固体脂质纳米颗粒的优化,配方和体外评估,用于通过皮肤输送德尔提亚化
Sandhya Jaiswal1, Ghanshyam Das Gupta2
1Chandigarh College of Pharmacy, department of pharmaceutics, Landran, Mohali, Punjab 140307, India.
Pharmaceutical nanotechnology
|October 14, 2024
概括
这项研究开发了一种使用固体脂质纳米颗粒 (SLN) 的新型透皮贴片,以改善diltiazem化用于心律失常管理的输送. 基于SLN的贴片显示了增强的生物可用性,降低了剂量频率,并改善了患者的遵守性.
科学领域:
- 制药科学 制药科学
- 纳米技术 纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 心律不整需要长期管理,通常使用诸如diltiazem化之类的药物,这些药物具有短半衰期和皮肤透性差等限制.
- 传统的药物输送方法在通过皮肤给药时面临着克服角层屏障的挑战.
- 固体脂质纳米颗粒 (SLN) 提供了一个有前途的颗粒载体系统,以增强通过皮肤的药物透和生物可用性.
研究的目的:
- 开发一种矩阵型的透皮贴片,其中包含在固体脂质纳米颗粒 (SLN) 中封装的diltiazem化物.
- 为了评估发育的透皮贴片的物理化学性质,体外药物释放和体外皮肤透.
主要方法:
- 固体脂质纳米颗粒 (SLN) 用溶剂扩散技术制备,并以形态,颗粒大小和封装效率为特征.
- 通过溶剂蒸发技术制定了一种通过皮肤贴片,其中包括HPMC E50,甘醇和油酸/甘醇混合物.
- 进行了体外药物释放和体外皮肤透研究,以评估diltiazem含化的SLN透皮贴片的性能.
主要成果:
- SLN是球形的,粒子大小为488.1±4.01nm,捕获效率为55.03±1.99%.
- 透皮贴片表现出均的药物含量 (89.37 ± 0.04%),适当的表面pH值 (6.1 ± 0.53),并在24小时内释放了70.7%的药物.
- 活体研究表明,在24小时后,按照希古奇矩阵释放模型,稳定状态流量为6.9μg/cm2/hr,累积药物透量为814.885μg.
结论:
- 开发的 Diltiazem 含化的 SLN 透皮贴片有效地提高了药物的生物可用性.
- 这种新型配方具有降低剂量频率的潜力,并改善患者在治疗心律不整时的遵守性.
- 补丁配方中的油酸和烯糖醇的协同作用有助于增强皮肤透.
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