Enhancing oral bioavailability of escitalopram by self-nanoemulsifying drug delivery systems (SNEDDS): An in-vivo, in-vitro and in-silico study.

IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Muhammad Junaid Asaad, Abdul Majeed, Syed Nisar Hussain Shah, Ghulam Abbas, Farhan Siddique, Muhammad Hanif, Furqan Muhammad Iqbal, Maryam Bashir
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引用次数: 0

Abstract

This study aimed to develop SNEDDS to address the issue of low water solubility of escitalopram (ETP), which consequently leads to inadequate oral bioavailability. The formulation consisted of Tween 80, geranium oil, and polyethylene glycol 400. An evaluation was conducted to determine the surface charge and particle size of ETP-SNEDDS. The stability and compatibility of excipients were evaluated by TGA, DSC and FTIR. Studies were carried out to examine the dissolution, digestion, permeability, in in-vitro, in-vivo, and ex-vivo settings. ETP-SNEDDS bioavailability was assessed in a group of six albino rats under normal conditions. The synthesized SNEDDS exhibited thermodynamic stability, characterized by a 145nm droplet size with a polydispersity index of 0.120 and a minute emulsification duration. Developed SNEDDS containing ETP in FSSIF had a dissolution rate of 96%. Based on the permeation results, the SNEDDS demonstrated a 4.2-fold and 3.1-fold increase in drug penetration relative to standard powder-ETP drug and a reference tablet, correspondingly. Statistically significant improvements (p<0.05) were reported in in-vitro digestion, dissolution and ex-vivo permeability. SNEDDS exhibited a 5.34-fold increase in Cmax and a 4.71-fold rise in AUC compared to the reference. Based on findings, the formulated SNEDDS have a valuable method for enhancing ETP oral bioavailability.

通过自纳米乳化给药系统(SNEDDS)提高艾司西酞普兰的口服生物利用度:一项体内、体外和计算机研究。
本研究旨在开发SNEDDS来解决艾司西酞普兰(ETP)水溶性低,从而导致口服生物利用度不足的问题。该配方由Tween 80、天竺葵油和聚乙二醇400组成。对ETP-SNEDDS的表面电荷和粒径进行了评价。采用热重分析(TGA)、差热分析(DSC)和红外光谱(FTIR)对辅料的稳定性和配伍性进行了评价。在体外、体内和离体条件下进行了溶出、消化、渗透性的研究。在正常情况下,评估ETP-SNEDDS在6只白化大鼠体内的生物利用度。合成的SNEDDS具有良好的热力学稳定性,其液滴尺寸为145nm,多分散性指数为0.120,乳化时间为1分钟。制备的含ETP的SNEDDS在FSSIF中溶出率为96%。通过透性测试,SNEDDS的透性分别比标准粉剂- etp药物和参比片提高了4.2倍和3.1倍。统计上显著的改善(p
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
1.40
自引率
12.50%
发文量
211
审稿时长
4.5 months
期刊介绍: Pakistan Journal of Pharmaceutical Sciences (PJPS) is a peer reviewed multi-disciplinary pharmaceutical sciences journal. The PJPS had its origin in 1988 from the Faculty of Pharmacy, University of Karachi as a biannual journal, frequency converted as quarterly in 2005, and now PJPS is being published as bi-monthly from January 2013. PJPS covers Biological, Pharmaceutical and Medicinal Research (Drug Delivery, Pharmacy Management, Molecular Biology, Biochemical, Pharmacology, Pharmacokinetics, Phytochemical, Bio-analytical, Therapeutics, Biotechnology and research on nano particles.
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