The application of poly (glycerol-sebacate) as biodegradable drug carrier.
Poly (glycerol-sebacate) (PGS) is an elastomeric biodegradable polymer which possesses the ideal properties of drug carriers. In the present study, we prepared a series of PGS implants (5-FU-PGSs) loaded with different weight percent of 5-fluorouracil (2, 5, 7.5 and 10%). We studied the infrared spectrum properties, in vitro degradation and drug release, in vivo degradation and tissue biocompatibility of 5-FU-PGSs, in order to provide detailed information for the application of PGS as biodegradable drug carrier in cancer therapy. Macroscopically, all 5-FU-PGS wafers in phosphate buffer solution (PBS) kept their geometries during the degradation period of 30 days. The in vitro degradation rates of 5-FU-PGSs were accelerated when higher concentration of 5-FU was doped. Scanning electron microscopy observation showed that the surfaces of 5-FU-PGSs with higher concentration of 5-FU had irregular pits. The cumulative drug release profiles of 5-FU-PGSs exhibited a biphasic release with an initial burst release in the first day. After 7 days, almost 100% cumulative release of 5-FU was found for all 5-FU-PGSs.The degradation rate of 5-FU-PGSs in vivo was much quicker than that in vitro. Hematoxylin and eosin staining showed that no remarkable inflammations were observed in the tissue surrounding 5-FU-PGS implants, suggesting 5-FU-PGSs had good biocompatibility and no tissue toxicity. In vitro anti-tumor activity assay suggested that 5-FU-PGSs exhibited anti-tumor activity through sustained-release drug mode. These results demonstrate that PGS is a candidate of biodegradable drug carriers.
Sun
Zhi-Jie
ZJ
Center for Biomedical Materials and Engineering, Harbin Engineering University, 145 Nantong Street, Nangang District, Harbin 150001, PR China. zhijiesun2005@yahoo.com.cn
Chen
Chang
C
Sun
Ming-Zhen
MZ
Ai
Chang-Hong
CH
Lu
Xi-Li
XL
Zheng
Yu-Feng
YF
Yang
Bao-Feng
BF
Dong
De-Li
DL
D020341:Absorbable Implants; D000230:Adenocarcinoma / Q000188:drug therapy; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000378:metabolism / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D003651:Decanoates / Q000737:chemistry / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism*; D005260:Female; D005472:Fluorouracil / Q000008:administration & dosage* / Q000378:metabolism / Q000627:therapeutic use; D005990:Glycerol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D011108:Polymers / Q000737:chemistry / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared
D000964:Antimetabolites, Antineoplastic; D003651:Decanoates; D004337:Drug Carriers; D011108:Polymers; C469892:poly(glycerol-sebacate); D005990:Glycerol; D005472:Fluorouracil