title: Evaluation of in vitro and in vivo antitumor activity of BCNU-loaded PLGA wafer against 9L gliosarcoma.
abstract: The purpose of the present study was to develop implantable BCNU-loaded poly(D,L-lactide-co-glycolide) (PLGA) wafer for the controlled release of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) and to evaluate its in vitro and in vivo antitumor activity. The release rate of BCNU from PLGA wafer increased with the increase of BCNU amount loaded and the release was continued until 7 days. In vitro and in vivo antitumor activity of BCNU-loaded PLGA wafer was investigated using in vitro cytotoxicity against 9L gliosarcoma cells and a subcutaneous (s.c.) solid tumor model of 9L gliosarcoma, respectively. The wafers containing BCNU showed more effective cytotoxicity than BCNU powder due to its short half-life and inhibited the proliferation of 9L gliosarcoma cells. BCNU-loaded PLGA wafer delayed the growth of the tumors significantly and increasing the dose of BCNU in the wafer resulted in a substantial regression of the tumor. These results of antitumor activity of BCNU-loaded PLGA wafer demonstrate the feasibility of the wafers for clinical application.
authors.affiliation: Department of Advanced Organic Materials Engineering, Chonbuk National University, Jeonju, South Korea.
authors.forename: Jin Soo
authors.initials: JS
authors.lastname: Lee
authors.forename: Tae Kun
authors.initials: TK
authors.lastname: An
authors.forename: Gang Soo
authors.initials: GS
authors.lastname: Chae
authors.forename: Je Kyo
authors.initials: JK
authors.lastname: Jeong
authors.forename: Sun Hang
authors.initials: SH
authors.lastname: Cho
authors.forename: Hai Bang
authors.initials: HB
authors.lastname: Lee
authors.forename: Gilson
authors.initials: G
authors.lastname: Khang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002330:Carmustine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D018316:Gliosarcoma / Q000188:drug therapy / Q000378:metabolism*; D019344:Lactic Acid / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008297:Male; D011100:Polyglycolic Acid / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D011916:Rats, Inbred F344
chemical_list: D000970:Antineoplastic Agents; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002330:Carmustine