title: Preparation and evaluation of PLGA microparticles as carrier for the pulmonary delivery of rhIL-2 : I. Effects of some formulation parameters on microparticle characteristics.
abstract: In this study, recombinant human interleukin-2 (rhIL-2) containing poly(lactic-co-glycolic acid) (PLGA) microparticles were prepared for pulmonary administration by modified w/o/w double emulsion solvent extraction method and the effects of various formulation parameters on the physicochemical properties of the microparticles were investigated. Microparticles in suitable size for pulmonary administration (4.02 µm) were obtained by increasing dichloromethane volume used in the organic phase. Also, a very high encapsulation efficiency (99.22%) value could be reached in these microparticles. In the sodium dodecyl sulphate-polyacrylamide gel electrophoresis analysis, rhIL-2 extracted from microparticles having a similar band with native rhIL-2 showed that the protein was not affected by the encapsulation process. The release curves of microparticles exhibited a biphasic fashion, characterized by a fast release phase at initial 1 day, followed by a slower one on the remaining days. Bioactivity investigations using T cells show that rhIL-2 encapsulated in PLGA microparticles retain their biological activity.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100 Tandoğan, Ankara, Turkey.
authors.forename: Burcu
authors.initials: B
authors.lastname: Devrim
authors.forename: Asuman
authors.initials: A
authors.lastname: Bozkir
authors.forename: Kandemir
authors.initials: K
authors.lastname: Canefe
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D016503:Drug Delivery Systems; D006801:Humans; D007376:Interleukin-2 / Q000008:administration & dosage* / Q000494:pharmacology; D019344:Lactic Acid / Q000737:chemistry*; D008168:Lung / Q000378:metabolism*; D008175:Lung Neoplasms / Q000188:drug therapy; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D055550:Protein Stability; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000494:pharmacology; D013601:T-Lymphocytes / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D007376:Interleukin-2; D011994:Recombinant Proteins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid