Drug-fortified liposomes as carriers for sustained release of NSAIDs: The concept and its validation in the animal model for the treatment of arthritis

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Vijay A PawarMange Ram Yadav

Abstract

Drug-fortified cationic liposomes of 6‑methoxy‑2‑naphthylacetic acid (6‑MNA) were prepared and characterized by various techniques. The residence time of drug-fortified liposomes in joint cavity was evaluated by intra-articular (IA) administration of the radio-labeled (99mTc) liposomal formulation in the inflamed joints in rats. The cationic liposomal formulation composed of 6‑MNA (3) as an active agent, its double salt (4) with the lipid 1,2‑distearoyl‑sn‑glycero‑3‑phosphoethanolamine (DSPE), and pharmaceutically acceptable excipients such as hydrogenated soyabean phospatidylcholine (HSPC) and 1,2‑dioleyloxy‑3‑trimethylammoniumpropane chloride (DOTAP) were developed using thin film hydration technique. The cryo-TEM analysis confirmed that the prepared optimized liposomal formulation (DFL-2) was a mixture of small unilamellar vesicles (SUVs), large unilamellar vesicles (LUVs) and multilamellar vesicles (MLVs). In addition, the TEM analysis confirmed that the prepared liposomes were of spherical in shape having liposome size in the range of 500-900 nm and zeta potential of about +30 mV. The developed cationic liposomes exhibited sustained release profile of payload of 6‑MNA for over >12 h and about five times higher retention in...Continue Reading

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