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聚合物的对恩扎拉胺固体自纳米乳化药物输送系统的影响和改善生物可用性

Su-Min Lee¹, Jeong-Gyun Lee¹, Tae-Han Yun¹

¹Department of Pharmaceutical Engineering, Gyeongsang National University, 33 Dongjin-ro, Jinju 52725, Republic of Korea.

|April 27, 2024

概括

这项研究开发了一种聚合物增强的固体自纳米乳化药物递送系统 (S-SNEDDS) 用于酶胺 (ENZ). 这种新的配方改进了ENZ ENZ.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
材料科学材料科学材料科学

背景情况:

恩扎胺 (ENZ) 是一种重要的前列腺癌药物,具有不良的溶解性和生物可用性.
以前的液体自纳米乳化药物递送系统 (L-SNEDDS) 面临着粉末配方导致药物结晶和减少溶解的挑战.
需要稳定,无形固体配方来提高ENZ的治疗疗效.

研究的目的:

开发一种稳定的固体自纳米乳化药物递送系统 (S-SNEDDS) 用于使用聚合物作为再结晶抑制剂的恩扎胺 (ENZ).
评估聚合物添加对ENZ无形状态,溶解和生物可用性的影响.
评估S-SNEDDS在改善难以溶解化合物的口服药物输送方面的潜力.

主要方法:

基于S-SNEDDS配方的可溶性测试来选择聚合物.
使用喷雾干燥技术生产S-SNEDDS.
使用X射线衍射 (XRD) 和差分扫描热度计 (DSC) 进行药物结晶性的表征.
在模拟的胃和肠液中溶解速度的评估.
与免费药物相比,口服生物可用性的体内评估.

主要成果:

优化的S-SNEDDS配方成功地结合了聚合物来抑制药物再结晶.
在S-SNEDDS中,XRD和DSC证实了酶胺结晶度的显著降低.
在模拟的胃和肠液中观察到更高的溶解率.
在体内研究表明,因S-SNEDDS配方而增加了因口服酶氨胺的生物可用性.

结论:

固体自纳米乳化药物递送系统 (S-SNEDDS) 添加了聚合物,可以有效地保持恩扎胺在稳定的无形状态.
这种方法显著提高了恩扎胺的溶解率和口服生物可用性.
S-SNEDDS代表了一种有前途的策略,用于开发改善的口服配方,用于溶解不良的药物,如恩扎胺.

关键词:

科利登 VA64 是一个生物可用性生物可用性酵素胺胺的使用方法固体自纳米乳化药物输送系统溶解度溶解度溶解度溶解度

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