美沙拉胺负载胡芦巴胶装饰果胶微球结肠给药的发展:离体和体外表征。

IF 1 Q4 PHARMACOLOGY & PHARMACY
Pruthvi P Khamkar, Kalpeshkumar S Wagh, Sopan N Nangare, Sachin S Mali, Gaurav S Patil
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引用次数: 0

摘要

美沙拉明(MES)是治疗包括炎症性肠病(IBD)在内的各种结肠疾病的首选治疗剂。然而,MES的传统口服剂型面临重大限制,这降低了它们在管理这些疾病方面的有效性。为了克服这些挑战,先进的MES剂型至关重要。葫芦巴胶(FG)是一种天然多糖,具有无毒、易于合成、生物降解和生物相容性等优点,是开发新型给药系统的关键成分。钙离子交联mes - fg修饰果胶微球(FG@MES/PM)成功设计用于结肠特异性药物递送。该微球具有良好的理化性能,粒径为586 nm,多分散指数为0.348,包封效率为85.20±1.02%,药物含量为98.52±0.96%。体外黏附试验显示出强大的黏附特性,突出了FG@MES/PM有效粘附结肠粘膜的潜力。体外释药研究表明,该药物在24 h内的释药率为99.02±1.80%。释放动力学分析证实FG@MES/PM符合Higuchi矩阵模型(R²= 0.9867),为扩散控制释药。药物释放机制为异常(非菲克式)转运,释放指数(n)为0.563。总体而言,FG@MES/PM显示出有希望的结肠特异性药物递送潜力,提供持续释放和增强粘膜粘附。这项研究强调了FG在开发针对结肠的先进药物输送系统中的实用性。未来的研究应探索FG和类似天然多糖在设计高效、生物相容性强的结肠靶向制剂方面的更广泛应用,以改善IBD及相关疾病的治疗效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of mesalamine loaded-fenugreek gum decorated pectin microspheres for colonic drug delivery: Ex-vivo and in-vitro characterizations.

Mesalamine (MES) is a preferred therapeutic agent for managing various colon disorders, including inflammatory bowel diseases (IBD). However, conventional oral dosage forms of MES face significant limitations, which reduce their effectiveness in managing these conditions. To overcome these challenges, advanced dosage forms of MES are essential. Fenugreek gum (FG), a natural polysaccharide with non-toxicity, ease of synthesis, biodegradability, and biocompatibility, was selected as a key component for developing a novel delivery system. Calcium ion crosslinked MES-incorporated FG-decorated pectin microspheres (FG@MES/PM) were successfully designed for colon-specific drug delivery using an ionotropic gelation technique. The microspheres exhibited favorable physicochemical characteristics, including a particle size of 586nm, a polydispersity index of 0.348, an entrapment efficiency of 85.20±1.02%, and a drug content of 98.52±0.96%. Ex vivo mucoadhesion tests demonstrated strong mucoadhesive properties, highlighting the potential of FG@MES/PM to adhere effectively to the colonic mucosa. In vitro drug release studies showed a modified release profile, with 99.02±1.80% MES released over 24h. Release kinetics analysis confirmed that FG@MES/PM followed the Higuchi matrix model (R2=0.9867), indicating diffusion-controlled release. The drug release mechanism was characterized as anomalous (non-Fickian) transport, with a release exponent (n) of 0.563. Overall, FG@MES/PM demonstrated promising potential for colon-specific drug delivery, offering sustained release and enhanced mucoadhesion. This study underscores the utility of FG for developing advanced drug delivery systems targeting the colon. Future research should explore the broader application of FG and similar natural polysaccharides in designing efficient and biocompatible colon-targeted formulations to improve therapeutic outcomes for IBD and related conditions.

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来源期刊
Annales pharmaceutiques francaises
Annales pharmaceutiques francaises PHARMACOLOGY & PHARMACY-
CiteScore
1.70
自引率
7.70%
发文量
98
期刊介绍: This journal proposes a scientific information validated and indexed to be informed about the last research works in all the domains interesting the pharmacy. The original works, general reviews, the focusing, the brief notes, subjected by the best academics and the professionals, propose a synthetic approach of the last progress accomplished in the concerned sectors. The thematic Sessions and the – life of the Academy – resume the communications which, presented in front of the national Academy of pharmacy, are in the heart of the current events.
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