Abstract Niosomes as drug delivery systems have the ability to decrease drugs' side effects and increase their therapeutic effectiveness. Metformin HCl is an oral antihyperglycemic agent belonging to biguanides. It is the most commonly chosen drug as a startup therapy for patients newly diagnosed with type 2 diabetes. This study aims to encapsulate metformin HCl inside niosomes to be used as a transdermal formulation helping to prolong its antidiabetic effect and investigate its ability to enhance wound healing in diabetic patients. Thin film hydration method was used to prepare metformin HCl niosomes using different proportions of Span 60, Span 40, Tween 80, and cholesterol. All formulations were characterized using transmission electron microscope, zeta potential, and vesicle size. In vitro release studies, stability studies and in vivo evaluation were conducted on selected niosomal formulations. The results of entrapment efficiency ranged from 13% to 32%. Vesicle sizes were determined in nano-range. The in vitro release profile of metformin HCl from niosomes occurred in two consecutive phases. Biological evaluation on diabetic rats revealed that metformin HCl niosomal gel given every 2 days showed a better sustained antidiabetic effect than oral doses given daily. It also showed an improvement in wound healing for diabetic rats given metformin formulations compared to nontreated ones.

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盐酸二甲双胍与伤口愈合：从纳米制剂到药理学评价

摘要 Niosomes 作为给药系统具有降低药物副作用和提高治疗效果的能力。盐酸二甲双胍是属于双胍类的口服降糖药。它是最常选择的药物，作为新诊断为 2 型糖尿病患者的启动疗法。本研究旨在将盐酸二甲双胍封装在 niosomes 内，用作透皮制剂，有助于延长其抗糖尿病作用，并研究其促进糖尿病患者伤口愈合的能力。使用不同比例的 Span 60、Span 40、Tween 80 和胆固醇，采用薄膜水合法制备盐酸二甲双胍 niosome。使用透射电子显微镜、zeta 电位和囊泡大小表征所有制剂。体外释放研究，对选定的 niosomal 制剂进行了稳定性研究和体内评估。截留效率的结果范围从 13% 到 32%。在纳米范围内确定囊泡尺寸。盐酸二甲双胍从 niosomes 的体外释放曲线发生在两个连续的阶段。对糖尿病大鼠的生物学评估显示，每 2 天给药一次盐酸二甲双胍凝胶显示出比每天口服给药更好的持续抗糖尿病效果。它还显示，与未治疗的糖尿病大鼠相比，给予二甲双胍制剂的糖尿病大鼠伤口愈合有所改善。对糖尿病大鼠的生物学评估显示，每 2 天给药一次盐酸二甲双胍凝胶显示出比每天口服给药更好的持续抗糖尿病效果。它还显示，与未治疗的糖尿病大鼠相比，给予二甲双胍制剂的糖尿病大鼠伤口愈合有所改善。对糖尿病大鼠的生物学评估显示，每 2 天给药一次盐酸二甲双胍凝胶显示出比每天口服给药更好的持续抗糖尿病效果。它还显示，与未治疗的糖尿病大鼠相比，给予二甲双胍制剂的糖尿病大鼠伤口愈合有所改善。