使用热可逆立方体配方增强大脑生物可用性
Harshvardhan Jain1, Bala Prabhakar1, Pravin K Shende1
1Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM'S NMIMS, V. L. Mehta Road, Vile Parle (W), Mumbai 400056, India.
Molecular pharmaceutics
|March 28, 2024
概括
这项研究开发了一种含有fluoxetine的cubosomal in situ凝,用于鼻内输送,通过绕过血脑屏障 (BBB) 增强大脑的生物可用性. 这种新型配方在体内表现出改善了药物释放和药物动力学特征.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 神经科学是一个神经科学.
背景情况:
- 血脑屏障 (BBB) 构成了向大脑输送治疗药物 (如素) 的重大挑战.
- 鼻内药物输送提供了一种潜在的非侵入性途径,可以绕过BBB并准中枢神经系统.
- 立方体在位凝是先进的配方,旨在持续释放药物并增强透.
研究的目的:
- 开发和表征内含素载入的立体体体 in situ 凝,以改善对脑的准.
- 评估开发的配方的体外,体外和体内性能.
- 评估该系统在提高fluoxetine生物可用性和疗效方面的潜力.
主要方法:
- 用同质化和冷方法制备了含素的立方体体.
- 在现场凝配方被开发,结合了充满素的立方体体.
- 进行了体外和体外药物释放研究.
- 在体内生物分布和药理动力学研究在雄性Wistar大鼠中通过鼻腔注射进行.
主要成果:
- 含有fluoxetine的立方体体表现出高的封装效率 (82.60 ± 1.25%).
- 鼻内立方体in situ凝显示持续的体外释放 (93.22 ± 2.47%) 和体外释放 (96.31 ± 2.88%超过24小时).
- 在体内研究表明,与药物溶液相比,生物可用性增加了2.83倍,药物动力学参数增强 (AUC,Cmax,Tmax,t1/2).
结论:
- 鼻腔内含素的立体体体 in situ 凝是有效的脑药物递送的有希望的载体.
- 粘粘性和持续释放性质可以增强药物的保留和通过鼻子粘膜的透.
- 这种配方提供了一种可行的策略,以改善向大脑的治疗结果.
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