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胶束核心脂质体:向更稳健的亲水分子载体发展。

Gelatinized-core liposomes: Toward a more robust carrier for hydrophilic molecules.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, 11566, Egypt.

出版信息

J Biomed Mater Res A. 2017 Nov;105(11):3086-3092. doi: 10.1002/jbm.a.36175. Epub 2017 Aug 21.

DOI:10.1002/jbm.a.36175
PMID:28779507
Abstract

The use of liposomes as a delivery system for hydrophobic and hydrophilic drugs is well recognized. However, they possess several limitations that remained unresolved, including stability problems, low entrapment of the hydrophilic drugs, and the subsequent rapid release. This study introduces a novel approach to incorporate gelatin in the liposomal core to overcome these limitations. A rheological study was conducted to select suitable masses of the gelatin used in the liposomal formulations. Moreover, a full-factorial experimental design was utilized to compare the newly produced gel-core liposomes to the conventional liposomes with respect to the amount of a model hydrophilic molecule loading. An advanced machine learning method, namely, artificial neural networks was utilized to capture the effects of gelatin and cholesterol incorporation in the liposomes on the entrapment efficiency. The results revealed the successful preparation of the novel vesicles and their superiority over the conventional liposomes in drug loading, sustaining the drug release and stability which pose the newly introduced liposomal system as a successful delivery carrier for hydrophilic molecules and drugs. © 2017 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 105A: 3086-3092, 2017.

摘要

脂质体作为疏水性和亲水性药物的递送系统已得到广泛认可。然而,它们存在一些尚未解决的局限性,包括稳定性问题、亲水性药物的包封率低以及随后的快速释放。本研究介绍了一种将明胶纳入脂质体核心的新方法来克服这些局限性。进行了流变学研究以选择适用于脂质体制剂的明胶的合适质量。此外,利用完全析因实验设计比较了新生产的凝胶核脂质体与常规脂质体在模型亲水分子的载药量方面的差异。利用先进的机器学习方法,即人工神经网络来捕捉明胶和胆固醇在脂质体中的掺入对包封效率的影响。结果表明成功制备了新型囊泡,并且与常规脂质体相比,它们在药物载药量、药物释放和稳定性方面具有优越性,这使得新引入的脂质体系统成为亲水分子和药物的有效递送载体。© 2017 Wiley Periodicals, Inc. J 生物材料研究杂志 A 部分:105A:3086-3092,2017。

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