基于自纳米乳化系统的法莫替丁递送改善口服生物利用度:体外和体内评价

IF 3.6 4区 化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR
Shah Fahad Khan, Muhammad Akhlaq, Jiang Ni, Anam Razzaq, Haroon Iqbal, Zaheer Ullah Khan, Asmat Ullah, Serag Eldin I. Elbehairi, Ali A. Shati, Mohammad Y. Alfaifi, Naveed Ullah Khan, Abid Hussain, Qiufang Gao
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引用次数: 0

摘要

近年来,自纳米乳化给药系统(SNEDDS)作为提高吸收不良药物的生物利用度的一种有前景的策略受到了药学专家的关注。本研究以低生物利用度药物法莫替丁为模型,旨在评价SNEDDS促进药物吸收的潜力。基于鱼油的SNEDDS配方中加入了Tween 80(表面活性剂)和丙二醇(共表面活性剂),并通过Box-Behnken设计进行了优化。这些配方进行了热力学稳定性测试、物理化学表征以及体外和体内评价。SNEDDS具有良好的热力学稳定性和理想的粒径特性。该制剂在初始爆发释放后呈现持续释放模式。ftir光谱证实了FM在sndds中的存在和稳定性。Caco2细胞的细胞摄取研究显示,与对照相比,SNEDDS的摄取显著增加,为提高生物利用度提供了概念证明。离体数据显示SNEDDS在黏液层中完全浸润。体内实验结果表明,SNEDDS具有良好的血液相容性,并明显增强了疏水药物进入体循环的通道,提高了其生物利用度。该制剂显示出体内口服生物利用度的极好提高,证明设计的口服剂型可以成为临床医生口服低溶性药物的有效临床倾向。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Self-Nano Emulsifying System-Based Delivery of Famotidine for Improved Oral Bioavailability: In Vitro and In Vivo Evaluations

Self-Nano Emulsifying System-Based Delivery of Famotidine for Improved Oral Bioavailability: In Vitro and In Vivo Evaluations

Pharmaceutical experts have focused on the Self-Nano Emulsifying Drug Delivery System (SNEDDS) in recent years as a promising strategy to enhance the bioavailability of poorly absorbed drugs. Using famotidine, a drug with low bioavailability—as a model, this study aimed to evaluate the potential of SNEDDS for improving drug absorption. Fish oil-based SNEDDS formulations incorporating Tween 80 (surfactant) and propylene glycol (co-surfactant) were developed using pseudo-ternary phase diagrams and optimized via Box-Behnken design. The formulations underwent thermodynamic stability testing, physicochemical characterization, as well as in vitro and in vivo evaluations. SNEDDS revealed excellent thermodynamic stability and desired particle’s size characteristics. The formulations showed a sustained release pattern after initial burst release. The FTIR-spectrum confirmed the incorporation and stability of FM in SNEDDS. The cell uptake study in Caco2 cells showed significantly higher uptake for SNEDDS as compared to control, providing proof of concept to improve bioavailability. The ex vivo data displayed the thoroughgoing infiltration of SNEDDS in the mucus layers. The in vivo results declared desirable hemocompatibility of SNEDDS and decidedly enhanced passage of hydrophobic drug into the systemic circulation, improving its bioavailability. The formulations showed excellent elevation of in vivo oral bioavailability, proving that the designed oral dosage form can be a potent clinical slant regarding oral delivery of low soluble drugs for clinicians.

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来源期刊
Journal of Cluster Science
Journal of Cluster Science 化学-无机化学与核化学
CiteScore
6.70
自引率
0.00%
发文量
166
审稿时长
3 months
期刊介绍: The journal publishes the following types of papers: (a) original and important research; (b) authoritative comprehensive reviews or short overviews of topics of current interest; (c) brief but urgent communications on new significant research; and (d) commentaries intended to foster the exchange of innovative or provocative ideas, and to encourage dialogue, amongst researchers working in different cluster disciplines.
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