Preparation and characterization of azelnidipine-loaded D-α-tocopheryl polyethylene glycol succinate (TPGS) / solutol micelles

Ali Kathem Ala Allah, Shaimaa Nazar Abd Alhammid
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Abstract

Azelnidipine is a calcium-channel antagonist classified as a “class 2” drug with high permeability and low aqueous solubility. It is used in the treatment of angina pectoris and hypertension without reflex tachycardia. Improvement of the solubility of azelnidipine and increasing drug’s bioavailability can be achieved through the drug encapsulation in solutol / D-α-tocopheryl polyethylene glycol succinate (TPGS) micelles. Six formulas were prepared by direct disso¬lution after using different amounts of solutol and TPGS. TPGS and solutol act as solubilizers, permeation enhancers, and P-glycoprotein inhibitors. The particle size, particle size distribution, zeta potential, and entrapment efficiency were determined. Depending on particle size and entrapment efficiency, formula #6 was selected and subjected to in vitro dilution stability and in vitro release studies. The results obtained showed that formula #6 was the best formula, with a high entrapment efficiency percentage equal to 86.5%±0.58% and a small particle size equal to 21.9±7.75 nm that did not change significantly after dilution up to 100-fold; a fact that reveals the high thermodynamic and kinetic stability of the optimum formula. The formula #6 release profile showed a controlled release of the drug from micelles when compared to plain drug release. Based on these results, polymeric nanomicelles are regarded as a promising delivery system for azelnidipine.
阿折地平负载型 D-α-生育酚聚乙二醇琥珀酸酯 (TPGS) / Solutol 胶束的制备与表征
阿折地平是一种钙通道拮抗剂,属于 "2 类 "药物,具有高渗透性和低水溶性。它用于治疗心绞痛和无反射性心动过速的高血压。通过将药物封装在 Solutol / D-α-tocopheryl polyethylene glycol succinate(TPGS)胶束中,可以改善阿折地平的溶解度并提高药物的生物利用度。在使用不同量的 Solutol 和 TPGS 后,通过直接分解法制备了六种配方。TPGS 和 Solutol 可用作增溶剂、渗透促进剂和 P 糖蛋白抑制剂。粒度、粒度分布、ZETA电位和夹带效率均已测定。根据粒度和夹带效率,选择了 6 号配方,并进行了体外稀释稳定性和体外释放研究。结果表明,6 号配方是最佳配方,其夹带效率高达 86.5%±0.58%,粒径小至 21.9±7.75 nm,稀释 100 倍后无明显变化,这表明最佳配方具有较高的热力学和动力学稳定性。6 号配方的释放曲线显示,与普通药物释放相比,胶束的药物释放得到了控制。基于这些结果,聚合物纳米胶束被认为是一种很有前景的阿折地平给药系统。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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