通过耳式配方改善口服生物可用性和hesperidin的大脑分布:统计优化和药物动力学研究
Komaldeep Kaur1, Yogesh A Kulkarni1, Sarika Wairkar2
1Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L.Mehta Road, Vile Parle (W), Mumbai, Maharashtra, 400056, India.
AAPS PharmSciTech
|December 17, 2025
概括
赫斯佩里丁质可显著增强口服生物可用性和脑部传递赫斯佩里丁,一种潜在的阿尔茨海默病治疗化合物. 这种配方克服了hesperidin的溶解性差和吸收性低.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物运输 药物运输 药物运输
- 神经科学是一个神经科学.
背景情况:
- 赫斯佩里丁是一种黄,由于抗氧化剂,抗炎症和抗胺基因作用,它对阿尔茨海默病具有有前途的作用.
- 低水溶性和低口服生物利用率 (<20%) 限制了hesperidin的治疗应用.
- 开发有效的输送系统对于hesperidin的临床潜力至关重要.
研究的目的:
- 为改善口服生物可用性,制定和优化赫斯佩里丁化物 (HC).
- 评估HC的体外释放特征和胃稳定性.
- 为了比较HC与hesperidin脂质体和普通hesperidin的体内药理动力学.
主要方法:
- 使用离子在脂质体中捕获的方法制备了hesperidin带.
- 为了对公式的统计优化,采用了三级因数设计.
- 在pH 7.4和1.2进行了体外药物释放研究.
- 在Wistar大鼠的药理动力学研究中,比较了HC,脂质体和普通hesperidin.
主要成果:
- 优化HC的粒子大小为398.9nm,泽塔电位为-39.1mV,捕获效率为92.2%.
- 实验室释放显示,在pH 7.4时24小时内97%的hesperidin释放,在pH 1.2时只有1%,表明胃的稳定性.
- 在Wistar大鼠中,HC导致血度比脂质体高2.21倍,脑度比脂质体高1.2倍,与普通度相比>25倍.
结论:
- 赫斯佩里丁状细胞代表了一种有前途的口服药物递送系统,用于增强赫斯佩里丁的生物可用性.
- 该HC配方在胃中表现出稳定性,并在肠道中有效释放药物.
- 状细胞提供了一种卓越的策略,可以为潜在的阿尔茨海默氏症治疗提供hesperidin.
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