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使用三甲基壳聚糖包衣胰岛素脂质体研究胰岛素跨肠膜模型的摄取与转运

Uptake and transport of insulin across intestinal membrane model using trimethyl chitosan coated insulin niosomes.

作者信息

Moghassemi Saeid, Parnian Ehsan, Hakamivala Amirhossien, Darzianiazizi Maedeh, Vardanjani Marzieh Mowlavi, Kashanian Susan, Larijani Bagher, Omidfar Kobra

机构信息

Biosensor Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran; Nanobiomaterials Laboratory (NBML), Biomaterials Center of Excellence, Amirkabir University of Technology, Tehran 15914, Iran.

Biosensor Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Mater Sci Eng C Mater Biol Appl. 2015 Jan;46:333-40. doi: 10.1016/j.msec.2014.10.070. Epub 2014 Oct 25.

Abstract

This study reports the development of a highly stable niosomal nanostructure based on Span 60/cholesterol (CH)/N-trimethyl chitosan (TMC) system and its potential application for oral delivery of insulin. Insulin loaded niosomes were prepared by reversed-phase evaporation and TMC coating was performed by incubation of niosomal suspensions with TMC solution. The efficiency of nanoparticulate delivery system in enhancement of insulin permeation was evaluated by Caco-2 cell monolayer as intestinal membrane models. The prepared niosomes were characterized for entrapment efficiency (EE), particle size, zeta potential and stability. The particles were between 100 and 180 nm in diameter, and they were stable for over 60 days at 4 °C. Insulin permeability through Caco-2 cell monolayer was enhanced 4-fold by niosomal nanoparticles, compared with insulin alone. Further work is demanded to optimize this formulation with the object of maximizing its potential to facilitate oral delivery of insulin.

摘要

本研究报道了基于司盘60/胆固醇(CH)/N-三甲基壳聚糖(TMC)体系的高度稳定的非离子型脂质体纳米结构的开发及其在胰岛素口服递送方面的潜在应用。通过反相蒸发制备负载胰岛素的非离子型脂质体,并通过将非离子型脂质体悬浮液与TMC溶液孵育进行TMC包衣。以Caco-2细胞单层作为肠膜模型评估纳米颗粒递送系统增强胰岛素渗透的效率。对制备的非离子型脂质体进行包封率(EE)、粒径、zeta电位和稳定性表征。颗粒直径在100至180nm之间,在4℃下稳定超过60天。与单独的胰岛素相比,非离子型脂质体纳米颗粒使胰岛素透过Caco-2细胞单层的渗透率提高了4倍。需要进一步开展工作来优化该制剂,以最大程度发挥其促进胰岛素口服递送的潜力。

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