使用响应表面方法开发和优化达帕格利弗洛辛口服纳米双体:体外评估,体内评估
Ananda Kumar Chettupalli1, Nihar Ranjan Kar2, V T Iswariya3
1Department of Pharmaceutical Siences, School of Pharmacy, Galgotias University, Greater Noida, Uttar Pradesh 203201, India.
这项研究开发了Dapagliflozin载荷双体细胞 (Dapa-BLs) 以改善2型糖尿病治疗. 优化的Dapa-BLs在糖尿病大鼠中显示出增强的口服治疗疗效和生物可用性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 2型糖尿病的管理需要控制高血糖和预防葡萄糖毒性.
- 像达帕格利弗洛辛这样的药物的口服管理在生物可用性和有效性方面面临挑战.
研究的目的:
- 制定和优化Dapagliflozin载荷双体体 (Dapa-BLs) 以提高2型糖尿病的口服治疗疗效.
- 评估优化Dapa-BLs的物理化学特性,体外释放,体外透,药理动力学和体内抗糖尿病活性.
主要方法:
- 用薄膜水化来制定比洛索姆,并通过Box Behnken设计,变化的胆汁盐度,边缘激活剂和表面活性剂进行优化.
- 特性包括粒子大小,多分散性指数,泽塔潜力,捕获效率,FTIR,DSC和SEM.
- 评估了体外药物释放,体外皮肤透和体内糖尿病大鼠的药理动力学.
主要成果:
- 优化的Dapa-BLs具有155.36nm的粒子大小,86.37%的捕获效率和球形形态.
- 与达帕格利弗洛辛溶液相比,观察到增强的体外药物释放 (75.31%) 和体外透 (4.49倍更高的流量).
- 在体内研究显示AUC0-t高3.41倍,抗糖尿病活性和生物化学参数显著改善.
结论:
- 带有达帕格利弗洛辛的双体体构成一种有效的口服输送系统,用于2型糖尿病.
- 比洛索姆配方显著提高了Dapagliflozin的治疗疗效和生物可用性.
- 这种方法有望改善糖尿病患者高血糖症的管理.
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