title: Preparation of pingyangmycin PLGA microspheres and related in vitro/in vivo studies.
abstract: Using a multiple emulsion solvent evaporation method, pingyangmycin was entrapped in poly(lactic-co-glycolic acid) (PLGA) to prepare a long-acting pingyangmycin PLGA microsphere formulation that can be sustainably released with high entrapment efficiency. Meanwhile, the effects of stirring speed during the multiple emulsion solvent evaporation process were also taken into consideration. Investigation of the in vitro release properties showed that the microsphere formulations could sustainably release the drug over nearly 28 d, and, moreover, it could stably control pingyangmycin release over nearly 24 d when intramuscularly injected into dogs. No serious toxic effect was observed in an acute toxicity test in mice. A subcutaneous xenotransplant model of hepatoma H(22) in mice was established for pharmacodynamic studies and the results showed that the process of preparing pingyangmycin PLGA microsphere formulations was feasible and that intramuscular injection of this microsphere formulation resulted in anti-tumor activity in vivo.
authors.affiliation: School of Pharmacy, Jilin University, Changchun, 130021 Jilin, PR China. hanb@jlu.edu.cn
authors.forename: Bing
authors.initials: B
authors.lastname: Han
authors.forename: Hao-Tian
authors.initials: HT
authors.lastname: Wang
authors.forename: Huai-Yu
authors.initials: HY
authors.lastname: Liu
authors.forename: Hua
authors.initials: H
authors.lastname: Hong
authors.forename: Wei
authors.initials: W
authors.lastname: Lv
authors.forename: Zu-Hui
authors.initials: ZH
authors.lastname: Shang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D001761:Bleomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D045744:Cell Line, Tumor; D004285:Dogs; D005260:Female; D006801:Humans; D019344:Lactic Acid / Q000138:chemical synthesis* / Q000627:therapeutic use; D008297:Male; D051379:Mice; D008863:Microspheres; D011100:Polyglycolic Acid / Q000138:chemical synthesis* / Q000627:therapeutic use; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011897:Random Allocation; D013678:Technology, Pharmaceutical / Q000379:methods*; D023041:Xenograft Model Antitumor Assays / Q000379:methods
chemical_list: D000970:Antineoplastic Agents; D001761:Bleomycin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C025703:bleomycetin