The research concerned the influence of the liposomally-entrapped indomethacin on its absorption after intragastric administration to rats. It was found that the indomethacin entrapped in liposomes has a favorable influence on the bioavailability in comparison to sole indomethacin suspension.
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Pharmaceutics
November 2024
Department of Pharmaceutics, School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou Higher Education Mega Center, 280 East Waihuan Road, Guangzhou 510006, China.
Indomethacin (IDM) is commonly used to treat chronic inflammatory diseases such as rheumatoid arthritis and osteoarthritis. However, long-term oral IDM treatment can harm the gastrointestinal tract. This study presents a design for encapsulating IDM within mixed micelles (MMs)-loaded dissolving microneedles (DMNs) to improve and sustain transdermal drug delivery.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
December 2024
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning Province 110016, PR China. Electronic address:
Mesoporous carriers have gained significant attention for enhancing the solubility and bioavailability of Biopharmaceutics Classification System (BCS) Class II drugs. However, the contribution of mesoporous carriers with varying morphologies to the physical stability of these drugs is not well-defined. In this work, mesoporous carbon nanoparticles (MCN) and hollow carbon mesoporous nanoparticles (HMC) were prepared, while the weakly acidic Indomethacin (IMC) and alkaline Celecoxib (CXB) were incorporated into these carriers in the amorphous state by the solvent evaporation method.
View Article and Find Full Text PDFMolecules
November 2024
College of Chemistry and Materials Science, Qinghai Minzu University, Xining 810007, China.
Indomethacin (INDO) is a synthetic non-steroidal antipyretic, analgesic, and anti-inflammatory drug that commonly exists in both amorphous and crystalline states. Its amorphous state (A-INDO) is utilized by pharmaceutical companies as an active pharmaceutical ingredient (API) in the production of INDO drugs due to its higher apparent solubility and bioavailability. The crystal state also encompasses various crystal forms such as the α-crystal form (α-INDO) and γ-crystal form (γ-INDO), with the highly crystalline and insoluble γ-INDO being commercially available.
View Article and Find Full Text PDFMol Pharm
November 2024
Drug Discovery Sciences, Bayer AG, Aprather Weg 18a, Wuppertal 42113, Germany.
Amorphous solid dispersions (ASDs) are a prevalent method for increasing the bioavailability and apparent solubility of poorly soluble drugs. Consequently, extensive research, encompassing both experimental and computational approaches, has been dedicated to developing methods for assessing the key factors influencing their stability, notably drug-polymer interactions. A common computational approach to rank the compatibility of a drug with a set of solvents or polymers is to compare thermodynamic observables, such as solvation free energies at infinite dilution.
View Article and Find Full Text PDFEur J Pharm Sci
January 2025
Soft Matter Chemistry, Department of Chemistry, and Helsinki Institute of Sustainability Science, Faculty of Science, University of Helsinki, Helsinki 00014, Finland. Electronic address:
Improving the solubility of poorly water-soluble drugs is essential for enhancing bioavailability, formulation flexibility and reducing patient-to-patient variability. The preparation of amorphous solid dispersions (ASDs) is an attractive strategy to formulate such drugs, leading to higher apparent water solubility and therefore higher bioavailability. For such ASDs, water-soluble polymer excipients, such as poly(vinyl pyrrolidone) (PVP) or poly(vinyl pyrrolidone-co-vinyl acetate) (P(VP-co-VA)), are employed to solubilize and stabilize the drug against crystallization.
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