达帕格利弗洛辛装载双体凝用于皮肤传递:配方,优化,物理化学表征和体内评估
Omar Awad Alsaidan1, Ameeduzzafar Zafar2, Dibyalochan Mohanty3
1Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, 72341, Al-Jouf, Saudi Arabia.
AAPS PharmSciTech
|March 12, 2026
概括
这项研究开发了一种新型的Dapagliflozin装载的双体凝,用于通过皮肤输送,增强药物透率和治疗2型糖尿病的疗效. 与口服药物相比,新配方显著改善了生物可用性和抗糖尿病活性.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物运输 药物运输 药物运输
- 材料科学 材料科学 材料科学
背景情况:
- 2型糖尿病 (DM) 是一种以高血糖症为特征的代谢障碍.
- 口服达帕格利弗洛辛 (DZ) 面临挑战,因为吸收有限和第一通代谢.
- 通过皮肤传递药物提供了一种替代途径,以克服口服药物的限制.
研究的目的:
- 为了配制和优化Dapagliflozin (DZ) 装载的双体细胞体 (BLS) 凝,用于通过皮肤输送.
- 提高DZ通过皮肤的透和治疗效果.
- 评估优化的DZ-BLS凝配方的物理化学,药理动力学和抗糖尿病性质.
主要方法:
- 使用薄膜水化方法制备了带达帕格利弗洛辛的双体体,并通过盒子-贝恩肯设计 (BBD) 进行了优化.
- 优化的DZ-BLS配方 (DZ-BLS13) 被纳入了酸盐凝 (DZ-BLS13G2).
- 进行了体外,体外和体内研究,包括物理化学表征,皮肤透,药理动力学分析和抗糖尿病活性评估.
主要成果:
- 优化的DZ-BLS13表现出了有利的特征:124.2纳米的囊泡大小,0.389 PDI,-40.9 泽塔潜力和90.76%的捕获效率.
- DZ-BLS13G2凝显示出适当的粘度,可扩散性和皮肤相容的pH值,药物释放持续 (95.17%在24小时内).
- 与常规凝和口服DZ相比,透皮配方的皮肤透率显著提高,生物可用性改善 (1.88倍),血水平延长,抗糖尿病活性增强.
结论:
- 比洛索姆凝是一种新且有效的载体系统,可以通过皮肤传递达帕格利弗洛辛.
- 这种方法提高了药物透,生物可用性和治疗疗效,用于管理2型糖尿病.
- 通过皮肤注射的比洛索姆凝为达帕格利弗洛辛治疗提供了口服的有希望的替代方案.
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