Department of Pharmacy, Nanomedicine Research Group, Quaid-i-Azam University, Islamabad, Pakistan.
Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan.
Drug Deliv. 2023 Dec;30(1):2251720. doi: 10.1080/10717544.2023.2251720.
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.
在此，我们设计、优化并表征了盐酸二甲双胍转乙氧基脂质体（MTF-TES），并将其纳入壳聚糖凝胶中，开发出盐酸二甲双胍负载转乙氧基脂质体凝胶（MTF-TES 凝胶），以提供持续释放、改善经皮通量和提高 MTF 的抗糖尿病作用。Design Expert®软件（版本 12，Stat-Ease，美国）用于 MTF-TES 的统计优化。具有平均粒径分布（MPSD）为 165.4±2.3nm、Zeta 电位（ZP）为-21.2±1.9mV、多分散指数（PDI）为 0.169±0.033 和 MTF 百分包封效率（%EE）为 89.76±4.12 的配方被认为是优化的。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）评估表面形貌、均匀性和分离情况。结果表明，纳米粒子呈球形和圆形，边界完整。与普通 MTF 溶液（MTFS）相比，在 pH 值为 7.4 时，所制备的 MTF-TES 表现出持续释放，随后释放效果更为明显。与 MTFS 相比，在 pH 值为 7.4 时，MTF-TES 表现出增强的渗透作用。进行了体内抗糖尿病试验，结果表明，与 MTF 凝胶相比，MTF-TES 凝胶具有改善的抗糖尿病潜力。总之，MTF-TES 是一种有前途的抗糖尿病候选药物，可用于经皮药物递送，能够提供持续释放 MTF 和增强的抗糖尿病作用。
