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

Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization. Research Abstract Details 

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Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization. Abstract Text:

Sang Cheon Lee,Kang Moo Huh,Jaehwi Lee,Yong Woo Cho,Raymond E Galinsky,Kinam Park,

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.

Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization. Publishing Authors By Initials

SC Lee,KM Huh,J Lee,YW Cho,RE Galinsky,K Park,

For similar environment and public health: environment: environment, controlled: temperature research abstracts see: environment and public health: environment: environment, controlled: temperature research

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Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Biomacromolecules

VOLUME: 8

Page Numbers: 202-8

Journal Abbreviation: Biomacromolecules

ISSN: 1525-7797

DAY: 3

MONTH: Jan

YEAR: 2007

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

Number of References:

LANGUAGE: eng

NlmUniqueID: 100892849

Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization. Keywords Mesh Terms:

KEYWORDS: Temperature

MESH TERMS: chemistry

Chemical & Substance for Abstract: Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization. Information

Substance Name: Paclitaxel

Registry Number: 33069-62-4

Grant and Affiliation Information for Hydrotropic polymeric micelles for enhanced paclitaxel solubility: in vitro and in vivo characterization.

AFFILIATION: Nanomaterials Application Division, Korea Institute of Ceramic Engineering and Technology, Seoul 153-801, Korea.

Country: United States

AGENCY: United States NIGMS

GRANT: GM 65284

ACRONYM: GM

MEDLINETA: Biomacromolecules

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