Remote loading of diclofenac, insulin and fluorescein isothiocyanate labeled insulin into liposomes by pH and acetate gradient methods
Remote loading of diclofenac, insulin and fluorescein isothiocyanate labeled insulin into liposomes by pH and acetate gradient methods
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DOI：
10.1016/s0378-5173(98)00392-5
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发表时间：
1999-03-01
影响因子：
5.8
通讯作者：
Nagai, T
中科院分区：
文献类型：
--
作者：
Hwang, SH;Maitani, Y;Nagai, T
研究了模型药物双氯芬酸、胰岛素和异硫氰酸荧光素标记的胰岛素（FITC-胰岛素）通过形成跨膜梯度远程装载到脂质体中。通过醋酸钙梯度法获得了几乎100%的双氯芬酸脂质体捕获效率，而通过常规反相蒸发囊泡法制备的脂质体具有1-8%的捕获效率。从捕集效率和药物释放来看，与胆固醇相比，大豆甾醇是二棕榈酰磷脂酰胆碱双层膜更好的稳定剂。pH梯度法导致5-50%的FITC-胰岛素脂质体捕获效率，而胰岛素不能通过该方法负载。脂质体响应于胰岛素释放钙黄绿素，表明胰岛素在跨膜梯度的存在下与脂质体膜相互作用。本工作已经证明了一种远程加载弱酸，如双氯芬酸脂质体的醋酸盐梯度法。从pH梯度法将FITC-胰岛素远程负载到脂质体的结果来看，该方法可用于脂质体肽的制备。(C)1999 Elsevier Science B. V.保留所有权利。
Remote loading of the model drugs diclofenac, insulin and fluorescein isothiocyanate labeled insulin (FITC-insulin) into liposomes by formation of transmembrane gradients were examined. A trapping efficiency of almost 100% was obtained for liposomal diclofenac, by the calcium acetate gradient method, whereas liposomes prepared by the conventional reverse-phase evaporation vesicle method had 1-8% trapping efficiencies. Soybean-derived sterol was a better stabilizer of the dipalmitoylphosphatidylcholine bilayer membrane than cholesterol, as shown from trapping efficiencies and drug release. The pH gradient method resulted in a 5-50% of FITC-insulin liposomal trapping efficiency, while insulin could not be loaded by this method. Liposomes released calcein in response to insulin, showing insulin interacts with the liposomal membrane in the presence of a transmembrane gradient. The present work has demonstrated a remote loading method for weak acids such as diclofenac into liposomes by the acetate gradient method. From the result of remote loading of FITC-insulin into liposomes by the pH gradient method, this method may be available for the preparation of liposomal peptides. (C) 1999 Elsevier Science B.V. All rights reserved.