Abstract

Herein we designed, optimized, and characterized the Metformin Hydrochloride Transethosomes (MTF-TES) and incorporate them into Chitosan gel to develop Metformin Hydrochloride loaded Transethosomal gel (MTF-TES gel) that provides a sustained release, improved transdermal flux and improved antidiabetic response of MTF. Design Expert® software (Ver. 12, Stat-Ease, USA) was applied for the statistical optimization of MTF-TES. The formulation with Mean Particle Size Distribution (MPSD) of 165.4 ± 2.3 nm, Zeta Potential (ZP) of −21.2 ± 1.9 mV, Polydispersity Index (PDI) of 0.169 ± 0.033, and MTF percent Entrapment Efficiency (%EE) of 89.76 ± 4.12 was considered to be optimized. To check the chemical incompatibility among the MTF and other formulation components, Fourier Transform Infrared (FTIR) spectroscopy was performed and demonstrated with no chemical interaction. Surface morphology, uniformity, and segregation were evaluated through Transmission Electron Microscopy (TEM). It was revealed that the nanoparticles were spherical and round in form with intact borders. The fabricated MTF-TES has shown sustained release followed by a more pronounced effect in MTF-TES gel as compared to the plain MTF solution (MTFS) at a pH of 7.4. The MTF-TES has shown enhanced permeation followed by MTF-TES gel as compared to the MTFS at a pH of 7.4. In vivo antidiabetic assay was performed and results have shown improved antidiabetic potential of the MTF-TES gel, in contrast to MTF-gel. Conclusively, MTF-TES is a promising anti-diabetic candidate for transdermal drug delivery that can provide sustained MTF release and enhanced antidiabetic effect.

摘要

在此，我们设计、优化和表征了盐酸二甲双胍转座体 (MTF-TES)，并将其合并到壳聚糖凝胶中，开发了负载盐酸二甲双胍的转座体凝胶 (MTF-TES 凝胶)，该凝胶可提供持续释放、改善的透皮通量和改善的抗糖尿病反应。 MTF。Design Expert® 软件（Ver. 12，Stat-Ease，美国）用于 MTF-TES 的统计优化。该配方的平均粒径分布 (MPSD) 为 165.4 ± 2.3 nm，Zeta 电位 (ZP) 为 -21.2 ± 1.9 mV，多分散指数 (PDI) 为 0.169 ± 0.033，MTF 百分比捕获效率 (%EE) 为 89.76 ± 4.12被认为是优化的。为了检查 MTF 和其他配方成分之间的化学不相容性，进行了傅里叶变换红外 (FTIR) 光谱分析，并证明没有化学相互作用。通过透射电子显微镜 (TEM) 评估表面形态、均匀性和偏析。结果表明，纳米粒子呈球形和圆形，边界完整。与 pH 7.4 的普通 MTF 溶液 (MTFS) 相比，制造的 MTF-TES 表现出持续释放，随后在 MTF-TES 凝胶中具有更明显的效果。在 pH 值为 7.4 时，与 MTFS 相比，MTF-TES 凝胶后的 MTF-TES 表现出增强的渗透性。进行了体内抗糖尿病测定，结果显示，与 MTF-gel 相比，MTF-TES 凝胶的抗糖尿病潜力有所提高。总之，MTF-TES 是一种有前途的透皮给药抗糖尿病候选药物，可以提供持续的 MTF 释放并增强抗糖尿病效果。