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一种新型药物递送系统的研发:包埋于海藻酸盐微粒中的壳聚糖纳米粒。

Development of a novel drug delivery system: chitosan nanoparticles entrapped in alginate microparticles.

作者信息

Garrait Ghislain, Beyssac Eric, Subirade Muriel

机构信息

Université d'Auvergne, UFR Pharmacie, Equipe d'Accueil Conception, Ingénierie et Développement de l'Aliment et du Médicament (EA CIDAM) , Clermont-Ferrand F-63001 , France and.

出版信息

J Microencapsul. 2014;31(4):363-72. doi: 10.3109/02652048.2013.858792. Epub 2014 Apr 3.

DOI:10.3109/02652048.2013.858792
PMID:24697173
Abstract

A novel carrier using chitosan nanoparticles entrapped into alginate microparticles is proposed for protecting molecules of interest from degradation in the digestive tract. The effects of polymer concentration, sonication, stirring, pH, and processing conditions on the physical characteristics of the carrier were studied. FITC and RBITC were used to localise the polymers within particles using CLSM. Diffusion of amaranth red (AR) from nanoparticles was quantified during dissolution under gastric and intestinal conditions. Under optimal preparation conditions, the size distribution of nanoparticles loaded with AR was uniform (690 nm) with an encapsulation efficacy of 21.9%. Alginate microparticles (285 µm) containing a homogenous distribution of nanoparticles and polymers were obtained. At gastric pH, the carrier released less than 5% of the loaded AR and, at intestinal pH, the release was rapid and complete. The drug carriers developed shows a promising use as a vehicle suitable to protect molecules of interest after oral administration.

摘要

提出了一种新型载体,它是将壳聚糖纳米颗粒包裹在藻酸盐微粒中,用于保护目标分子在消化道中不被降解。研究了聚合物浓度、超声处理、搅拌、pH值和加工条件对载体物理特性的影响。使用异硫氰酸荧光素(FITC)和四甲基罗丹明异硫氰酸酯(RBITC)通过共聚焦激光扫描显微镜(CLSM)来定位颗粒内的聚合物。在胃和肠道条件下溶解过程中,对苋菜红(AR)从纳米颗粒中的扩散进行了定量分析。在最佳制备条件下,负载AR的纳米颗粒尺寸分布均匀(690纳米),包封率为21.9%。获得了含有均匀分布的纳米颗粒和聚合物的藻酸盐微粒(285微米)。在胃pH值下,载体释放的负载AR不到5%,而在肠道pH值下,释放迅速且完全。所开发的药物载体显示出有望作为一种适合口服给药后保护目标分子的载体。

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