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K5多糖-棉酚纳米载体构建及药物传递研究
发表时间：2016-03-15 浏览量：2224 下载量：1077
| 全部作者： | 施瑜，彭换换，田慧慧，王睿，徐晓宇，陈敬华 |
| 作者单位： | 江南大学药学院 |
| 摘 要： | 抗前列腺癌药物棉酚（gossypol，GP）水溶性差，治疗选择性不佳，毒副作用大。研究制备了基于硼酸酯键的pH响应型K5多糖-GP缀合物（简记KGP），考察其自组装和体外药物释放行为，并初步评价其对前列腺癌细胞的抑制作用。结果表明，KGP可在水溶液中自组装形成平均粒径为221.6 nm的纳米粒子；体外药物释放实验证实其可表现出受pH调控的释药行为，在pH=5.0酸性环境下药物释放速率较pH=7.4下更快。体外细胞毒性结果显示其能显著抑制前列腺癌细胞增殖，并且对正常细胞毒性较小，表现出治疗的选择性。细胞摄取结果表明，异硫氰酸荧光素（fluorescein isothiocyanate，FITC）标记KGP可被PC-3细胞迅速摄取，且摄取率高于COS7细胞。KGP纳米载体有望用于治疗前列腺癌。 |
| 关 键 词： | 药剂学；K5多糖；棉酚；硼酸酯；前列腺癌 |
| Title： | Construction of K5 polysaccharide-gossypol nanocarrier for drug delivery |
| Author： | SHI Yu, PENG Huanhuan, TIAN Huihui, WANG Rui, XU Xiaoyu, CHEN Jinghua |
| Organization： | School of Pharmaceutical Sciences, Jiangnan University |
| Abstract： | Gossypol is a chemotherapeutic agent for prostate cancer therapy, but its poor solubility, lack of selectivity and high side-effects limit the application. In this paper, a K5 polysaccharede-gossypol conjugate (KGP) based on boronate ester, which is pH sensitive, was prepared as a drug delivery system. The self-assembly, in vitro drug release behaviors, and anticancer efficacy were evaluated. The results showed that KGP could self-assemble into nanoparticles in water medium with the average size at 221.6 nm. In vitro drug release assay indicated the drug release rate could be adjusted by the variation of pH values. The nanoparticles exhibited faster drug release rate at acidic pH=5.0 than that at pH=7.4. The cytotoxicity assay in vitro illustrated that KGP could significantly inhibit the proliferation of prostate cancerous cells as compared with that of normal cells, showing favaroble selectivity. Moreover, fluorescein isothiocyanate (FITC) labeled KGP had rapid cellular internalization of PC-3 cells as compared with COS7 cells. In general, it suggested that KGP could be a promising nanocarrier for therapy of prostate cancer. |
| Key words： | pharmaceutics; K5 polysaccharide; gossypol; boronate ester; prostate cancer |
| 发表期数： | 2016年3月第5期 |
| 引用格式： | 施瑜，彭换换，田慧慧，等. K5多糖-棉酚纳米载体构建及药物传递研究[J]. 中国科技论文在线精品论文，2016，9（5）：512-517. |
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