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从脂质纳米乳液中延长释放通过修改药物的脂友性

Nina Baumann¹, Janosch Baumgarten², Conrad Kunick²

¹Technische Universität Braunschweig, Institut für Pharmazeutische Technologie und Biopharmazie, Mendelssohnstr. 1, 38106 Braunschweig, Germany; Technische Universität Braunschweig, Zentrum für Pharmaverfahrenstechnik - PVZ, Franz-Liszt-Str. 35a, 38106 Braunschweig, Germany.

Journal of controlled release : official journal of the Controlled Release Society

|August 16, 2024

概括

药物脂性显著影响从脂质纳米乳液释放. 通过ClogD/P值表示的较高的脂友性,与药物转移到受体介质的速度较慢相关,有助于有针对性的输送.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
物理化学物理化学

背景情况:

脂质纳米乳液有望溶解脂性药物,并使向输送成为可能.
有效的药物向要求药物保持封装,直到达到作用部位.
药物释放动力学主要由药物的脂性而不是配方来决定.

研究的目的:

系统地研究药物脂性对从脂纳米乳液转移到生理接受介质的药物转移的影响.
探索药物脂友性 (ClogD/P) 和药物释放率之间的关系.
评估logP计算和逆相HPLC对药物释放动态的预测能力.

主要方法:

药物脂友性的系统性调查,使用5-phenylanthranilic 酸和模型药物 (orlistat,lumefantrine,胆固醇乙酸) 的前体药物.
使用差分扫描热度计 (DSC) 量化药物转移,通过监测超冷的三氨酸纳米滴的初始结晶温度.
在同位素条件下使用逆相高性能液体染色学 (HPLC) 估计药物脂性.

主要成果:

药物释放率随着药物脂友性 (ClogD/P值) 的增加而下降.
结果通常与HPLC保留时间的脂性估计相一致,除了胆固醇酸盐.
脂质纳米乳液的药物载荷能力增加,对于具有较低点的脂性前药物.

结论:

药物脂性是从脂质纳米乳液中释放药物的关键决定因素.
逻辑P计算和逆相HPLC可以提供药物释放动态的近似预测.
量身定制前药的脂友性和点可以增强药物加载和控制释放以实现有针对性的输送.

关键词:

脂质纳米乳液是一种纳米乳液.脂质纳米颗粒的使用方法脂友性前药物脂友性前药物预测药物释放的情况.持续的药物释放持续的药物释放的 logPP 记录.

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