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用于增强替莫唑胺向脑部递送的脂质纳米载体

Lipid Nanocarriers for Enhanced Delivery of Temozolomide to the Brain.

作者信息

Khosa Archana, Krishna Kowthavarapu V, Dubey Sunil Kumar, Saha Ranendra Narayan

机构信息

Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Pilani, India.

Birla Institute of Technology and Science, Pilani, Dubai, UAE.

出版信息

Methods Mol Biol. 2020;2059:285-298. doi: 10.1007/978-1-4939-9798-5_15.

Abstract

Brain disorders, a diverse range of conditions comprising of neurological and psychiatric conditions, are the leading cause of disability, severely affect the quality of life, and in many cases lead to mortality. The prime challenge in treatment of brain disorders is to deliver therapeutics by overcoming the blood-brain barrier (BBB), a unique anatomical and physiological barrier which restricts the passage of a number of molecules, proteins, and cells from the bloodstream. Lipid nanoparticles have emerged as promising drug delivery systems primarily because of biodegradability, low toxicity potential, and the ability to cross physiological barriers especially the BBB even without surface modifications.In this chapter we discuss the preparation and characterization of nanostructured lipid carriers of temozolomide, a chemotherapeutic drug. Evaluation of pharmacokinetics and biodistribution of the nanocarrier system in rats revealed improved delivery of the chemotherapeutic agent to the brain with the potential of lesser side effects.

摘要

脑部疾病是一系列由神经和精神疾病组成的病症,是导致残疾的主要原因,严重影响生活质量,并且在许多情况下会导致死亡。治疗脑部疾病的主要挑战在于通过克服血脑屏障(BBB)来递送治疗药物,血脑屏障是一种独特的解剖学和生理学屏障,它限制了许多分子、蛋白质和细胞从血液中通过。脂质纳米颗粒已成为有前景的药物递送系统,主要是因为其具有生物可降解性、低潜在毒性,并且即使没有表面修饰也能够穿过生理屏障,尤其是血脑屏障。在本章中,我们讨论了化疗药物替莫唑胺的纳米结构脂质载体的制备和表征。对大鼠体内纳米载体系统的药代动力学和生物分布的评估表明,化疗药物向脑部的递送得到改善,且副作用可能较小。

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