Heat-treated emulsions with cross-linking bovine serum albumin interfacial films and different dextran surfaces: Effect of paclitaxel delivery
Heat-treated emulsions with cross-linking bovine serum albumin interfacial films and different dextran surfaces: Effect of paclitaxel delivery
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具有交联牛血清白蛋白界面膜和不同葡聚糖表面的热处理乳液：紫杉醇递送的影响
DOI：
10.1002/jps.23468
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发表时间：
2013-04-01
影响因子：
3.8
通讯作者：
Yao, Ping
中科院分区：
文献类型：
--
作者：
Qi, Jianing;Huang, Chong;Yao, Ping
本研究对一种生物相容性和生物可降解的水包油型疏水性药物缓释乳剂进行了体内外评价。以不同葡聚糖分子量和不同结合度的牛血清白蛋白（BSA）葡聚糖结合物作为乳化剂和稳定剂。紫杉醇（PTX），一种疏水性的抗肿瘤药物，有效地装载在油滴内，通过高压均质。将乳液在90 ° C下加热1小时以消除BSA的过敏反应。由于热处理产生的油水界面处的交联BSA膜和亲水性葡聚糖表面，乳液在血清中稳定，并且对长期储存稳定。体外细胞毒性研究证实未负载乳剂具有生物相容性，负载PTX乳剂具有与PTX溶液相似的抗肿瘤活性。小鼠腹水型肝癌H22荷瘤小鼠的体内研究表明，具有更短和更致密的葡聚糖表面的PTX负载的乳液具有比商业PTX注射剂更好的肿瘤抑制和存活效力。(c)2013 Wiley Periodicals，Inc.和American Pharmacologist Association J Pharm Sci 102：13071317，2013
In this study, a type of biocompatible and biodegradable oil-in-water emulsion for hydrophobic drug delivery was evaluated in vitro and in vivo. Bovine serum albumin (BSA)dextran conjugates with different dextran molecular weights and different conjugation degrees were used as the emulsifier and stabilizer. Paclitaxel (PTX), a hydrophobic antitumor drug, was effectively loaded inside the oil droplets via high-pressure homogenization. The emulsions were heated at 90 degrees C for 1h to eliminate the anaphylaxis of BSA. By virtue of the cross-linked BSA films at the oilwater interfaces produced by the heat treatment and the hydrophilic dextran surfaces, the emulsions are stable in blood serum, as well as stable against long-term storage. In vitro cytotoxicity study verifies that the unloaded emulsions are biocompatible and the PTX-loaded emulsions have similar antitumor activity as PTX solution. In vivo investigation of murine ascites hepatoma H22-tumor-bearing mice demonstrates that the PTX-loaded emulsion with shorter and denser dextran surface has better tumor inhibition and survivability efficacy than the commercial PTX injection. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:13071317, 2013