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优化基于离子液体的NLC,用于鼻到脑输送甲化

Namdeo R Jadhav¹, Sonali R Yede², Asha S Jadhav²

¹Krishna Institute of Pharmacy, Krishna Vishwa Vidyapeeth (Deemed to Be University), Karad, Maharashtra, 415539, India. nrjadhav18@rediffmail.com.

AAPS PharmSciTech

|January 8, 2026

概括

研究人员开发了混合纳米结构脂质载体 (NLCs),以增强鼻至脑的甲化物 (TBZ) 输送. 这些新型混合NLC显著改善了大脑中的药物生物可用性,为治疗神经系统疾病提供了一个有希望的策略.

科学领域:

纳米技术和药物输送
神经科学和药理学神经科学和药理学

背景情况:

传统的纳米结构脂质载体 (NLCs) 面临着鼻至大脑药物输送的挑战,包括药物溶解性差,有效载荷能力有限,透性不足.
贝纳化 (TBZ) 是BCS级IV类药物,需要改进的输送系统,以有效治疗神经疾病.

研究的目的:

开发和优化混合NLC,利用生物离子液体,以提高TBZ的可溶性,透性,有效载荷和鼻至脑的生物可用性.
评估TBZ载荷混合NLCs在in-situ凝配方中的潜力,以改善非侵入性脑部输送.

主要方法:

混合NLCs是通过用生物离子液体取代液体脂质来制备的.
使用中央复合设计进行了配方优化.
物理化学表征包括粒子大小,PDI,泽塔潜力和药物加载效率. 在Wistar大鼠中进行了体外,活体药物释放和活体药理学研究.

主要成果:

优化的TBZ混合NLC表现出有利的特征:粒子大小 (149.84 nm),PDI (0.33),泽塔电位 (-38.96 mV) 和高捕获效率 (97.65%).
混合NLC显示,与普通NLC (28.2%) 相比,TBZ药物负载 (34.4%) 显著更高.
在体外和体外释放研究表明,混合NLCs (分别为74.22%和74.73%) 与普通NLCs (分别为66.44%和61.18%) 的TBZ释放增强.
与普通NLCs凝相比,对大鼠注射TBZ载荷的混合NLC凝导致大脑生物可用性增加1.51倍.

结论:

混合NLC代表了与传统NLC相比的成功进步,用于增强TBZ的鼻至脑输送.
开发的混合NLCs配方显著提高了TBZ在大脑中的生物可用性,证明了其作为有效的非侵入性输送策略的潜力.
这种方法对神经疾病和需要直接针对大脑药物治疗的疾病的治疗管理具有前景.

关键词:

在现场凝凝.生物离子液体生物离子液体生物可用性生物可用性混合纳米结构脂质载体混合纳米结构脂质载体从鼻子到大脑的输送.贝纳二化四贝纳二化

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