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开发Norelgestromin溶解双层微阵列贴片,用于持续释放荷尔蒙避孕药

Lalitkumar K Vora¹, Ismaiel A Tekko¹, Fabiana Volpe Zanutto¹

¹School of Pharmacy, Medical Biology Centre, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK.

|July 27, 2024

概括

溶解微针微阵列贴片 (MAPs) 提供诺瑞尔格斯特,用于潜在的长效避孕. 这些患者友好的MAP显示了长达7天的治疗药物水平,提供了一个有前途的替代性输送系统.

科学领域:

制药科学制药科学
生物材料工程生物材料工程
药物输送系统药物输送系统

背景情况:

微阵列贴片 (MAP) 提供了一种非侵入性的,可自给药的药物输送方法.
在资源有限的环境中,MAP对自我管理的荷尔蒙避孕药特别有希望.

研究的目的:

开发含有诺瑞尔格斯特 (NGMN) 的可溶解双层MAP,用于持续的荷尔蒙避孕.
评估NGMN载MAP的药物释放动力学和体内药理动力学.

主要方法:

制造溶解双层MAP,以优化针的长度来透角层.
使用新生猪皮肤进行ex vivo药物输送评估.
在Sprague Dawley大鼠体内药理动力学研究,将MAP与肌内注射 (IM) 进行比较.

主要成果:

活体研究显示,每MAP的平均输送量为176±60.9μg的NGMN (15.3±5.3%的药物).
在生体内对大鼠进行的研究显示,MAP的Tmax为4小时,Cmax为67.4±20.1 ng/mL,相对于IM注射,相对生物利用率为~10%.
治疗性血水平与MAPs保持在应用后长达7天.

结论:

含有NGMN的溶解双层MAP显示出作为激素避孕药物持续药物递送系统的潜力.
需要进一步开发,以提高药物释放时间和生物可用性,以延长避孕疗效.

关键词:

荷尔蒙避孕药是一种荷尔蒙避孕药.皮肤内输送是指皮肤内输送.微阵列补丁贴片的微阵列补丁微针是一种微针.在Norelgestromin中使用.预防怀孕预防怀孕持续释放的释放物是一种持续释放物.

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