Formulation and Assessment of an Optimized Glimepiride Transdermal Therapeutic System Using 32 Full Factorial Design Approach.

Q2 Pharmacology, Toxicology and Pharmaceutics

Pharmaceutical nanotechnology Pub Date : 2024-12-10 DOI:10.2174/0122117385348069241017070659

Audumbar Mali, Sunayana Mali

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引用次数: 0

Abstract

Background: Currently, a large number of populations are suffering from diabetes mellitus, which significantly increases the burden on public health. Glimepiride is an antidiabetic drug with a shorter half-life (approximately 5 hours), low bioavailability, and first-pass metabolism. Due to these limitations, it is required to maintain a uniform therapeutic level, and it has been chosen as a transdermal drug delivery approach.

Objectives: The main objective of this investigation was to evaluate glimepiride-loaded transdermal patches on the skin to treat diabetes mellitus. To overcome the issue of oral glimepiride and provide a localized effect, a transdermal drug delivery approach was developed.

Methods: The glimepiride transdermal drug delivery approach was developed by using the solvent evaporation method. To examine the impact of altering amounts of polyvinyl alcohol (X1) and polyvinyl pyrrolidone (X2) on tensile strength, % of glimepiride released in 12 hours (Q12), and % of glimepiride released in 24 hours (Q24), as reliant on variables, a 32 complete factorial design was employed. For dependent variables, regression estimation and estimation of variance were employed. In-vitro release statistics were fixed to different models for various glimepiride release kinetics. In-vitro glimepiride release was tested using the best formulation.

Results: The formulation F4 with 1300.00 milligrams of polyvinyl alcohol and 600.00 milligrams of polyvinyl pyrrolidone demonstrated a release of 96.17% for up to 24 hours and zero order release kinetics consisting of r2=0.987, which was the best batch. The optimized formulation F4 showed a controlled release of glimepiride and better permeation and deposition properties.

Conclusion: The findings of this research work demonstrated the potential of the 32 full factorial mathematical models created to anticipate formulations with additional desirable release and permeability qualities for the treatment of diabetes mellitus.

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采用32全因子设计方法优化格列美脲透皮治疗系统的配方和评价。

背景：目前，大量人群患有糖尿病，这大大增加了公共卫生负担。格列美脲是一种降糖药，半衰期短（约5小时），生物利用度低，首过代谢。由于这些限制，它需要保持一个统一的治疗水平，并已被选择作为透皮给药方法。目的：本研究的主要目的是评估格列美脲皮肤透皮贴片对糖尿病的治疗效果。为了克服口服格列美脲的问题并提供局部效果，研究人员开发了一种经皮给药方法。方法：采用溶剂蒸发法建立格列美脲经皮给药途径。为了研究改变聚乙烯醇（X1）和聚乙烯醇吡咯烷酮（X2）的量对抗拉强度、格列美脲在12小时内释放的百分比（Q12）和格列美脲在24小时内释放的百分比（Q24）的影响，采用了32全因子设计。因变量采用回归估计和方差估计。将体外释放统计数据固定在不同模型上，用于各种格列美脲释放动力学。采用最佳配方测试格列美脲体外释放度。结果：以1300.00 mg聚乙烯醇和600.00 mg聚乙烯醇吡罗烷酮为最佳配方，其24 h的释放度为96.17%，零级释放动力学r2=0.987。优化后的配方F4具有控释格列美脲和较好的渗透沉积性能。结论：本研究工作的发现证明了32个全因子数学模型的潜力，这些模型可以预测治疗糖尿病的处方具有额外的理想释放和通透性。

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

Pharmaceutical nanotechnology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

4.20

自引率

0.00%

发文量

期刊介绍： Pharmaceutical Nanotechnology publishes original manuscripts, full-length/mini reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.