期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 394, 期 1-2, 页码 154-161出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2010.04.041
关键词
Hyaluronic acid; Hydrotropic oligomer; Paclitaxel; Self-assembled nanoparticles
资金
- Kyung Hee University [KHU-20090715]
- National Research Foundation of Korea [과06A2601] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Amphiphilic hyaluronic acid conjugates were synthesized as a potential drug carrier by chemical conjugation of an amine-terminated hydrotropic oligomer, which has a unique ability to enhance the solubility of paclitaxel (PTX), to a hyaluronic acid (HA) backbone using carbodiimide chemistry. The physicochemical properties of the hydrotropic hyaluronic acid (HydroHA) conjugates were investigated using H-1 NMR, dynamic light scattering, transmission electron microscopy (TEM), and fluorescence spectroscopy. HydroHA conjugates could form self-assembled nanoparticles in an aqueous medium because of hydrophobic interactions among hydrotropic oligomers. Their particle sizes were in the range of 274-356 nm, depending on the degree of substitution (DS) of the hydrotropic oligomer. TEM images showed that particle morphology was spherical in shape. Critical aggregation concentrations of HydroHA conjugates ranged from 0.034 to 0.125 mg/mL, which decreased with an increase in the DS of the hydrotropic oligomer. The HydroHA conjugates were selectively taken up by the cancer cell line (SCC7) over-expressing CD44, a hyaluronic receptor. The nanoparticles could encapsulate PTX up to 20.7 wt.% by the dialysis method. The in vitro release pattern of PTX from nanoparticles was significantly dependent on drug loading content, in which the release rate was lower for the nanoparticles that contained larger amounts of the drug. From the cytotoxicity test, it was found that the drug-loaded HydroHA nanoparticles exhibited stronger cytotoxicity to SCC-7 than to normal fibroblast cell (CV-1). These results suggest that HydroHA nanoparticles have potential as the carrier of PTX for cancer therapy. (C) 2010 Elsevier B.V. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据