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Hydrotropic polymeric micelles for enhanced paclitaxel solubility: In vitro and in vivo characterization

Title
Hydrotropic polymeric micelles for enhanced paclitaxel solubility: In vitro and in vivo characterization
Author
조용우
Keywords
AMPHIPHILIC DIBLOCK COPOLYMERS; BLOCK-COPOLYMER; ORAL BIOAVAILABILITY; DRUG-DELIVERY; TAXOL; FORMULATIONS; FLUORESCENCE; NANOSPHERES; CARRIERS; ANESTHESIA
Issue Date
2007-01
Publisher
AMER CHEMICAL SOC
Citation
BIOMACROMOLECULES, v. 8, No. 1, Page. 202-208
Abstract
The purpose of this investigation was to characterize the in vitro stability and in vivo disposition of paclitaxel in rats after solubilization of paclitaxel into hydrotropic polymeric micelles. The amphiphilic block copolymers consisted of a micellar shell-forming poly(ethylene glycol) (PEG) block and a core-forming poly(2-(4-vinylbenzyloxy)-N,N-diethylnicotinamide) (P(VBODENA)) block. N,N-Diethylnicotinamide (DENA) in the micellar inner core resulted in effective paclitaxel solubilization and stabilization. Solubilization of paclitaxel using polymeric micelles of poly(ethylene glycol)-b-P(D,L-lactide) (PEG-b-PLA) served as a control for the stability study. Up to 37.4 wt % paclitaxel could be loaded in PEG-b-P(VBODENA) micelles, whereas the maximum loading amount for PEG-b-PLA micelles was 27.6 wt %. Thermal analysis showed that paclitaxel in the polymeric micelles existed in the molecularly dispersed amorphous state even at loadings over 30 wt %. Paclitaxel-loaded hydrotropic polymeric micelles retained their stability in water for weeks, whereas paclitaxel-loaded PEG-b-PLA micelles precipitated in a few days. Hydrotropic polymer micelles were more effective than PEG-PLA micelle formulations in inhibiting the proliferation of human cancer cells. Paclitaxel in hydrotropic polymer micelles was administered orally (3.8 mg/kg), intravenously (2.5 mg/kg), or via the portal vein (2.5 mg/kg) to rats. The oral bioavailability was 12.4% of the intravenous administration. Our data suggest that polymeric micelles with a hydrotropic structure are superior as a carrier of paclitaxel due to a high solubilizing capacity combined with long-term stability, which has not been accomplished by other existing polymeric micelle systems.
URI
https://pubs.acs.org/doi/abs/10.1021/bm060307bhttp://repository.hanyang.ac.kr/handle/20.500.11754/106208
ISSN
1525-7797
DOI
10.1021/bm060307b
Appears in Collections:
COLLEGE OF ENGINEERING SCIENCES[E](공학대학) > MATERIALS SCIENCE AND CHEMICAL ENGINEERING(재료화학공학과) > Articles
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