[Preparation of adriamycin-loaded temperature/pH sensitive self-assembly block copolymer micelles].
The dialysis method was employed to load adriamycin into the micelles formed by temperature and pH sensitive polyhistidine-co-DL-lactide-co-glycolide-polyethylene glycol poly DL-lactide-co-glycolide-co-histidine (OLH-b-PLGA-b-PEG-b-PLGA-b-OLH). The critical micelle concentration (CMC) of the copolymer was measured with pyrene fluorescent probe method under different temperatures. The entrapment rate and drug-loading rate were determined with dialysis method. The diameter, morphology and surface potential of the copolymer micelles were investigated by corresponding instruments, respectively. The release behavior of adriamycin from copolymer micelles and the pH sensitivity were studied. The CMC of the copolymers ranged from 0.022 4 to 0.001 7 microg x mL(-1). The entrapment rate and drug-loading rate were 92.8% and 15.7%, respectively. The micelles have a mean diameter of (61.7 +/- 13.4) nm, and zeta potential was -9.88 mV. The in vitro adriamycin release rate increased with the pH dropping from 7.4 to 5.0. The results indicated that the CMC of the copolymers decreased as the raising of temperature, drug release behavior from the micelles possessed clearly pH sensitivity, and the copolymers may have a potential in targeted delivery system for anticancer drugs.
Gu
Jian-Chun
JC
School of Pharmaceutical Sciences, Shenyang Pharmaceutical University, Shenyang 110016, China.
Qiao
Ming-Xi
MX
Gao
Wei
W
Zhao
Xiu-Li
XL
Hu
Hai-Yang
HY
Xu
Jia
J
Jin
Yun-Huan
YH
Chen
Da-Wei
DW
D004317:Doxorubicin / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D004337:Drug Carriers; D006863:Hydrogen-Ion Concentration; D008823:Micelles; D011092:Polyethylene Glycols / Q000737:chemistry; D011098:Polyglactin 910 / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods*; D013696:Temperature
D004337:Drug Carriers; D008823:Micelles; C102418:poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer; D011098:Polyglactin 910; D011092:Polyethylene Glycols; D004317:Doxorubicin