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用于鼻腔内给药的胰岛素羧甲基壳聚糖-透明质酸水凝胶体系的物理化学特性表征和初步评价。

Physico-Chemical Characterization and Initial Evaluation of Carboxymethyl Chitosan-Hyaluronan Hydrocolloid Systems with Insulin Intended for Intranasal Administration.

机构信息

Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia Str., 020950 Bucharest, Romania.

Innovative Therapeutic Structures Research and Development Centre (InnoTher), "Carol Davila" University of Medicine and Pharmacy, 020956 Bucharest, Romania.

出版信息

Int J Mol Sci. 2024 Sep 27;25(19):10452. doi: 10.3390/ijms251910452.

Abstract

The nasal route of administration can bypass the blood-brain barrier in order to obtain a higher concentration in the brain, thus offering a feasible alternative route of administration for diseases associated with the central nervous system. The advantages of the intranasal administration and the potential favorable therapeutic effects of intranasally administered insulin led to the formulation of carboxymethyl chitosan (CMC) and sodium hyaluronate (NaHA) hydrocolloidal systems with insulin for nasal administration, targeting nose-to-brain delivery and the initial assessment of these systems. The influence of the formulation variables on the response parameters defined as surface properties, rheology, and in vitro release of insulin were analyzed using experimental design and statistical programs (Modde and Minitab software). The systems recorded good wetting and adhesion capacity, allowing the spread of the hydrocolloidal systems on the nasal mucosa. The samples had a pseudoplastic flow and the rapid release of the insulin was according to our objective. According to the physico-chemical characterization and preliminary assessment, these formulations are appropriate for administration on the nasal mucosa, but further studies are necessary to demonstrate the beneficial therapeutic actions and the safety of using intranasal insulin.

摘要

鼻腔给药途径可以绕过血脑屏障,从而在大脑中获得更高的浓度,因此为与中枢神经系统相关的疾病提供了一种可行的替代给药途径。鼻腔给药的优势以及鼻腔给予胰岛素的潜在有利治疗效果促使人们开发了用于鼻腔给药的羧甲基壳聚糖 (CMC) 和透明质酸钠 (NaHA) 水胶体系统,以实现鼻内递药,并对这些系统进行了初步评估。使用实验设计和统计程序(Modde 和 Minitab 软件)分析了制剂变量对定义为表面性质、流变学和胰岛素体外释放的响应参数的影响。这些系统具有良好的润湿性和粘附性,允许水胶体系统在鼻黏膜上扩散。样品具有假塑性流动,胰岛素的快速释放符合我们的目标。根据理化特性和初步评估,这些制剂适合于鼻腔黏膜给药,但需要进一步研究来证明使用鼻腔内胰岛素的有益治疗作用和安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b7e1/11476560/636da4a1b7d2/ijms-25-10452-g001.jpg

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