哌啶超小型单拉美米尔载体的制备与评估

Pub Date : 2024-04-01 DOI:10.46542/pe.2024.242.5257
Anugrah Putra Pharmaheri, Salman Umar, H. Lucida
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引用次数: 0

摘要

背景:胡椒碱是一种生物碱,对黑色素细胞的增殖和密度有刺激作用。因此,它是一种治疗白癜风的潜在药物:用初榨椰子油、大豆卵磷脂和吐温80配制一种含胡椒碱的超小单铵载体(USUC)Emulgel,并评估其理化性质:以 2.3% 的油相、1% 的表面活性剂和 2.3% 的辅助表面活性剂为基本成分,采用自发水相滴定法在 1500 转/分钟的搅拌速度下配制胡椒碱载体 USUC,搅拌时间为 15 分钟。将 USUC 胡椒碱混入 5% 的 carbopol 基质中,制成 Emulgel 制剂:结果:哌啶负载USUC呈球状,Z-平均尺寸为15.0 nm,zeta电位为-39.5 mV,多分散指数为0.312。该乳胶制剂的 pH 值为(6.5 ± 0.1),粘度为(44.800 ± 0.367)cP,具有物理稳定性。胡椒碱从 USUC 胶体中的渗透遵循零阶动力学(y = 0.130x-2.027;R2 = 0.9998),通量值为(3.408 ± 1.110)微克/厘米2/小时,与非 USUC 胡椒碱凝胶的渗透(0.000 ± 0)微克/厘米2/小时有显著差异(p <0.05):含胡椒碱的 USUC 在乳液配方中产生了纳米级的球状小球,这表明与传统的胡椒碱凝胶相比,胡椒碱的渗透量明显不同。
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Formulation and evaluation of piperine-loaded ultra-small unilamellar carrier
Background: Piperine is an alkaloid that has a stimulatory effect on the proliferation and dentricity of melanocytes. Therefore, it is a potential drug for vitiligo. Objectives: To formulate an Emulgel containing piperine-loaded Ultra-Small Unilamellar Carrier (USUC) with virgin coconut oil, soy lecithin and tween 80, and to evaluate the physicochemical properties. Method: Piperine-loaded USUC was formulated using a spontaneous water phase titration method at a stirring speed of 1500 rpm for 15 minutes with a base composition of 2.3% oil phase, 1% surfactant and 2.3% co-surfactant. Emulgel preparations were made by mixing USUC piperine into a 5% carbopol base. Result: Piperine-loaded USUC was obtained in the form of spherical globules with a Z-average size of 15.0 nm, a zeta potential of -39.5 mV and a polydispersion index of 0.312. The emulgel preparation has a pH of (6.5 ± 0.1), and a viscosity (of 44.800 ± 0.367) cP and is physically stable. Permeation of piperine from USUC emulgel follows zero-order kinetics (y = 0.130x-2.027; R2 = 0.9998) with a flux value of (3.408 ± 1.110) µg/cm2/hour, which is significantly different from permeation of non-USUC piperine gel (0.000 ± 0) µg/cm2/hour)(p <0.05). Conclusion: Piperine-loaded USUC in emulgel formulation produced nanosized spherical globules, indicating a significantly different amount of permeated piperine compared to conventional piperine gel.
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