Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: synthesis, characterization, and in vivo biodistribution
- Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: synthesis, characterization, and in vivo biodistribution
- G. Saravanakumar; 민경현; 민동식; 김아영; 이창문; 조용우; 이상천; 김광명; 정서영; 박기남; 박재형; 권익찬
- Hydrotropic oligomer; Glycol chitosan; Self-assembled nanoparticles; Paclitaxel; Cancer therapy
- Issue Date
- Journal of controlled release : official journal of the Controlled Release Society
- VOL 140, 210-217
- 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.
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