Kaur Jaskiran, Gulati Monica, Kapoor Bhupinder, Jha Niraj Kumar, Gupta Piyush Kumar, Gupta Gaurav, Chellappan Dinesh Kumar, Devkota Hari Prasad, Prasher Parteek, Ansari Md Salahuddin, Aba Alkhayl Faris F, Arshad Mohammed F, Morris Andrew, Choonara Yahya E, Adams Jon, Dua Kamal, Singh Sachin Kumar
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, Punjab, India.
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, Punjab, India; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW, 2007, Australia.
Chem Biol Interact. 2022 Jul 1;361:109960. doi: 10.1016/j.cbi.2022.109960. Epub 2022 May 6.
In recent years, unique physicochemical properties of amphiphilic block copolymers have been utilized to design the polymeric micelles for brain-specific delivery of drugs, proteins, peptides and genes. Their unique properties such as nano-size, charge-switching ability, stimuli-responsive cargo release, flexible structure, and self-assembly enable them to overcome limitations of conventional dosage forms that include rapid drug release, drug efflux, and poor brain bioavailability, and poor stability. These limitations hinder their therapeutic efficacy in treating brain diseases. Their ease of functionalization and enhanced penetration and retention effect make them suitable nanocarriers for the diagnosis of various brain diseases. In this context, the present manuscript provides an insight into the progress made in the functionalization of micelles such as the incorporation of stimuli-sensitive moieties in copolymers, conjugation of cargo molecules with the core-forming block via responsive smart linkers, and conjugation of active ligands and imaging moieties with the corona forming block for brain targeting and imaging. Further, the review also expounds on the role of polymeric micelles in delivering neurotherapeutic to the brain. Some patents related to polymeric micelles formulated for brain delivery are also enlisted.
近年来，两亲性嵌段共聚物独特的物理化学性质已被用于设计聚合物胶束，用于脑特异性递送药物、蛋白质、肽和基因。它们的独特性质，如纳米尺寸、电荷转换能力、刺激响应性药物释放、灵活的结构和自组装能力，使它们能够克服传统剂型的局限性，包括药物快速释放、药物外排、脑生物利用度差和稳定性差。这些局限性阻碍了它们在治疗脑部疾病中的治疗效果。它们易于功能化以及增强的渗透和滞留效应，使其成为诊断各种脑部疾病的合适纳米载体。在此背景下，本手稿深入探讨了胶束功能化方面取得的进展，例如在共聚物中引入刺激敏感部分、通过响应性智能接头将货物分子与形成核心的嵌段偶联，以及将活性配体和成像部分与形成冠层的嵌段偶联以实现脑靶向和成像。此外，该综述还阐述了聚合物胶束在向脑部递送神经治疗药物中的作用。还列举了一些与用于脑递送的聚合物胶束相关的专利。
