Song Weitong, Bai Lu, Xu Pingxiang, Zhao Yuming, Zhou Xuelin, Xiong Jie, Li Xiaorong, Xue Ming
Department of Pharmacology, School of Basic Medical Sciences, Capital Medical University, Beijing 100069, China.
Beijing Laboratory for Biomedical Detection Technology and Instrument, Capital Medical University, Beijing 100069, China.
Pharmaceutics. 2024 Jul 24;16(8):975. doi: 10.3390/pharmaceutics16080975.
Isoliquiritigenin (ISL) has excellent neuroprotective effects. However, its limitations, including poor solubility, low bioavailability, and low accumulation in the brain, restrict its clinical promotion. In this study, a novel type of ISL-loaded liposome (ISL-LP) modified with the brain-targeting polypeptide angiopep-2 was prepared to improve these properties. The zeta potential, morphology, particle size, encapsulation efficiency, drug loading, and in vitro release of ISL-LP were evaluated. The pharmacokinetics and tissue distribution of ISL and ISL-LP were also investigated. The results demonstrated that ISL-LP had an average particle size of 89.36 ± 5.04 nm, a polymer dispersity index of 0.17 ± 0.03, a zeta potential of -20.27 ± 2.18 mV, and an encapsulation efficiency of 75.04 ± 3.28%. The in vitro release experiments indicate that ISL-LP is a desirable sustained-release system. After intravenous administration, LPC-LP prolonged the circulation time of ISL in vivo and enhanced its relative brain uptake. In conclusion, ISL-LP could serve as a promising brain-targeting system for the treatment and prevention of central nervous system (CNS) disorders.
异甘草素（ISL）具有出色的神经保护作用。然而，其局限性，包括溶解度差、生物利用度低以及在脑中的蓄积量低，限制了其临床推广。在本研究中，制备了一种用脑靶向多肽血管活性肠肽-2修饰的新型载异甘草素脂质体（ISL-LP），以改善这些特性。评估了ISL-LP的ζ电位、形态、粒径、包封率、载药量和体外释放情况。还研究了ISL和ISL-LP的药代动力学和组织分布。结果表明，ISL-LP的平均粒径为89.36±5.04nm，多分散指数为0.17±0.03，ζ电位为-20.27±2.18mV，包封率为75.04±3.28%。体外释放实验表明，ISL-LP是一种理想的缓释系统。静脉给药后，LPC-LP延长了ISL在体内的循环时间并增强了其相对脑摄取。总之，ISL-LP可作为一种有前景的脑靶向系统，用于治疗和预防中枢神经系统（CNS）疾病。
