3,658 results match your criteria AAPS PharmSciTech[Journal]


Development, Characterization, and Optimization of a Novel Abiraterone Acetate Formulation to Improve Biopharmaceutical Attributes Aided by Pharmacokinetic Modelling.

AAPS PharmSciTech 2021 Nov 22;23(1). Epub 2021 Nov 22.

Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat, 382481, India.

Abiraterone acetate has very low bioavailability and drastic food effect to warrant a dosing regimen under fasting state only. Therefore, we aimed to develop and optimize a liquisolid compact formulation of abiraterone acetate to improve biopharmaceutical attributes aided by pharmacokinetic modelling and achieve dose reduction with no food effect on the formulation. Preliminary studies highlighted the importance of the selection of olive oil as a compatible vehicle. Read More

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November 2021

Quantification of Compatibility Between Polymeric Excipients and Atenolol Using Principal Component Analysis and Hierarchical Cluster Analysis.

AAPS PharmSciTech 2021 Nov 19;23(1). Epub 2021 Nov 19.

Department of Analytical Chemistry, Medical University of Gdansk, Gen. Hallera 107, 80-416, Gdansk, Poland.

An important challenge to overcome in the solid dosage forms technology is the selection of the most biopharmaceutically efficient polymeric excipients. The excipients can be selected, among others, by compatibility studies since incompatibilities between ingredients of the drug formulations adversely affect their bioavailability, stability, efficacy, and safety. Therefore, new, fast, and reliable methods for detecting incompatibility are constantly being sought. Read More

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November 2021

Inclusion Complexes of Daidzein with Cyclodextrin-Based Metal-Organic Framework-1 Enhance Its Solubility and Antioxidant Capacity.

AAPS PharmSciTech 2021 Nov 18;23(1). Epub 2021 Nov 18.

Graduate School of Medicine, University of Yamanashi, 1110 Shimokato, Chuo, Yamanashi, 4093898, Japan.

Daidzein, an aglycone-type isoflavone, is useful in the prevention of atherosclerotic cardiovascular diseases. However, the solubility of daidzein remains relatively low even with pharmaceutical interventions (e.g. Read More

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November 2021

The Influence of Relative Humidity and Storage Conditions on the Physico-chemical Properties of Inhalation Grade Fine Lactose.

AAPS PharmSciTech 2021 Nov 17;23(1). Epub 2021 Nov 17.

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

Dry powder inhalers (DPIs) are favorable devices for the delivery of dry formulations to the lungs; still, they largely fail to deliver higher doses of active pharmaceutical ingredient (API) to the lower airways. Addition of fine particles of excipient (fines) to the blend of API and carrier was shown to improve aerosolization performance. Lactose monohydrate is ubiquitous excipient used for this purpose. Read More

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November 2021

Correction to: Piperine-Loaded Glycyrrhizic Acid- and PLGA-Based Nanoparticles Modified with Transferrin for Antitumor.

AAPS PharmSciTech 2021 Nov 15;22(8):276. Epub 2021 Nov 15.

Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, No. 1160 Shengli South Street, Yinchuan, 750004, China.

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November 2021

A Software Tool for Lyophilization Primary Drying Process Development and Scale-up Including Process Heterogeneity, I: Laboratory-Scale Model Testing.

AAPS PharmSciTech 2021 Nov 12;22(8):274. Epub 2021 Nov 12.

Davidson School of Chemical Engineering, Purdue University, West Lafayette, Indiana, USA.

Freeze-drying is a deceptively complex operation requiring sophisticated design of a robust and efficient process that includes understanding and planning for heterogeneity across the batch and shifts in parameters due to vial or lyophilizer changes. A software tool has been designed to assist in process development and scale-up based on a model that includes consideration of the process heterogeneity. Two drug formulations were used to test the ability of the new tool to develop a freeze-drying cycle and correctly predict product temperatures and drying times. Read More

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November 2021

Preparation and Characterization of pH-Independent Sustained-Release Tablets Containing Hot Melt Extruded Solid Dispersions of Clarithromycin : Tablets Containing Solid Dispersions of Clarithromycin.

AAPS PharmSciTech 2021 Nov 12;22(8):275. Epub 2021 Nov 12.

Punjab University College of Pharmacy, University of the Punjab Lahore, Lahore, Pakistan.

The limited solubility of clarithromycin (CAM), coupled with low bioavailability and rapid elimination, are major shortcomings, needed to be addressed to achieve optimum therapeutic goals. Therefore, sustained-release (SR) tablets containing solid dispersion (SD) granules of CAM were prepared in this study. Initially, SD granules of CAM were prepared by hot melt extrusion (HME) technique using Kollidon VA64 as a hydrophilic carrier. Read More

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November 2021

A Practical Discussion on Estimating Shelf Life Through Tolerance Intervals.

AAPS PharmSciTech 2021 Nov 12;22(8):273. Epub 2021 Nov 12.

Early Development Biostatistics, Novartis, East Hanover, NJ, USA.

This paper is a companion article to the research originally presented in "Estimating Shelf Life through Tolerance Intervals" (Schwenke et al., 21:290, 2020) published in AAPS PharmSciTech where tolerance intervals are introduced as an alternative methodology for estimating pharmaceutical shelf life. An industry stability shelf life example data set was used to demonstrate the proposed methods. Read More

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November 2021

Development and Optimization of Microballoons Assisted Floating Tablets of Baclofen.

AAPS PharmSciTech 2021 Nov 11;22(8):272. Epub 2021 Nov 11.

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Elite Status and Centre of Excellence (Maharashtra), Deemed University, N.P. Marg, Matunga East, Mumbai, Maharashtra, 400019, India.

The objective of the present study was to develop microballoons aided gastro-retentive floating tablets of baclofen, a skeletal muscle relaxant with a low elimination half-life of ~ 3.5 h. Baclofen floating tablet was prepared to offer convenience by designing a tablet that would float in the stomach for a prolonged period and allow controlled drug release to enable once-a-day administration. Read More

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November 2021

Highlighting DEM's Potential to Gauge Mechanistic Attributes of MUPS Tablet and Capsule Formulations.

AAPS PharmSciTech 2021 Nov 11;22(8):271. Epub 2021 Nov 11.

Operations Science & Technology, AbbVie Deutschland GmbH & Co. KG, 67061, Ludwigshafen, Germany.

Simulation of pharmaceutical unit operations by the discrete element method (DEM) has elevated our understanding of the impact of single-particle interactions on themselves, and on the entire tablets/powder. Studies in the past have shown how this knowledge helps to mitigate/solve multiple challenges during conventional formulation and process development/modernization/troubleshooting, with minimal use of active drug material. This communication adds to this- highlighting the tool's potential for a rapid preliminary assessment of the mechanistic attributes of multiple unit particle system (MUPS) based tablet and capsule drug products. Read More

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November 2021

AddaVax Formulated with PolyI:C as a Potential Adjuvant of MDCK-based Influenza Vaccine Enhances Local, Cellular, and Antibody Protective Immune Response in Mice.

AAPS PharmSciTech 2021 Nov 11;22(8):270. Epub 2021 Nov 11.

National Engineering Technology Research Center for Combined Vaccines, Wuhan, 430207, China.

Poor immune responses to inactivated influenza vaccine can be improved by effective and safe adjuvants to increase antibody titers and cellular protective response. In our study, AddaVax and PolyI:C combined adjuvant (AP adjuvant) were used for influenza vaccine development. After immunizing BALB/c mice and Wistar rats intramuscularly, Split inactivated H3N2 vaccine adjuvanted with AP elicited higher serum hemagglutination-inhibition antibodies and IgG titers. Read More

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November 2021

Brucine-Loaded Ethosomal Gel: Design, Optimization, and Anti-inflammatory Activity.

AAPS PharmSciTech 2021 Nov 11;22(8):269. Epub 2021 Nov 11.

Department of Pharmaceutics, College of Pharmacy, University of Ha'il, Hail, Saudi Arabia.

Brucine, one of the natural medications obtained from Nux vomica seeds, is used as an anti-inflammatory drug. Several investigations were performed to overcome its drawbacks, which will affect significantly its pharmaceutical formulation. The goal of the current investigation was to design, optimize, and evaluate the anti-inflammatory performance of BRU ethosomal gel. Read More

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November 2021

A Novel Method for Rapid Particle Size Analysis of Ibuprofen Using Near-infrared Spectroscopy.

AAPS PharmSciTech 2021 Nov 8;22(8):268. Epub 2021 Nov 8.

Institute of Chemistry, Faculty of Natural Sciences and Mathematics, Ss. Cyril and Methodius University in Skopje, Arhimedova 5, 1000, Skopje, Republic of North Macedonia.

Particle size distribution (PSD) is often considered as critical material attribute for active pharmaceutical ingredients (APIs), and the need for regular evaluation stands as an important quality control parameter in the pharmaceutical industry. Near-infrared (NIR) spectroscopy, used routinely for API identification, was introduced as analytical tool for simultaneous determination of particle size of ibuprofen. The demonstrated potential was highlighted by the development of rapid, robust, and noninvasive method coupled with multivariate data analysis (MVA), which can be easily transferred in QC laboratories for routine analysis. Read More

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November 2021

Recommended Best Practices for Lyophilization Validation 2021 Part II: Process Qualification and Continued Process Verification.

AAPS PharmSciTech 2021 Nov 8;22(8):266. Epub 2021 Nov 8.

Birck Nanotechnology Center, Purdue University, 1205 W State St., West Lafayette, IN, 47907, USA.

This work describes the lyophilization process validation and consists of two parts. Part one (Part I: Process Design and Modeling) focuses on the process design and is described in the previous paper, while the current paper is devoted to process qualification and continued process verification. The goal of the study is to show the cutting edge of lyophilization validation based on the integrated community-based opinion and the industrial perspective. Read More

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November 2021

Design and Characterization of HY-038 Solid Dispersions via Spray Drying Technology: In Vitro and In Vivo Evaluations.

AAPS PharmSciTech 2021 Nov 8;22(8):267. Epub 2021 Nov 8.

Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai, 201203, People's Republic of China.

The aim of this study was to prepare HY-038 solid dispersions (SDs) with single carrier at high drug loading and then forming a tablet to enhance solubility, dissolution, and bioavailability via spray drying technology. At the same time, we hope to develop a more convenient in vitro method to predict the absorption behavior of different formulations in vivo. Different solid dispersions, varying in drug/polymer ratios, were prepared. Read More

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November 2021

Interrelationships Between Coating Uniformity and Efficiency in Pan Coating Processes.

AAPS PharmSciTech 2021 Nov 4;22(8):265. Epub 2021 Nov 4.

The University of British Columbia, Vancouver, British Columbia, Canada.

The relationships between coating uniformity and efficiency were explored for tablet coating processes in pan coaters. The factors affecting the size of the spray zone were modeled using one-dimensional deposition analysis of spray droplets. This model was incorporated into the analytical model developed for coating uniformity by Choi et al. Read More

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November 2021

Budding Multi-matrix Technology-a Retrospective Approach, Deep Insights, and Future Perspectives.

AAPS PharmSciTech 2021 Nov 3;22(8):264. Epub 2021 Nov 3.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500037, India.

The human race is consistently striving for achieving good health and eliminate disease-causing factors. For the last few decades, scientists have been endeavoring to invent and innovate technologies that can substitute the conventional dosage forms and enable targeted and prolonged drug release at a particular site. The novel multi-matrix technology is a type of matrix formulation where the formulation is embraced to have a matrix system with multiple number of matrices. Read More

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November 2021

Preformulation Studies to Guide the Production of Medicines by Fused Deposition Modeling 3D Printing.

AAPS PharmSciTech 2021 Nov 2;22(8):263. Epub 2021 Nov 2.

Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, Brasília, DF, 70910-900, Brazil.

Fused deposition modeling (FDM) 3D printing has demonstrated high potential for the production of personalized medicines. However, the heating at high temperatures inherent to this process causes unknown risks to the drug product's stability. The present study aimed to assess the use of a tailored preformulation protocol involving physicochemical assessments, including the rheological profiles of the samples, to guide the development of medicines by FDM 3D printing. Read More

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November 2021

Quick and Simultaneous Analysis of Dissolved Active Pharmaceutical Ingredients and Formulation Excipients from the Dissolution Test Utilizing UHPLC and Charged Aerosol Detector.

AAPS PharmSciTech 2021 Nov 1;22(8):262. Epub 2021 Nov 1.

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Kyoto, Japan.

The objective of the study is to develop a quick and simultaneous analysis system for the dissolution of the active pharmaceutical ingredient (API) and the formulation excipient in samples from the dissolution test by UHPLC using the charged aerosol and PDA detectors. The combination of two columns for size-exclusion chromatography (SEC) and the equipment of the charged aerosol detector allowed the quick determination of various water-soluble polymers. Three model sustained-release tablets, each containing a different API of different water solubility (propranolol (soluble), ranitidine (very soluble), and cilostazol (practically insoluble)), were prepared from polyethylene oxide (PEO) matrix to verify the applicability and utility of the analysis system. Read More

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November 2021

Enhancing Biopharmaceutical Attributes of Khellin by Amorphous Binary Solid Dispersions.

Authors:
Sonali S Bharate

AAPS PharmSciTech 2021 Oct 27;22(8):260. Epub 2021 Oct 27.

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, 400056, India.

Khellin, a furanochromone isolated from fruits and seeds of Ammi visnaga, is traditionally used in many eastern Mediterranean countries. The plant decoction and the crystalline substance khellin have many pharmacological activities. For instance, it acts as a bronchodilator and also relieves renal colic and urethral stones, etc. Read More

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October 2021

Low-Frequency Sonophoresis as an Active Approach to Potentiate the Transdermal Delivery of Agomelatine-Loaded Novasomes: Design, Optimization, and Pharmacokinetic Profiling in Rabbits.

AAPS PharmSciTech 2021 Oct 27;22(8):261. Epub 2021 Oct 27.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

The first melatonergic antidepressant drug, agomelatine (AGM), is commonly used for controlling major depressive disorders. AGM suffers low (< 5%) oral bioavailability owing to the hepatic metabolism. The current work investigated the potential of low-frequency sonophoresis on enhancing transdermal delivery of AGM-loaded novasomes and, hence, bioavailability of AGM. Read More

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October 2021

Cliv-92-Loaded Glycyrrhetinic Acid-Modified Chitosan Nanoparticles for Enhanced Hepatoprotection-Preparation, Characterization, and In Vivo Evaluation.

AAPS PharmSciTech 2021 Oct 26;22(8):259. Epub 2021 Oct 26.

Division of Bioprospection and Product Development, CSIR-Central Institute of Medicinal and Aromatic Plants, P.O.-CIMAP, Lucknow, 226015, Uttar Pradesh, India.

Cliv-92 is a mixture of three structurally similar coumarinolignoids and a proven hepatoprotective agent. Low aqueous solubility and poor bioavailability are notable hindrances for its further use. Therefore, glycyrrhetinic acid-linked chitosan nanoparticles loaded with Cliv-92 were prepared for active targeting to the liver. Read More

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October 2021

Investigation of the Fused Deposition Modeling Additive Manufacturing I: Influence of Process Temperature on the Quality and Crystallinity of the Dosage Forms.

AAPS PharmSciTech 2021 Oct 25;22(8):258. Epub 2021 Oct 25.

Pharmaceutical Engineering and 3D Printing (PharmE3D) Lab, Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, 78712, USA.

With the advancements in cutting-edge technologies and rapid development of medical sciences, patient-focused drug development (PFDD) through additive manufacturing (AM) processes is gathering more interest in the pharmaceutical area than ever. Hence, there is an urgent need for researchers to comprehensively understand the influence of three-dimensional design on the development of novel drug delivery systems (DDSs). For this research, fused deposition modeling (FDM) 3D printing was investigated, and phenytoin (PHT) was selected as the model drug. Read More

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October 2021

Amalgamation of Solid Dispersion and Melt Adsorption Technique: Improved In Vitro and In Vivo Performance of Ticagrelor Tablets.

AAPS PharmSciTech 2021 Oct 21;22(8):257. Epub 2021 Oct 21.

Maliba Pharmacy College, Uka Tarsadia University, Maliba Campus, Gopal Vidyanagar, Bardoli-Mahuva Road, At & Po: Tarsadi-394350, Dist: Surat, Gujrat, India.

Ticagrelor (TG) suffers from low peroral bioabsorption (36%) due to P-gp efflux and poor solubility (10 µg/mL). TG solid dispersion adsorbates (TG-SDAs) were formulated using an amalgamation of solid dispersion and melt adsorption techniques which were simple, economic, scalable, and solvent-free. FTIR indicated no incompatibility between drug and excipients. Read More

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October 2021

Development of Self-Microemulsifying Drug Delivery System to Improve Nisoldipine Bioavailability: Cell Line and In Vivo Evaluations : Development of Self-Microemulsifying Drug Delivery System.

AAPS PharmSciTech 2021 Oct 21;22(8):256. Epub 2021 Oct 21.

Drug Delivery Research Laboratory, Shri G. H. Patel Pharmacy Building, Faculty of Pharmacy, The M. S. University of Baroda, Fatehgunj, Vadodara, 390002, Gujarat, India.

The authors attempted to fabricate a novel lipid-based formulation of a lipophilic drug, nisoldipine (NISO). As NISO belongs to BCS class 2 drug, it suffers from low bioavailability (5%). Hence, the research was intended to ameliorate oral bioavailability of NISO via intestinal lymphatic transport. Read More

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October 2021

Correction to: Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine.

AAPS PharmSciTech 2021 Oct 20;22(8):255. Epub 2021 Oct 20.

Department of Pharmacy, Shenyang Pharmaceutical University, No. 103 Wenhua Road, Shenyang, 110016, China.

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October 2021

Effects of Formulation and Manufacturing Process on Drug Release from Solid Self-emulsifying Drug Delivery Systems Prepared by High Shear Mixing.

AAPS PharmSciTech 2021 Oct 19;22(8):254. Epub 2021 Oct 19.

Laboratory of Nanosystems and Drug Delivery Devices (NanoSYS), School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, Goiania, GO, 74605-170, Brazil.

This study sought to investigate the influence of formulation and process factors of the high shear mixing (HSM) on the properties of solid self-emulsifying drug delivery systems (S-SEDDS) containing the model drug carvedilol (CAR). Firstly, liquid SEDDS (L-SEDDS) were prepared by mixing castor oil with different proportions of surfactant (Solutol or Kolliphor RH40) and cosolvent (Transcutol or PEG400). A miscible L-SEDDS with high drug solubility (124. Read More

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October 2021

Thiolated Chitosan-Centella asiatica Nanocomposite: A Potential Brain Targeting Strategy Through Nasal Route.

AAPS PharmSciTech 2021 Oct 19;22(8):251. Epub 2021 Oct 19.

Pharmaceutics and Pharmacokinetics Division, Central Drug Research Institute, Lucknow, 226031, Uttar Pradesh, India.

The major challenge associated with the treatment of neurological disorders is the inefficiency of drugs to enter the Central Nervous System (CNS). Polymer-drug conjugates are now being tailored to overcome this hindrance associated with conventional drugs. The study aimed at developing polymer hybrid nasal nanocomposite for enhanced delivery of Centella to the CNS. Read More

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October 2021

Development and Evaluation of Icariin-Loaded PLGA-PEG Nanoparticles for Potentiation the Proapoptotic Activity in Pancreatic Cancer Cells.

Authors:
Nabil A Alhakamy

AAPS PharmSciTech 2021 Oct 19;22(8):252. Epub 2021 Oct 19.

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.

Therapeutic efficacy of antineoplastic agents possessing a selective target to the nucleus of the cancer cells could be enhanced through novel formulation approaches. Thus, towards improvement of anticancer potential of icariin (ICA) on pancreatic cancer, the drug was entrapped into the polymeric poly lactic-co-glycolic acid (PLGA) with polyethylene glycol (PEG) as diblock copolymer. Optimization of the formulation was done using Statgraphics software to standardize percentages of PEG-PLGA and tween 80 (TW80) to obtain the smallest particle size. Read More

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October 2021

Fabrication and Evaluation of Transdermal Delivery of Carbamazepine Dissolving Microneedles.

AAPS PharmSciTech 2021 Oct 19;22(8):253. Epub 2021 Oct 19.

Department of Neurosciences, Faculty of Medicine, Jordan University of Science and Technology, Irbid, Jordan.

This project aims to prepare hydrogel microneedle patches (MNs) as a painless method to deliver carbamazepine transdermally. This can be used as a sustained release system that offers the advantages of lower gastrointestinal side effects and avoids the first-pass metabolism of the drug. MNs were composed of two medicated layers, a microneedle layer and a base layer. Read More

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October 2021