Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: synthesis, characterization, and in vivo biodistribution

Title
Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: synthesis, characterization, and in vivo biodistribution
Authors
G. Saravanakumar민경현민동식김아영이창문조용우이상천김광명정서영박기남박재형권익찬
Keywords
Hydrotropic oligomer; Glycol chitosan; Self-assembled nanoparticles; Paclitaxel; Cancer therapy
Issue Date
2009-11
Publisher
Journal of controlled release : official journal of the Controlled Release Society
Citation
VOL 140, 210-217
Abstract
Development of successful formulations for poorly water-soluble drugs remains a longstanding critical and challenging issue in cancer therapy. As a potential drug carrier of paclitaxel, hydrotropic oligomer-glycol chitosan (HO-GC) was synthesized by chemical conjugation of the N,N-diethylnicotinamide-based oligomer, uniquely designed for enhancing the aqueous solubility of paclitaxel, to the backbone of glycol chitosan. Owing to its amphiphilicity, the conjugate formed self-assembled nanoparticles with a mean diameter of 313± 13 nm in a phosphate-buffered saline (PBS, pH 7.4 at 37 °C). HO-GC nanoparticles maintained their structure for up to 50 days in PBS. They could encapsulate a high quantity (20 wt.%) of paclitaxel (PTX) with amaximum drug-loading efficiency of 97%, due to the presence of hydrotropic inner cores.When HO-GC-PTX particles were exposed to the 0.1 M sodium salicylate solution in PBS (pH 7.4), PTX was released from nanoparticles in a sustained manner. From the cytotoxicity test, it was confirmed that HO-GC-PTX nanoparticles showed lower cytotoxicity than free PTX formulation in 50%/50% Cremophor EL/ethanolmixture. The optical imaging results indicated that near-infrared fluorescence dye (Cy5.5)-labeled HO-GC-PTX showed an excellent tumor specificity in SCC7 tumor-bearing mice, due to the enhanced permeation and retention effect. Overall, HO-GCPTX nanoparticles might be a promising carrier for PTX delivery in cancer therapy.
URI
http://pubs.kist.re.kr/handle/201004/36439
ISSN
0168-3659
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KIST Publication > Article
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