Preparation of pingyangmycin PLGA microspheres and related in vitro/in vivo studies.
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.
Han
Bing
B
School of Pharmacy, Jilin University, Changchun, 130021 Jilin, PR China. hanb@jlu.edu.cn
Wang
Hao-Tian
HT
Liu
Huai-Yu
HY
Hong
Hua
H
Lv
Wei
W
Shang
Zu-Hui
ZH
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
D000970:Antineoplastic Agents; D001761:Bleomycin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C025703:bleomycetin