3,808 results match your criteria Aaps Pharmscitech[Journal]


Correction to: Puerarin-Loaded PLGA Nanoparticles: Optimization Processes of Preparation and Anti-Alcohol Intoxication Effects in Mice.

AAPS PharmSciTech 2022 May 25;23(5):154. Epub 2022 May 25.

Experimental Teaching Center, School of Public Health, Chengdu Medical College, Chengdu, 610500, People's Republic of China.

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Nano-strategies as Oral Drug Delivery Platforms for Treatment of Cancer: Challenges and Future Perspectives.

AAPS PharmSciTech 2022 May 23;23(5):152. Epub 2022 May 23.

Department of Pharmaceutical Sciences, Mohanlal Sukhadia University, Udaipur, Rajasthan, 313001, India.

Oral drug administration is the oldest and widely used method for drug administration. The objectives behind developing an oral drug delivery for the treatment of cancer are to achieve low cost treatment by utilizing novel techniques to target cancer through gut-associated lymphoid tissue (GALT) and to enhance patient comfort and compliance through a hospital-free treatment leading to "Chemotherapy at Home." Unfortunately, due to the physiological environment of the GIT and physicochemical properties of drug candidate, the efficacy of oral drug delivery methods is limited in the treatment of cancer. Read More

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Correction to: Co-spray Drying Drugs with Aqueous Polymer Dispersions (APDs)-a Systematic Review.

AAPS PharmSciTech 2022 May 24;23(5):153. Epub 2022 May 24.

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

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Current Status and Challenges of Analytical Methods for Evaluation of Size and Surface Modification of Nanoparticle-Based Drug Formulations.

AAPS PharmSciTech 2022 May 20;23(5):150. Epub 2022 May 20.

School of Pharmacy, Kitasato University, Shirokane 5-9-1, Minato-ku, Tokyo, 108-8641, Japan.

The present review discusses the current status and difficulties of the analytical methods used to evaluate size and surface modifications of nanoparticle-based pharmaceutical products (NPs) such as liposomal drugs and new SARS-CoV-2 vaccines. We identified the challenges in the development of methods for (1) measurement of a wide range of solid-state NPs, (2) evaluation of the sizes of polydisperse NPs, and (3) measurement of non-spherical NPs. Although a few methods have been established to analyze surface modifications of NPs, the feasibility of their application to NPs is unknown. Read More

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Oxidative Stability in Lipid Formulations: a Review of the Mechanisms, Drivers, and Inhibitors of Oxidation.

AAPS PharmSciTech 2022 May 20;23(5):151. Epub 2022 May 20.

Gattefossé, Paramus, NJ, USA.

The importance of lipid-based formulations in addressing solubility and ultimately the bioavailability issues of the emerging drug entities is undeniable. Yet, there is scarcity of literature on lipid excipient chemistry and performance, notably in relation to oxidative stability. While not all lipid excipients are prone to oxidation, those with sensitive moieties offer drug delivery solutions that outweigh the manageable oxidative challenges they may present. Read More

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Venlafaxine HCl Encapsulated in Niosome: Green and Eco-friendly Formulation for the Management of Pain.

AAPS PharmSciTech 2022 May 20;23(5):149. Epub 2022 May 20.

Pharmaceutics Research Laboratory, School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, UK.

The goal of this experimentation was to increase the cutaneous absorption of venlafaxine HCl (VFX) encapsulated in a niosome (venlasosme) produced by an ultrasonic approach. The impact of the cholesterol:surfactant (Chol:Surf) proportion was examined to modify the venlasosme properties. Photon correlation spectroscopy, powder X-ray diffraction (PXRD), SEM, DSC, and ATR-FTIR spectroscopy were utilized to investigate the solid-state and morphology of VFX in the venlasosme. Read More

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Choline-Amino Acid-Derived Bio-ionic Liquids for Solubility Enhancement of Zafirlukast.

AAPS PharmSciTech 2022 May 18;23(5):146. Epub 2022 May 18.

Department of Pharmaceutics, Sinhgad College of Pharmacy, Vadgaon, Pune, 411041, Maharashtra, India.

This study investigated the application of bio-ionic liquids (ILs) prepared from choline as cation and amino acid as anion for solubility enhancement of poorly water-soluble drug, Zafirlukast (ZFL). Herein, the solubility of ZFL in water and mixtures of water and ILs was assessed using UV spectroscopy at two temperature points 25°C and 37°C with increasing concentrations of IL. ZFL solubility was found to improve linearly with increasing concentration of [Ch][Pro] in water, representing 35- to 37-fold improvement in ZFL solubility at maximum concentration of [Ch][Pro] (1% w/v) compared to when only pure water was present. Read More

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Preparation of 2-Methoxyestradiol Self-emulsified Drug Delivery System and the Effect on Combination Therapy with Doxorubicin Against MCF-7/ADM Cells.

AAPS PharmSciTech 2022 May 18;23(5):147. Epub 2022 May 18.

Department of Pharmaceutical Sciences, School of Basic Medical Sciences, Henan University of Science and Technology, Luoyang, 471023, Henan, People's Republic of China.

Due to the poor solubility and bioavailability of 2-methoxyestradiol (2-ME), 2-ME emulsified drug delivery system (2-ME-SEDDS) was designed and characterized. After dilution with 5% glucose, 2-ME-SEDDS formed fine emulsions with mean diameter of 171 ± 14 nm and zeta potential of - 7.4 ± 0. Read More

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Enhancing Atorvastatin In Vivo Oral Bioavailability in the Presence of Inflammatory Bowel Disease and Irritable Bowel Syndrome Using Supercritical Fluid Technology Guided by wbPBPK Modeling in Rat and Human.

AAPS PharmSciTech 2022 May 18;23(5):148. Epub 2022 May 18.

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

Inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) are common disorders that can change the body's physiology and drugs pharmacokinetics. Solid dispersion (SD) preparation using supercritical fluid technology (SFT) has many advantages. Our study aimed to explore the effect of IBS and IBD on atorvastatin (ATV) pharmacokinetics, enhance ATV oral bioavailability (BCS II drug) using SFT, and analyze drug-disease-formulation interaction using a whole-body physiologically based pharmacokinetic (wbPBPK) model in rat and human. Read More

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Spray Pattern and Plume Geometry Testing and Methodology: An IPAC-RS Working Group Overview.

AAPS PharmSciTech 2022 May 18;23(5):145. Epub 2022 May 18.

Faegre Drinker Biddle and Reath LLP, Suite 1100, District of Columbia, Washington, 20005, USA.

Plume characterization for orally inhaled and nasal drug products (OINDP) provides valuable information during OINDP development. Spray pattern and plume geometry techniques, methods, and technology have evolved over the past 20 years since the publication of the original 1998 FDA MDI DPI draft guidance. The International Pharmaceutical Aerosol Consortium on Regulation and Science (IPAC-RS) discusses the historical context and background to plume geometry and spray pattern characterization studies; provides an analysis of the current regulatory context; addresses results from its industry surveys on application and value of such testing; and presents case studies and best practices-seeking to provide insights to regulatory bodies and other stakeholders. Read More

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Effect of Different Absorption Enhancers on the Nasal Absorption of Nalmefene Hydrochloride.

AAPS PharmSciTech 2022 May 16;23(5):143. Epub 2022 May 16.

Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Academy of Military Sciences, Beijing, 100850, China.

The purpose of this work is to explore the effects of novel absorption enhancers on the nasal absorption of nalmefene hydrochloride (NMF). First, the influence of absorption enhancers with different concentrations and types and drug concentrations on the nasal absorption of NMF was investigated in vivo in rats. The absorption enhancers studied include n-dodecyl-β-D-maltoside (DDM), hydroxypropyl-β-cyclodextrin (HP-β-CD), and polyethylene glycol (15)-hydroxy Stearate (Solutol®HS15). Read More

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Effect of Different Molecular Weights of Chitosan on Formulation and Evaluation of Allopurinol-Loaded Nanoparticles for Kidney Targeting and in Management of Hyperuricemic Nephrolithiasis.

AAPS PharmSciTech 2022 May 16;23(5):144. Epub 2022 May 16.

Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.

Present research study was conducted to formulate kidney-targeted allopurinol (AO)-loaded chitosan nanoparticles (ANPs) for management of hyperuricemic related nephrolithiasis. Different molecular weights of chitosan were used for fabricating ANP formulation by adopting modified ionotropic gelation method. The prepared batches were than evaluated for particle size analysis, entrapment efficiency, transmission electron microscopy, X-ray diffraction, Differential Scanning Calorimetry, in vitro release and in vivo animal study. Read More

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Stiripentol Enteric Solid Dispersion-Loaded Effervescent Tablets: Enhanced Dissolution, Stability, and Absorption.

AAPS PharmSciTech 2022 May 10;23(5):141. Epub 2022 May 10.

Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.

Due to poor solubility and stability in acid conditions, the gastrointestinal administration of stiripentol (STP) is still a significant challenge. This study aimed to explore the applicability of effervescent tablets compressed from STP-loaded enteric solid dispersions to improve the solubility and stability of the insoluble and acid-labile drug. STP-loaded solid dispersions (STP-SDs) and the effervescent tablets (STP-SD-ETs) were prepared using solvent evaporation and dry granulation technology, respectively, and their formulations were optimized. Read More

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Nanoemulsions Containing Megestrol Acetate: Development, Characterization, and Stability Evaluation.

AAPS PharmSciTech 2022 May 10;23(5):142. Epub 2022 May 10.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330, Yenimahalle, Ankara, Turkey.

Many active pharmaceutical ingredients (API) are poorly soluble in water and their low oral bioavailability is a major hindrance to their potential use. Megestrol acetate (MGA) is insoluble in water and its oral absorption is limited and considerably affected by food. Nanoemulsions (NEs) can be used as effective oral drug delivery systems where the hydrophobic API is loaded into the oil phase. Read More

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Co-spray Drying Drugs with Aqueous Polymer Dispersions (APDs)-a Systematic Review.

AAPS PharmSciTech 2022 May 10;23(5):140. Epub 2022 May 10.

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

Aqueous colloidal dispersions of water-insoluble polymers (APDs) avoid hassles associated with the use of organic solvents and offer processing advantages related to their low viscosity and short processing times. Therefore, they became the main vehicle for pharmaceutical coating of tablets and multiparticulates, a process commonly employed using pan and fluidized-bed machinery. Another interesting although less common processing approach is co-spray drying APDs with drugs in aqueous systems. Read More

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3D Bioprinting of Human Hollow Organs.

AAPS PharmSciTech 2022 May 10;23(5):139. Epub 2022 May 10.

Department of Pharmaceutical Technology, Maulana Abul Kalam Azad University of Technology, Haringhata, Nadia-741249, West Bengal, India.

3D bioprinting is a rapidly evolving technique that has been found to have extensive applications in disease research, tissue engineering, and regenerative medicine. 3D bioprinting might be a solution to global organ shortages and the growing aversion to testing cell patterning for novel tissue fabrication and building superior disease models. It has the unrivaled capability of layer-by-layer deposition using different types of biomaterials, stem cells, and biomolecules with a perfectly regulated spatial distribution. Read More

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The Molecular Mechanism of Propylene Glycol Monocaprylate on Skin Retention: Probing the Dual Roles on the Molecular Mobility and Collagen Connection in Roflumilast Cream.

AAPS PharmSciTech 2022 May 9;23(5):136. Epub 2022 May 9.

Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, Liaoning, China.

The present work was to construct a roflumilast (ROF) cream for the treatment of psoriasis and clarify the dual roles of propylene glycol monocaprylate (PGM) in both molecular mobility of the cream, and drug-skin miscibility via drug-PGM-ceramide and drug-PGM-collagen intermolecular interaction. The cream formulation was screened through the stability study and in vitro skin administration study, optimized by Plackett-Burman and Box-Behnken design, and finally verified by the in vivo tissue distribution study. PGM demonstrated a significant drug skin retention enhancement effect (R = 19. Read More

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Preparation and Spectroscopic Characterization of Inclusion Complexes of 3D Ball-Milled Rifampicin with β-cyclodextrin and γ-cyclodextrin : 3D Ball-Milled Rifampicin with β-cyclodextrin and γ-cyclodextrin.

AAPS PharmSciTech 2022 May 9;23(5):138. Epub 2022 May 9.

Pharmaceutical Research and Drug Development Laboratories, Department of Pharmacy, School of Health Care Professions, University of San Carlos, 6000, Cebu City, Philippines.

Rifampicin (RFP) solutions, intended to reduce incidence of prosthetic graft infection, were prepared as three-dimensional ground mixtures (3DGMs) using β-cyclodextrin (βCD) and γ-cyclodextrin (γCD) and characterized for their spectroscopic properties and solubility. Phase solubility diagrams revealed that 3DGMs (RFP/βCD and RFP/γCD) produced a complex at 1:1 molar ratio. Pulsed field gradient nuclear magnetic resonance experiments indicated that the diffusion coefficients for RFP/βCD and RFP/γCD were similar to the respective diffusion coefficients for βCD and γCD. Read More

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Self-Emulsifying Systems for Delivery of Bioactive Compounds from Natural Origin.

AAPS PharmSciTech 2022 May 9;23(5):134. Epub 2022 May 9.

Postgraduate Program in Pharmaceutical Sciences, Laboratory of Research and Development of Drug Delivery Systems, Department of Pharmacy, State University of Maringa, Avenida Colombo, n. 5790, K68, S05, Maringa, Parana, 87020-900, Brazil.

Nature has been used as therapeutic resources in the treatment of diseases for many years. However, some natural compounds have poor water solubility. Therefore, physicochemical strategies and technologies are necessary for development of systems for carrying these substances. Read More

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Transformation of Ritonavir Nanocrystal Suspensions into a Redispersible Drug Product via Vacuum Drum Drying.

AAPS PharmSciTech 2022 May 9;23(5):137. Epub 2022 May 9.

Department of Pharmaceutical Technology, University of Bonn, Gerhard-Domagk-Straße 3, 53121, Bonn, Germany.

The present study explored vacuum drum drying (VDD) as potential drying technique for the solidification of crystalline ritonavir nanosuspensions prepared by wet-ball milling. In detail, the impact of drying protectants (mannitol, lactose, trehalose) added to the ritonavir nanosuspension was assessed in dependence of the drum temperature with respect to processibility via VDD, resulting intermediate powder properties, remaining nanoparticulate redispersibility and crystallinity. A clear impact of the glass transition temperature (T) of the drying protectant on the redispersibility/crystallinity of the VDD intermediate was observed. Read More

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Optimization of DOTAP/chol Cationic Lipid Nanoparticles for mRNA, pDNA, and Oligonucleotide Delivery.

AAPS PharmSciTech 2022 May 9;23(5):135. Epub 2022 May 9.

Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, Binghamton University, Johnson City, NY, 13790, USA.

Lipid nanoparticles (LNPs) can be used as delivery vehicles for nucleic acid biotherapeutics. In fact, LNPs are currently being used in the Pfizer/BioNTech and Moderna COVID-19 vaccines. Cationic LNPs composed of 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP)/cholesterol (chol) LNPs have been classified as one of the most efficient gene delivery systems and are being tested in numerous clinical trials. Read More

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Pharmacotechnical Evaluation by SeDeM Expert System to Develop Orodispersible Tablets.

AAPS PharmSciTech 2022 May 9;23(5):133. Epub 2022 May 9.

Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near R.T.O., Pune, 411001, India.

Sediment delivery model (SeDeM) system is innovative tool to correlate micromeritic properties of powders with compressibility. It involves computation of indices which facilitate direct compressibility of solids and enable corrective measures through particle engineering. Study had multiple objectives, viz, (i) to enhance solubility of BCS class II, nevirapine using solid dispersions; (ii) SeDeM analyses of excipients and solid dispersions to analyze direct compressibility; and (iii) prepare orodispersible tablets (ODT). Read More

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A Non-destructive Quantitative Transmission Raman Spectroscopy Method for Active Pharmaceutical Ingredient in Drug Product In-Use Samples Prepared in Dosing Vehicles.

AAPS PharmSciTech 2022 May 2;23(5):132. Epub 2022 May 2.

Research & Development, AbbVie Inc., 1 N Waukegan Road, North Chicago, Illinois, 60064, USA.

Compatibility and in-use stability screening studies are required for dosing vehicle selection based on the FDA's guidance, "Use of Liquids and/or Soft Foods as Vehicles for Drug Administration: General Considerations for Selection and In Vitro Methods for Product Quality Assessments." One of the major analytical challenges in these studies is sample preparation because extracting active pharmaceutical ingredient (API) from the drug product mixed into viscous soft-food matrices (e.g. Read More

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Co-crystallization of Amoxicillin Trihydrate and Potassium Clavulanate Provides a Promising Approach for Preparation of Sustained-Release Microspheres.

AAPS PharmSciTech 2022 May 2;23(5):131. Epub 2022 May 2.

Department of Medicinal Chemistry, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.

This work aimed to prepare sustained-release microspheres for amoxicillin trihydrate and potassium clavulanate. Co-crystals of amoxicillin trihydrate and potassium clavulanate were prepared using three different techniques, including supercritical fluid technology. Full characterization was performed for the prepared co-crystals, including molecular dynamic simulation. Read More

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Sorafenib-Loaded PLGA-TPGS Nanosystems Enhance Hepatocellular Carcinoma Therapy Through Reversing P-Glycoprotein-Mediated Multidrug Resistance.

AAPS PharmSciTech 2022 Apr 29;23(5):130. Epub 2022 Apr 29.

Department of Pharmacy, Anhui University of Chinese Medicine, No. 350, Longzihu Road, Hefei, Anhui, 230012, People's Republic of China.

Multidrug resistance (MDR) is a key determinant for hepatocellular carcinoma chemotherapy failure. P-glycoprotein is one of the main causes of MDR by causing drug efflux in tumor cells. In order to solve this thorny problem, we prepared a sorafenib-loaded polylactic acid-glycolic acid (PLGA) - D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) nanoparticles (SPTNs). Read More

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Spray-Dried Microspheres of Carboplatin: Technology to Develop Longer-Acting Injectable with Improved Physio-Chemical Stability, Toxicity, and Therapeutics.

AAPS PharmSciTech 2022 Apr 28;23(5):128. Epub 2022 Apr 28.

Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, 143005, India.

The present study aims to develop carboplatin injectable microspheres using spray-drying technology. The optimized powdered microspheres (MS-19-ST2) were morphologically spherical, with a 1.795 μm particle size and good micromeritic properties. Read More

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Formulation and Evaluation of Topical Linezolid Nanoemulsion for Open Incision Wound in Diabetic Animal Model.

AAPS PharmSciTech 2022 Apr 28;23(5):129. Epub 2022 Apr 28.

Drug Delivery and Cosmetics Lab (DDCL), Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, D.I. Khan, 29050, Pakistan.

The present study aimed to investigate the role of topical nanoemulsion of linezolid in attenuating diabetic wound by delivering the drug to the target tissue. The nanoemulsions (NEs) were prepared by high-pressure homogenization and subjected to thermodynamic stability, pH, droplet size, viscosity, surface charge, polydispersity index (PDI), entrapment efficiency, drug content, and in vitro drug release. All formulations were thermodynamically stable. Read More

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Evaluation of Piperine as Natural Coformer for Eutectics Preparation of Drugs Used in the Treatment of Cardiovascular Diseases.

AAPS PharmSciTech 2022 Apr 26;23(5):127. Epub 2022 Apr 26.

Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, 1174-1200, Pavas, San José, Costa Rica.

Piperine (PIP) was evaluated as a natural coformer in the preparation of multicomponent organic materials for enhancing solubility and dissolution rate of the poorly water-soluble drugs: curcumin (CUR), lovastatin (LOV), and irbesartan (IBS). A screening based on liquid assisted grinding technique was performed using 1:1 drug-PIP molar ratio mixtures, followed by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) analyses. Three eutectic mixtures (EMs) composed of CUR-PIP, LOV-PIP, and IBS-PIP were obtained. Read More

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Silymarin-Encapsulated Xanthan Gum-Stabilized Selenium Nanocarriers for Enhanced Activity Against Amyloid Fibril Cytotoxicity.

AAPS PharmSciTech 2022 Apr 26;23(5):125. Epub 2022 Apr 26.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)-Raebareli, A Transit Campus at Bijnor-Sisendi Road, Sarojini Nagar, Near CRPF Base Camp, Lucknow, Uttar Pradesh, 226002, India.

The accumulation of amyloid-beta at the neuronal sites is a major pathological hallmark involved in the etiology of Alzheimer's disease. To reduce the Aβ-induced neuronal cytotoxicity, selenium nanoparticles and silymarin were fabricated in a single polysaccharide matrix for dual antioxidant and Aβ fibril disaggregation activity. These nanoparticles were further stabilized by an exopolysaccharide xanthan gum. Read More

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Assessment of Resonant Acoustic Mixing for Low-Dose Pharmaceutical Powder Blends.

AAPS PharmSciTech 2022 Apr 26;23(5):126. Epub 2022 Apr 26.

Drug Product Development, Bristol Myers Squibb, 556 Morris Avenue, Summit, New Jersey, 07901, USA.

Obtaining a homogeneous low-dose pharmaceutical powder blend without multi-step processing remains a challenge. One promising technology to address this risk is resonant acoustic mixing (RAM). In this study, the performance of a laboratory resonant acoustic mixer (LabRAM) was studied at low active pharmaceutical ingredient (API) concentrations (0. Read More

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