开发非索非那定自微乳化给药系统：改善肠道渗透性的有效方法。

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2024-01-01 Epub Date: 2024-06-28 DOI:10.1080/20415990.2024.2363635

Ziba Islambulchilar, Ashkan Barfar, Shahla Mirzaeei

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引用次数: 0

摘要

目的：本研究旨在制备和评估非索非那定自微乳化给药系统（SMEDDS）制剂，并采用原位单通道肠道灌注（SPIP）技术测定和比较其肠道渗透性。研究方法制备并优化了负载非索非那定的 SMEDDS。对液滴大小、多分散指数、ZETA电位、药物释放和肠道渗透性进行了评估。结果显示优化配方由 15%的油、80% 的表面活性剂和 5% 的共溶剂组成。优化配方的液滴大小和载药量分别为 13.77 纳米和 60 毫克/克，释放了 90% 的药物成分。与游离非索非那定相比，SMEDDS 中非索非那定的肠道渗透性提高了三倍。结论我们的研究结果表明，SMEDDS 可以提高非索非那定的溶出率和肠道渗透性，是一种很有前途的口服给药工具。

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Development of fexofenadine self-microemulsifying delivery systems: an efficient way to improve intestinal permeability.

Aim: The present study aimed to prepare and evaluate fexofenadine self-microemulsifying drug-delivery systems (SMEDDS) formulation and to determine and compare its intestinal permeability using in situ single-pass intestinal perfusion (SPIP) technique.Methods: Fexofenadine-loaded SMEDDS were prepared and optimized. Droplet size, polydispersity index, zeta potential, drug release and intestinal permeability were evaluated.Results: Optimized formulation consisted of 15% oil, 80% surfactant and 5% cosolvent. Droplet size and drug loading of optimized formulation was 13.77 nm and 60 mg/g and it has released 90% of its drug content. Intestinal permeability of fexofenadine was threefold enhanced in SMEDDS compared with free fexofenadine.Conclusion: The results of our study revealed that SMEDDS could be a promising tool for oral delivery of fexofenadine with enhanced dissolution rate and intestinal permeability.

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.