Preparation and characterization of novel polymeric micelles for 9-nitro-20(S)-camptothecin delivery.
9-Nitro-20(S)-camptothecin (9-NC) has achieved remarkable curative effect in anticancer research. However, the clinical application of 9-NC is largely hampered by its poor solubility and stability. In this paper, novel amphiphilic block copolymers derived from d,l-lactide, trimethylene carbonate, and methylated poly(ethylene glycol) (mPEG) (PECA) with different molecular weight were synthesized and characterized. Self-assembly PECA micelles loaded with 9-NC were prepared. The micelles were regular spheres with a diameter ranged from 20 to 120 nm. The critical micelle concentration (CMC) decreased with the increase of the hydrophobic components. The solubility of 9-NC was improved obviously with micelle encapsulation. The stability experiments proved that over 90% of 9-NC could keep its lactone form in micelle solution after incubating in phosphate-buffered saline for 100 min, while the corresponding proportion for free drug solution was 25%. The release of 9-NC was nearly zero-order after the burst release, and the long hydrophobic chain length led to slower release rate. The novel PECA copolymer micelles could be effective carriers to improve the solubility, stability, and release performance of 9-NC.
Gao
Jieming
J
College of Material Science and Engineering, Southwest Jiaotong University, Chengdu, PR China.
Ming
Jing
J
He
Bin
B
Fan
Yujiang
Y
Gu
Zhongwei
Z
Zhang
Xingdong
X
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004146:Dioxanes; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004355:Drug Stability; D004563:Electrochemistry; D005079:Excipients; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D010316:Particle Size; D011092:Polyethylene Glycols; D011108:Polymers; D012995:Solubility; D013816:Thermodynamics
D000970:Antineoplastic Agents; D004146:Dioxanes; D004337:Drug Carriers; D005079:Excipients; D008823:Micelles; D011108:Polymers; D011092:Polyethylene Glycols; C443643:trimethylene carbonate; C079905:rubitecan; D002166:Camptothecin