In vitro and in vivo evaluation of docetaxel-loaded stearic acid-modified Bletilla striata polysaccharide copolymer micelles.
Bletilla striata polysaccharides (BSPs) have been used in pharmaceutical and biomedical industry, the aim of the present study was to explore a BSPs amphiphilic derivative to overcome its application limit as poorly water-soluble drug carriers due to water-soluble polymers. Stearic acid (SA) was selected as a hydrophobic block to modify B. striata polysaccharides (SA-BSPs). Docetaxel (DTX)-loaded SA-BSPs (DTX-SA-BSPs) copolymer micelles were prepared and characterized. The DTX release percentage in vitro and DTX concentration in vivo was carried out by using high performance liquid chromatography. HepG2 and HeLa cells were subjected to MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazonium bromide) assay to evaluate the cell viability. In vitro evaluation of copolymer micelles showed higher drug encapsulation and loading capacity. The release percentage of DTX from DTX-SA-BSPs copolymer micelles and docetaxel injection was 66.93 ± 1.79% and 97.06 ± 1.56% in 2 days, respectively. The DTX-SA-BSPs copolymer micelles exhibited a sustained release of DTX. A 50% increase in growth inhibition was observed for HepG2 cells treated with DTX-SA-BSPs copolymer micelles as compared to those treated with docetaxel injection for 72 h. DTX-SA-BSPs copolymer micelles presented a similar growth inhibition effect on Hela cells. Furthermore, absolute bioavailability of DTX-SA-BSPs copolymer micelles was shown to be 1.39-fold higher than that of docetaxel injection. Therefore, SA-BSPs copolymer micelles may be used as potential biocompatible polymers for cancer chemotherapy.
School of Pharmacy, Jilin University, Changchun, China.
Qingxiang
Q
Guan
School of Pharmacy, Jilin University, Changchun, China.
Guangyuan
G
Zhang
School of Pharmacy, Jilin University, Changchun, China.
Dandan
D
Sun
Faculty of Chemistry, Northeast Normal University, Changchun, China.
Yue
Y
Wang
School of Pharmacy, Jilin University, Changchun, China.
Kun
K
Liu
School of Pharmacy, Jilin University, Changchun, China.
Miao
M
Wang
School of Pharmacy, Jilin University, Changchun, China.
Cheng
C
Sun
China-Japan Union Hospital of Jilin University, Changchun, China.
Zhuo
Z
Zhang
The Second Hospital of Jilin University, Changchun, China.
Bingjin
B
Li
China-Japan Union Hospital of Jilin University, Changchun, China.
Jiayin
J
Lv
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D011108:Polymers / Q000737:chemistry*; D011134:Polysaccharides / Q000737:chemistry*; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry*; D043823:Taxoids / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D011134:Polysaccharides; D013229:Stearic Acids; D043823:Taxoids; D000077143:Docetaxel; C031183:stearic acid