title: Liposomes and PLG microparticles as sustained release antitubercular drug carriers--an in vitro-in vivo study.
abstract: Liposomes and PLG microparticles were investigated as sustained release antitubercular drug carriers for isoniazid (INH) and rifampicin (RIF). In vitro release of drugs from liposomes showed a sustained release of INH and RIF up to 4 weeks. PLG microparticles exhibited a sustained release of INH and RIF up to 6 and 49 days, respectively. In vivo drug disposition studies from liposomes indicated a sustained release of INH in plasma and various tissues up to 24 h and 5 days, respectively, while release of rifampicin was obtained for 24 and 72 h in plasma and various tissues. In vivo drug disposition studies from PEG-PLG microparticles indicated a sustained release of INH up to 9 and 27 days in plasma and various tissues, while rifampicin was detected in plasma and lungs up to 12 h and 27 days. Hepatotoxicity studies revealed no toxicity induced using biochemical tests. PLG microparticles exhibited a more sustained release of antitubercular drugs than a liposomal carrier system.
authors.affiliation: Department of Biochemistry, Postgraduate Institute of Medical Education and Research, Chandigarh 160 012, India.
authors.forename: M
authors.initials: M
authors.lastname: Dutt
authors.forename: G K
authors.initials: GK
authors.lastname: Khuller
mesh_terms: D000469:Alkaline Phosphatase / Q000097:blood; D000818:Animals; D000904:Antibiotics, Antitubercular / Q000097:blood / Q000493:pharmacokinetics*; D000995:Antitubercular Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000633:toxicity; D001219:Aspartate Aminotransferases / Q000097:blood; D001663:Bilirubin / Q000097:blood; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005260:Female; D007538:Isoniazid / Q000378:metabolism; D019344:Lactic Acid; D008081:Liposomes; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D008297:Male; D051379:Mice; D010316:Particle Size; D011092:Polyethylene Glycols; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D012293:Rifampin / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D000904:Antibiotics, Antitubercular; D000995:Antitubercular Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008081:Liposomes; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D001219:Aspartate Aminotransferases; D000469:Alkaline Phosphatase; D001663:Bilirubin; D007538:Isoniazid; D012293:Rifampin