Quercetin-containing self-assemble proliposome preparation and evaluation.
Quercetin-containing self-assemble proliposome preparation and evaluation.
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含槲皮素的自组装前体脂质体的制备及评价。
DOI：
10.1080/08982104.2016.1239635
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发表时间：
2017
影响因子：
4.4
通讯作者：
Du Qian
中科院分区：
文献类型：
--
作者：
Ren Jin;Fang Zhengjie;Jiang Liqun;Du Qian
本研究的目的是研制一种液体自组装前体脂质体，用于槲皮素口服给药。将磷脂、表面活性剂和药物在乙醇中溶解，制备了该液体前体脂质体。这种液体自组装前体脂质体的制备过程只需一步，不需要特殊的设备。并对前体脂质体转化的机理进行了探讨。制备了不同浓度(0%、20%、23%、26%、30%)的槲皮素RH40前体脂质体。RH40浓度越大，粒径越小，多分散指数越小。同时，药物包封率随着克隆莫尔RH40浓度的增加而略有下降。RH40前体脂质体的体外释药时间较长，浓度较高时药物释放较慢。在体肠吸收和药代动力学研究表明，前体脂体能显著提高槲皮苷的吸收和体内生物利用度。此外，所制得的槲皮素前体脂质体在室温下保存具有良好的稳定性。综上所述，成功制备了槲皮素液体自组装前体脂质体。加入乳剂RH40后，可迅速转化为粒径和多分散指数均令人满意的脂质体囊泡。克隆莫尔RH40在制剂中的浓度应低于26%，以获得较高的药物包封率(90%)和较小的刺激性。药物释放受克莫莫尔RH40浓度的影响，通过调整克莫莫尔RH40的含量即可获得所需的药物释放。生物利用度的提高表明，液体自组装前体脂质体有望成为一种口服给药的载体。
The purpose of this study was to develop a liquid self-assemble proliposome for quercetin oral delivery. This liquid proliposome was prepared by dissolving phospholipids, surfactants and drug in ethanol. There was only one step in the preparation process of this liquid self-assemble proliposome and no special devices were required. The mechanism about proliposome transformation was discussed. Quercetin proliposomes with different cremorphor RH40 concentrations (0%, 20%, 23%, 26%, 30%) were prepared. The particle size and polydispersity index decreased as cremorphor RH40 concentration increased. Meantime, the drug entrapped efficiency decreased slightly with an increase in cremorphor RH40 concentration. Thein vitrodrug release showed prolonged drug release in case of proliposome and the release of quercetin was slower when cremorphor RH40 concentration was higher. The absorption of quercetin and itsin vivobioavailability were significantly improved by proliposome, which was evidenced by the in situ intestinal absorption and pharmacokinetic study. Besides, the obtained quercetin proliposome was with good stability when stored at room temperature. In conclusion, quercetin liquid self-assemble proliposome was successfully prepared. It could transform into liposomal vesicle with satisfied particle size and polydispersity index instantly when cremorphor RH40 was added. Cremorphor RH40 concentration in the formulation should below 26% to get higher drug entrapped efficiency (>90%) and less irritation. The drug release was affected by the cremorphor RH40 concentration and the required drug release could be obtained by adjusting cremorphor RH40 content. The enhanced bioavailability showed liquid self-assemble proliposome could be a promising vehicle for the oral delivery of quercetin.