Aerosil固体口腔膜用于缬沙坦的改进和持续递送:分子对接研究

IF 1.6 4区 生物学 Q4 BIOTECHNOLOGY & APPLIED MICROBIOLOGY
Rakesh Swain, Souvik Nandi, Pallavi Bardhan, S. S. Swain, S. Mohapatra, S. Mallick
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引用次数: 0

摘要

为了克服口服生物利用度低和生物半衰期短的问题,提出了改进和持续的缬沙坦口腔给药。以HPMC为基质,采用流延法和溶剂蒸发法,制备了含有胶体二氧化硅的缬沙坦薄膜。缬沙坦和Aerosil可能是通过吸附水和二氧化硅的硅烷醇之间形成氢键而相互作用的。体外药物释放和离体口腔渗透随着Aerosil在膜中的增加而增加。缬沙坦与Aerosil的比例为1:0.02的制剂在模拟生理液(pH 6.8)中的8小时研究中分别表现出80%和70%的持续释放和渗透。分子对接研究显示,Aerosil掺入的缬沙坦口腔膜具有稳定的结构,有利得分为–2.15 kcal mol–1。总之,Aerosil掺入的水凝胶形成口腔膜可用于缬沙坦的改善和持续递送。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Aerosil in Solid-state Buccal Film for Improved and Sustained Delivery of Valsartan: Molecular Docking Studies
To overcome low oral bioavailability and short biological half-life, improved and sustained buccal delivery of valsartan has been proposed. Valsartan film with colloidal silicon dioxide has been prepared using HPMC as mucoadhesive polymer matrix by casting and solvent evaporation method. Valsartan and Aerosil might have been interacted by hydrogen bond formation between adsorbed water and silanol of SiO 2 . In vitro drug release and ex vivo buccal permeation increased with the increase of Aerosil in the film. The formulation of valsartan to Aerosil at 1:0.02 ratio exhibited a sustained type of release and permeation of 80 and 70 %, respectively, in 8 h of study in simulated physiological fluid (pH 6.8). Molecular docking study revealed a stable configuration with favourable score of –2.15 kcal mol –1 of the Aerosil incorporated valsartan buccal film. In conclusion, Aerosil incorporated hydrogel forming buccal film could be used for improved and sustained delivery of valsartan.
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来源期刊
Chemical and Biochemical Engineering Quarterly
Chemical and Biochemical Engineering Quarterly 工程技术-工程:化工
CiteScore
2.70
自引率
6.70%
发文量
23
审稿时长
>12 weeks
期刊介绍: The journal provides an international forum for presentation of original papers, reviews and discussions on the latest developments in chemical and biochemical engineering. The scope of the journal is wide and no limitation except relevance to chemical and biochemical engineering is required. The criteria for the acceptance of papers are originality, quality of work and clarity of style. All papers are subject to reviewing by at least two international experts (blind peer review). The language of the journal is English. Final versions of the manuscripts are subject to metric (SI units and IUPAC recommendations) and English language reviewing. Editor and Editorial board make the final decision about acceptance of a manuscript. Page charges are excluded.
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