title: Poly(DL-lactide-co-glycolide) microporous microsphere-based depot formulation of a peptide-like antineoplastic agent.
abstract: In the present investigation, a poly(DL-co-glycolide) (PLGA)-based, microspheric depot system for bleomycin (BLM) has been formulated, and the same has been evaluated in-vivo in C57BL/6J mice bearing transplantable melanoma B16F1 murine solid tumour. The microparticulate delivery systems were formulated employing a water-in-oil-in-water (W/O/W) emulsion-solvent evaporation technique and characterized in-vitro. The microspheres were injected subcutaneously to form a drug depot at the site of injection in mice bearing experimental tumours and the drug was continuously infused into the systemic circulation with progressive biodegradation. The drug-loaded microspheres exhibited improved pharmacodynamic efficacy, as evidenced by retarded tumour growth kinetics. Preliminary pharmacokinetic studies illustrated controlled release of the drug into the systemic circulation over the study period to exert an anti-neoplastic action. These studies demonstrated the feasibility of employing a PLGA-based microparticulate system as an effective biodegradable, injectable, depot-forming therapeutic system for long-term administration of anti-neoplastic agents.
authors.affiliation: Dr T.M.A. Pai Pharmaceutical Research Centre, College of Pharmaceutical Sciences, Manipal 576 119, Karnataka, India. shenoydin@yahoo.com
authors.forename: D B
authors.initials: DB
authors.lastname: Shenoy
authors.forename: R J
authors.initials: RJ
authors.lastname: D'Souza
authors.forename: N
authors.initials: N
authors.lastname: Udupa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001673:Biodegradation, Environmental; D002214:Capsules; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D066298:In Vitro Techniques; D019344:Lactic Acid; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000378:metabolism; D051379:Mice; D008810:Mice, Inbred C57BL; D008863:Microspheres; D010316:Particle Size; D010455:Peptides / Q000008:administration & dosage / Q000493:pharmacokinetics; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers
chemical_list: D000970:Antineoplastic Agents; D002214:Capsules; D003692:Delayed-Action Preparations; D010455:Peptides; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid