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用不同聚合物为局部应用而制备的含阿西梅他的双体凝配方:Box-Behnken设计用于双体的配方优化和配方体内评估
Demirturk Esra1, Tilbe Çevikelli2, Aylin Balcı Özyurt3
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Çukurova University, Adana, Turkey. demirturkesra@hotmail.com.
BMC chemistry
|February 1, 2026
概括
这项研究开发了acemetacin (ACIN) 双体荷载水凝,用于增强局部输送. 优化的配方显示出有希望的物理化学特性,持续释放,以及良好的生物相容性,用于有效的皮肤应用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 皮肤病学 皮肤病学
背景情况:
- 乙甲 (ACIN) 是一种非类固醇抗炎药物,其水溶性较差,阻碍其局部应用.
- 开发有效的局部配方对于局部抗炎疗法至关重要.
研究的目的:
- 通过创建双细胞体载荷的水凝配方来增强乙甲 (ACIN) 的皮肤传递和治疗潜力.
- 优化双体组合参数,并评估它们被纳入适合用于局部药物递送的水凝基中.
主要方法:
- 用薄膜水合制备了比洛索姆,并通过盒式设计 (BBD) 进行了优化,使用不同的型胆,胆固醇和型胆酸盐.
- 优化的双体体被纳入基甲基纤维素 (HPMC) 和卡博波尔水凝中.
- 评估了物理化学性质,药物释放动力学和细胞相容性 (MTT测定).
主要成果:
- 优化的双体体具有137.3nm的大小,zeta潜力为-30.1mV,PDI为0.384,捕获效率为84.5%.
- 基于HPMC的水凝显示出与皮肤相容的pH值 (~4),并提供长达8小时的持续阿西梅他释放.
- 该配方表现出极好的细胞兼容性,在测试度下细胞活力超过90%.
结论:
- 双体载荷HPMC水凝代表着一种有前途的配方,用于局部输送阿西梅他 (ACIN).
- 开发的配方提供了改进的物理化学特性,持续的药物释放,以及良好的生物相容性.
- 需要进一步的体内和抗炎性研究来验证其治疗潜力.
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