The objective of the present investigation is to enhance the dissolution and flow properties of raloxifene hydrochloride (RXH), a biopharmaceutical classification system class II drug. Melt dispersion of RXH with polyethylene glycol (PEG) 6000 was prepared by the fusion method. The melt dispersion was then adsorbed onto a porous adsorbent, Neusilin, by the melt adsorption method. Response surface methodology was employed to establish the design space for formulation variables such as the ratio of RXH to PEG 6000 in melt dispersion and amount of porous adsorbent to melt dispersion. Differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, Fourier-transform infrared spectroscopy, and accelerated stability techniques were utilized to characterize formulations. Negative Gibbs free energy values indicated spontaneous solubilization of RXH in PEG 6000. The time required for 80% of drug release from optimized formulation was <20 min compared with plain RXH. Accelerated stability studies confirmed the stabilization of amorphous melt dispersion in nanopores (nanoconfinement) of inorganic silicate Neusilin. Melt dispersion, adsorbed on porous carriers, is a promising technique to improve the dissolution characteristic as well as flow properties of drug molecules.
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http://dx.doi.org/10.1089/adt.2020.990 | DOI Listing |
ACS Nano
January 2025
Key Laboratory of Bioinorganic and Synthetic Chemistry of Ministry of Education, LIFM, GBRCE for Functional Molecular Engineering, School of Chemistry, IGCME, Sun Yat-Sen University, Guangzhou 510275, China.
Lead halide perovskite nanocrystal materials such as CsPbX (X = Cl, Br, and I) have triggered an intense research upsurge due to their excellent scintillation performance. Herein, an crystallization strategy is developed to grow CsPbBr nanocrystals (NCs) within a low-melting-point (280 °C) coordination polymer (CP) glass. The viscosity of coordination glass is reduced through a low-temperature (e.
View Article and Find Full Text PDFMacromol Rapid Commun
January 2025
Department of Bioengineering, Imperial College London, South Kensington, London, SW7 2AZ, UK.
Intrinsically conductive polymers have garnered a great deal of attention for use in medical and bioelectronic applications. Despite this, challenges associated with the mechanical stability, processability, and fabrication of conducting polymers have limited their utility. To circumvent these limitations, thiophene substituted 2-oxazolines (2Ox) and 2-oxazines (2Ozi) are introduced, which can be polymerized to form a thermally stable and potentially melt-processable polymers as precursors for conductive polymers.
View Article and Find Full Text PDFPharmaceutics
December 2024
Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, 3 Rokietnicka St., 60-806 Poznan, Poland.
Curcumin and hesperetin are plant polyphenols known for their poor solubility. To address this limitation, we prepared amorphous PVP K30-phosphatidylcholine dispersions via hot-melt extrusion. This study aimed to evaluate the effects of the amounts of active ingredients and phosphatidylcholine, as well as the process temperature, on the performance of the dispersions.
View Article and Find Full Text PDFMolecules
January 2025
Institute of Food Engineering-FoodUPV, Universitat Politècnica de València, 46022 Valencia, Spain.
Int J Pharm
January 2025
Laboratory of Pharmaceutical Technology, Division of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 541 24 Thessaloniki, Greece; Natural Products Research Centre of Excellence-AUTH (NatPro-AUTH), Center for Interdisciplinary Research and Innovation (CIRI-AUTH), Thessaloniki 57001, Greece. Electronic address:
Amorphous solid dispersions (ASDs) are widely recognized for their potential to enhance the solubility of poorly water-soluble drugs, with factors such as molecular mobility, intermolecular interactions, and storage conditions playing critical roles in their performance. However, the influence of preparation methods on their performance remains underexplored, especially regarding their supersaturation . To address this gap, the present study systematically investigates ASDs of ibuprofen (IBU, used as a model drug) prepared using two widely utilized techniques (solvent evaporation, SE, and melt-quench cooling, M-QC).
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