investigate the capacity of mogroside V (MOG-V), a food additive, as a novel carrier to improve the bioavailability and liver distribution of silybin (SLY). Solid dispersion particles (SDPs) of SLY/MOG-V were prepared utilizing the solvent evaporation method. The physicochemical characterizations of SDPs were evaluated by using dynamic light scattering (DLS), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) measurements. Read More

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http://dx.doi.org/10.1208/s12249-020-01645-9DOI Listing

Chemotherapeutic Efficacy Enhancement in P-gp-Overexpressing Cancer Cells by Flavonoid-Loaded Polymeric Micelles.

AAPS PharmSciTech 2020 Apr 26;21(4):121. Epub 2020 Apr 26.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, 50200, Thailand.

Multidrug resistance is the major problem in cancer treatment nowadays. Compounds from plants are the new targets to solve this problem. Quercetin (QCT), quercetrin (QTR), and rutin (RUT) are potential anticancer flavonoids but their poor water solubility leads to less efficacy. Read More

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http://dx.doi.org/10.1208/s12249-020-01657-5DOI Listing

The Role of Surface Properties on Protein Aggregation Behavior in Aqueous Solution of Different pH Values.

AAPS PharmSciTech 2020 Apr 26;21(4):122. Epub 2020 Apr 26.

Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu, 610041, People's Republic of China.

This study aimed to investigate the effect of pH-mediated surface properties of bovine serum albumin (BSA) on protein aggregation and the changes of protein structure and colloidal stability at different solution pH levels. The hydrophobicity of BSA surface was characterized by endogenous fluorescence spectroscopy, fluorescence quenching of acrylamide, and fluorescence probe. The results showed that the hydrophobicity of BSA surface was similar at pH 5, 6, 7. Read More

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http://dx.doi.org/10.1208/s12249-020-01663-7DOI Listing

Cold Flow Evaluation in Transdermal Drug Delivery Systems by Measuring the Width of the Oozed Adhesive.

AAPS PharmSciTech 2020 Apr 22;21(4):120. Epub 2020 Apr 22.

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

The objective of this study was to develop a simpler and more practical quantitative evaluation method of cold flow (CF) in transdermal drug delivery systems (TDDSs). CF was forcibly induced by loading a weight on a punched-out sample (bisoprolol and tulobuterol tapes). When the extent of CF was analyzed using the area of oozed adhesive as following a previously reported method, the CF profiles were looked different between the samples 12 mm in diameter subjected to a 0. Read More

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http://dx.doi.org/10.1208/s12249-020-01661-9DOI Listing

Preparation, Physicochemical Characterisation and DoE Optimisation of a Spray-Dried Dry Emulsion Platform for Delivery of a Poorly Soluble Drug, Simvastatin.

AAPS PharmSciTech 2020 Apr 21;21(4):119. Epub 2020 Apr 21.

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

In the presented study, insight into the development and optimisation of the dry emulsion formulation and spray drying process is provided. The aim was to facilitate the dissolution of the poorly soluble, highly lipophilic drug, simvastatin, by forming spray-dried dry emulsion particles having adequate powder flow properties, while assuring sufficient drug content. Simvastatin and a mixture of caprylic, capric triglyceride and 1-oleoyl-rac-glycerol were employed as a model drug and solubilising oils, respectively. Read More

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http://dx.doi.org/10.1208/s12249-020-01651-xDOI Listing

Improved Oral Pharmacokinetics of Pentoxifylline with Palm Oil and Capmul® MCM Containing Self-Nano-Emulsifying Drug Delivery System.

AAPS PharmSciTech 2020 Apr 21;21(4):118. Epub 2020 Apr 21.

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.

Pentoxifylline (PTX), an anti-hemorrhage drug used in the treatment of intermittent claudication, is extensively metabolized by the liver resulting in a reduction of the therapeutic levels within a short duration of time. Self-nano-emulsifying drug delivery system (SNEDDS) is well reported to enhance the bio-absorption of drugs by forming nano-sized globules upon contact with the biological fluids after oral administration. The present study aimed to formulate, characterize, and improve the oral bioavailability of PTX using SNEDDS. Read More

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http://dx.doi.org/10.1208/s12249-020-01644-wDOI Listing

Determination of Rate and Extent of Scopolamine Release from Transderm Scōp® Transdermal Drug Delivery Systems in Healthy Human Adults.

AAPS PharmSciTech 2020 Apr 16;21(3):117. Epub 2020 Apr 16.

Pharmaceutical Sciences and Experimental Therapeutics, University of Iowa College of Pharmacy, 180 South Grand Avenue, 552 CPB, Iowa City, IA, 52242-1112, USA.

To estimate strength of a scopolamine transdermal delivery system (TDS) in vivo, using residual drug vs. pharmacokinetic analyses with the goal of scientifically supporting a single and robust method for use across the dosage form and ultimately facilitate the development of more consistent and clinically meaningful labeling. A two-arm, open-label, crossover pharmacokinetic study was completed in 26 volunteers. Read More

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http://dx.doi.org/10.1208/s12249-020-01658-4DOI Listing
April 2020
1.776 Impact Factor

Development of Nanocrystal Ziprasidone Orally Disintegrating Tablets: Optimization by Using Design of Experiment and In Vitro Evaluation.

AAPS PharmSciTech 2020 Apr 15;21(3):115. Epub 2020 Apr 15.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, Turkey.

The objective of the current study was to develop ziprasidone hydrochloride monohydrate (ZHM) nanocrystal-based orally dispersible tablet (ODT) formulations. Design of experiment approach was used to develop ODTs. The tablets were compressed using direct compression method and characterized with quality control tests. Read More

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http://dx.doi.org/10.1208/s12249-020-01653-9DOI Listing

The Route to Palatable Fecal Microbiota Transplantation.

Authors:
Hala M Fadda

AAPS PharmSciTech 2020 Apr 15;21(3):114. Epub 2020 Apr 15.

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Butler University, 4600 Sunset Ave, Indianapolis, Indiana, 46208, USA.

The community of symbiotic microorganisms that reside in our gastrointestinal tract is integral to human health. Fecal microbiota transplantation (FMT) has been shown to be highly effective in treating recurrent Clostridioides difficile infection (rCDI) and is now recommended by medical societies for patients suffering from rCDI who have failed to respond to conventional therapy. The main challenges with FMT are its accessibility, acceptability, lack of standardization, and regulatory complexity, which will be discussed in this review. Read More

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http://dx.doi.org/10.1208/s12249-020-1637-zDOI Listing

Quantification of Monomer Units in Insoluble Polymeric Active Pharmaceutical Ingredients Using Solid-State NMR Spectroscopy I: Patiromer.

AAPS PharmSciTech 2020 Apr 15;21(3):116. Epub 2020 Apr 15.

Department of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky, USA.

Although extensive precautions are taken to limit batch-to-batch variation in pharmaceutical manufacturing, differences between lots may still exist, particularly in complex formulations. When polymerization is used in the production process, the potential for varying chain lengths and incorporation of different monomers increases the likelihood of batch-to-batch variation. This poses a significant challenge for demonstrating active pharmaceutical ingredient (API) sameness between the innovator and generic drug under development. Read More

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http://dx.doi.org/10.1208/s12249-020-01654-8DOI Listing

Novel Enhanced Therapeutic Efficacy of Dapoxetine HCl by Nano-Vesicle Transdermal Gel for Treatment of Carrageenan-Induced Rat Paw Edema.

AAPS PharmSciTech 2020 Apr 14;21(3):113. Epub 2020 Apr 14.

Department of Pharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, Nahda University, Beni Suef, Egypt.

The aim of this was to develop a well-balanced, replaceable, and patient non-infringing innovative transdermal drug delivery system "nano-vesicle transdermal gel" (NVTG) approaches for inhibiting inflammation. To consummate this objective, we developed a skin permeation nanogel system containing surface active agent along with ethanol. Carbopol 971p, hydroxypropyl methyl cellulose (HPMC K15M), and chitosan were used to fabricate the nanogels. Read More

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http://dx.doi.org/10.1208/s12249-020-01656-6DOI Listing

A Novel Prototype Device for Microencapsulation of Benznidazole: In Vitro/In Vivo Studies.

AAPS PharmSciTech 2020 Mar 31;21(3):112. Epub 2020 Mar 31.

Departamento Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, S2002LRK, Rosario, Argentina.

This study was aimed to design a simple and novel prototype device for the production of polymeric microparticles. To prove the effectiveness of this device, benznidazole microparticles using chitosan as carrier and NaOH, KOH, or SLS as counter ions were used. For comparison, benznidazole microparticles were prepared by the conventional dripping technique (syringe and gauge) using the same excipients. Read More

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http://dx.doi.org/10.1208/s12249-020-01659-3DOI Listing

Data-Driven Modeling of the Bicalutamide Dissolution from Powder Systems.

AAPS PharmSciTech 2020 Mar 31;21(3):111. Epub 2020 Mar 31.

Department of Pharmaceutical Technology and Biopharmaceutics, Jagiellonian University Medical College, Medyczna 9 St, 30-688, Kraków, Poland.

Low solubility of active pharmaceutical compounds (APIs) remains an important challenge in dosage form development process. In the manuscript, empirical models were developed and analyzed in order to predict dissolution of bicalutamide (BCL) from solid dispersion with various carriers. BCL was chosen as an example of a poor water-soluble API. Read More

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http://dx.doi.org/10.1208/s12249-020-01660-wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7109170PMC

Transdermal Delivery of the Free Base of 3-Fluoroamphetamine: In Vitro Skin Permeation and Irritation Potential.

AAPS PharmSciTech 2020 Mar 25;21(3):109. Epub 2020 Mar 25.

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

This work aimed to continue our effort in establishing the feasibility of 3-fluoroamphetamine (also known as PAL-353) to be a transdermal drug candidate by studying the delivery of the base form through the human cadaver skin in lieu of the previously investigated salt form, and for the first time using an EPIDERM™-reconstructed human epidermal model to predict the skin irritation potential of PAL-353, in support of development for a matrix-type transdermal delivery system. Passive and enhanced (with chemical permeation enhancers) transdermal delivery were investigated via in vitro permeation studies that were performed on Franz diffusion cells with dermatomed human cadaver skin. After 24 h, PAL-353 free base revealed high passive permeation of 417. Read More

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http://dx.doi.org/10.1208/s12249-020-01649-5DOI Listing

Lyophilisation Improves Bioactivity and Stability of Insulin-Loaded Polymeric-Oligonucleotide Nanoparticles for Diabetes Treatment.

AAPS PharmSciTech 2020 Mar 25;21(3):108. Epub 2020 Mar 25.

School of Pharmacy and Biomedical Sciences, Curtin University, Bentley, 6102, Australia.

The oral bioavailability of therapeutic proteins is limited by the gastrointestinal barriers. Encapsulation of labile proteins into nanoparticles is a promising strategy. In order to improve the stability of nanoparticles, lyophilisation has been used to remove water molecules from the suspension. Read More

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http://dx.doi.org/10.1208/s12249-020-01648-6DOI Listing
March 2020
1.776 Impact Factor