通过聚合物基口腔注射提高efavirenz生物可用性:优化和描述纳米水晶装载溶解微针输送系统
Khairiyah Khairiyah1, Muh Bisfain Asaf1, Nur Afni Annisa Achmad1
1Department of Pharmaceutical Science and Technology, Faculty of Pharmacy, Hasanuddin University, Makassar, 90245, Indonesia.
The AAPS journal
|March 15, 2025
概括
这项研究开发了通过溶解微针传递的Efavirenz纳米晶体,以改善艾滋病毒/艾滋病治疗. 与口服伊法维伦兹相比,口服服剂增强了生物可用性和药物释放.
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:
- 伊法维伦兹 (EFV) 是艾滋病毒/艾滋病的关键抗逆转录病毒药物,但副作用限制了其使用.
- 嘴口服绕过肠道降解和第一通代谢,提供更好的药物输送.
- 开发新的输送系统对于提高EFV的有效性和患者的遵从性至关重要.
研究的目的:
- 用Pluronic® F-127稳定了Efavirenz纳米晶体 (EFV-NC) 的设计和特征.
- 为了将EFV-NC制成溶解微针 (EFV-NC-DMN) 用于口腔输送.
- 评估EFV-NC-DMN在艾滋病毒/艾滋病管理中的体外和体内性能.
主要方法:
- 分子对接以评估EFV-聚合物相互作用.
- 纳米晶体的制备和表征 (粒子大小,PDI,泽塔潜力).
- 溶解微针的配方和机械性能和药物释放动力学的评估.
- 实体外和体内药理动力学研究以确定生物利用性.
主要成果:
- 普鲁罗尼克®F-127对EFV显示出强烈的结合亲和力.
- EFV-NC表现出最佳的粒子大小,PDI和稳定性.
- EFV-NC-DMN证明了受控释放 (希古奇模型) 和增强的溶解性.
- 与口服EFV相比,体内研究显示EFV-NC-DMN的相对生物利用率为137.40%.
结论:
- EFV-NC-DMN是一种有前途的口腔输送系统,用于增强艾滋病毒/艾滋病治疗.
- 这种新型配方提高了EFV的生物可用性,并延长了药物释放时间.
- 通过微针进行口腔输送,为EFV提供了比传统口服更优质的替代方案.
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