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研究海藻酸钠-MaterBi®干燥乳液制备的聚合物薄膜的体外亲水性和疏水性双重药物释放。

Investigation of in vitro hydrophilic and hydrophobic dual drug release from polymeric films produced by sodium alginate-MaterBi® drying emulsions.

机构信息

Smart Materials, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy; Dipartimento di Informatica Bioingegneria, Robotica e Ingegneria dei Sistemi (DIBRIS), Universita Degli Studi di Genova, Via All'Opera Pia 13, 16145 Genova, Italy.

Smart Materials, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy; Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.

出版信息

Eur J Pharm Biopharm. 2018 Sep;130:71-82. doi: 10.1016/j.ejpb.2018.06.019. Epub 2018 Jun 18.

Abstract

Emulsions are known to be effective carriers of hydrophobic drugs, and particularly injectable emulsions have been successfully implemented for in vivo controlled drug release. Recently, high internal phase emulsions have also been used to produce porous polymeric templates for pharmaceutical applications. However, emulsions containing dissolved biopolymers both in the oil and water phases are very scarce. In this study, we demonstrate such an emulsion, in which the oil phase contains a hydrophobic biodegradable polymer, MaterBi®, and the water phase is aqueous sodium alginate dispersion. The two phases were emulsified simply by ultrasonic processing without any surfactants. The emulsions were stable for several days and were dried into composite solid films with varying MaterBi®/alginate fractions. The films were loaded with two model drugs, a hydrophilic eosin-based cutaneous antiseptic and the hydrophobic curcumin. Drug release capacity of the films was investigated in detail, and controlled release of each model drug was achieved either by tuning the polymer fraction in the films during emulsification or by crosslinking sodium alginate fraction of the films by calcium salt solution immersion. The emulsions can be formulated to carry either a single model drug or both drugs depending on the desired application. Films demonstrate excellent cell biocompatibility against human dermal fibroblast, adult cells.

摘要

乳液是众所周知的疏水药物的有效载体,特别是可注射乳液已成功地用于体内控制药物释放。最近,高内相比乳液也被用于生产用于药物应用的多孔聚合物模板。然而,含有溶解的生物聚合物的乳液在油相和水相都非常罕见。在本研究中,我们展示了这样一种乳液,其中油相含有疏水性可生物降解聚合物 MaterBi®,而水相是水性海藻酸钠分散体。这两种相通过简单的超声处理乳化,而不使用任何表面活性剂。乳液在数天内保持稳定,并通过改变 MaterBi®/海藻酸钠的比例干燥成具有不同比例的复合固体膜。将两种模型药物,亲水性基于曙红的皮肤防腐剂和疏水性姜黄素载入到薄膜中。详细研究了薄膜的药物释放能力,并通过在乳化过程中调整薄膜中的聚合物比例或通过钙盐溶液浸泡交联薄膜中的海藻酸钠部分来实现每种模型药物的控制释放。根据所需的应用,可以配制乳液以携带单一模型药物或两种药物。薄膜对人真皮成纤维细胞、成人细胞表现出极好的细胞生物相容性。

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