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

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Title: Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: Synthesis, characterization, and in vivo biodistribution
Authors: Saravanakumar, G.1, Min, Kyung Hyun2,3, Min, Dong Sik2,3, Kim, Ah Young2,3, Lee, Chang-Moon4, Cho, Yong Woo4, Lee, Sang Cheon5, Kim, Kwangmeyung3, Jeong, Seo Young2, Park, Kinam6, Park, Jae Hyung1,2, Kwon, Ick Chan3 ikwon@kist.re.kr
Source: Journal of Controlled Release. Dec2009, Vol. 140 Issue 3, p210-217. 8p.
Subjects: Oligomers, Chitosan, Paclitaxel, Water-soluble polymers, Cancer treatment, Nanoparticles, Drug carriers
Abstract: 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±13nm in a phosphate-buffered saline (PBS, pH 7.4 at 37°C). HO-GC nanoparticles maintained their structure for up to 50days in PBS. They could encapsulate a high quantity (20wt.%) of paclitaxel (PTX) with a maximum drug-loading efficiency of 97%, due to the presence of hydrotropic inner cores. When HO-GC-PTX particles were exposed to the 0.1M 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/ethanol mixture. 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-GC-PTX nanoparticles might be a promising carrier for PTX delivery in cancer therapy. [Copyright &y& Elsevier]
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Database: Engineering Source
Description
Abstract: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±13nm in a phosphate-buffered saline (PBS, pH 7.4 at 37°C). HO-GC nanoparticles maintained their structure for up to 50days in PBS. They could encapsulate a high quantity (20wt.%) of paclitaxel (PTX) with a maximum drug-loading efficiency of 97%, due to the presence of hydrotropic inner cores. When HO-GC-PTX particles were exposed to the 0.1M 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/ethanol mixture. 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-GC-PTX nanoparticles might be a promising carrier for PTX delivery in cancer therapy. [Copyright &y& Elsevier]
ISSN:01683659
DOI:10.1016/j.jconrel.2009.06.015