Department of Pharmaceutical Science, School of Medical and Allied Science, GD Goenka University, Gurugram, Haryana, India.
Department of Pharmaceutical Science, MD University, Rohtak, Haryana, India.
Recent Adv Drug Deliv Formul. 2024;18(1):50-60. doi: 10.2174/0126673878279693231227081931.
To develop and characterize the topical insulin-loaded organogel formulation for the management of diabetic wounds.
To formulate and evaluate organogel of insulin that can serve as a topical administration for promoting enhanced wound healing in diabetic patients by providing sustained and localized delivery of drug to the wound site.
The insulin organogel formulated by the micro-emulsion method involves mixing the "aqueous and oil phases" at high shear. Physical and chemical properties, as well as an in vitro study with a Franz diffusion chamber, were used to evaluate the prepared organogel.
All formulations proved to be off-white, homogeneous, washable, and had a pH between 6 and 6.5; moreover, they were non-irritating and skin-compatible. Formulations F1-F6 had viscosity ranging from 2058 to 3168 cps, spreadability ranges of 0.35 to 0.52 g*cm/s, and gel transition ranges of 28.33 to 35.33 °C. In formulations F1-F3, the concentration of lecithin was gradually increased, and in formulations F4-F6, the concentration of PF-127 was increased, resulting in a decrease in gel transition temperature, an increase in viscosity, and a gradual change in spreadability. The higher-viscosity formulations were much more stable and had better drug release. All formulations were fitted to a kinetic model belonging to first-order kinetics. However, after examining the parameter evaluation, it was found that the formulations F2 and F6 were better suited to the kinetic model and were consistent with the first-order and Higuchi models in Korsmeyer-Peppas F2 (r2 = 0.9544 and n = 1.0412); F6 (r2 = 0.9019 and n = 1.0822), which was a confirmation of the sustainability of the release system with matrix diffusion and drug delivery mechanisms that were based on the Super-Case II transport.
Further research and clinical trials are needed to validate its efficacy, optimize the formulation, and establish its long-term safety. Topical insulin organogel has the potential to revolutionize diabetic wound management by improving healing outcomes, reducing complications, and raising the standard of living for those who have diabetes.
开发并表征用于治疗糖尿病创面的局部胰岛素载体制剂。
将胰岛素制成凝胶剂，通过向创面提供持续的局部药物输送，为糖尿病患者提供一种局部给药的方式，以促进创面愈合。
采用乳化法制备胰岛素凝胶，将“水相”和“油相”在高剪切下混合。采用物理化学性质和Franz 扩散室的体外研究对所制备的凝胶进行评价。
所有制剂均为乳白色、均匀、可水洗，pH 值在 6 到 6.5 之间；此外，它们无刺激性且与皮肤相容。制剂 F1-F6 的粘度范围为 2058 到 3168 cps，铺展性范围为 0.35 到 0.52 g*cm/s，凝胶转变温度范围为 28.33 到 35.33°C。在制剂 F1-F3 中，逐渐增加卵磷脂的浓度，在制剂 F4-F6 中，增加 PF-127 的浓度，导致凝胶转变温度降低，粘度增加，铺展性逐渐变化。较高粘度的制剂更稳定，药物释放更好。所有制剂均拟合到属于一级动力学的动力学模型。然而，在检查参数评估后发现，制剂 F2 和 F6 更适合动力学模型，并且与第一级和 Higuchi 模型在 Korsmeyer-Peppas F2（r2 = 0.9544 和 n = 1.0412）；F6（r2 = 0.9019 和 n = 1.0822）一致，这证实了以基质扩散和基于 Super-Case II 转运的药物传递机制为基础的释放系统的可持续性。
需要进一步的研究和临床试验来验证其疗效、优化配方并建立其长期安全性。局部胰岛素凝胶有可能通过改善愈合效果、减少并发症和提高糖尿病患者的生活质量来彻底改变糖尿病创面管理。
