The Sojourn of Polymeric Micelles for Effective Brain Drug Delivery System.

IF 3.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Prabhjot Kaur, Ankita Rajput, Dilpreet Singh, Gurdeep Singh, Anshula Mehra, Sarabjit Kaur, Neena Bedi, Saroj Arora
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Abstract

The brain is a delicate organ and targeting neurological diseases with conventional approaches is still a daunting task. This is due to the presence of necessary physiological barriers, mainly the blood-brain barrier, that blocks the entry of dangerous and poisonous substances from the bloodstream, thus helping in maintaining homeostasis. Furthermore, the presence of multidrug resistance transporters which act by prohibiting the entry of drugs across the cell membrane and by channelizing them to the outside environment is another defense mechanism. Despite the advancements in the understanding of disease pathology, only a restricted number of drugs and drug therapies can treat and target neurological diseases. To overcome this shortcoming, the therapeutic approach using amphiphilic block copolymers - using polymeric micelles has gained momentum because of its wide applications like drug targeting, delivery, and imaging. Polymeric micelles are nanocarriers that arise when amphiphilic block copolymers spontaneously assemble in aqueous solutions. The hydrophobic core-hydrophilic shell configuration of these nanoparticles makes it easier to load hydrophobic drugs into the core and as a result, the solubility of these medications is improved. Micelle-based drug delivery carriers can target the brain with reticuloendothelial system uptake and produce a long-circulating effect. PMs can also be combined with targeting ligands that increase their uptake by specific cells and thus decreasing off-target effects. In the present review, we primarily focused on polymeric micelles for brain delivery along with the method of preparation, mechanism of micelle formulation, and the ongoing formulations under clinical trials for brain delivery.

高分子胶束在脑药物传递系统中的应用。
大脑是一个脆弱的器官,用传统方法治疗神经系统疾病仍然是一项艰巨的任务。这是由于存在必要的生理屏障,主要是血脑屏障,它阻止危险和有毒物质从血液中进入,从而有助于维持体内平衡。此外,多药耐药性转运蛋白的存在是另一种防御机制,它通过阻止药物进入细胞膜并将其引导到外部环境来发挥作用。尽管对疾病病理学的理解有所进步,但只有数量有限的药物和药物疗法可以治疗和靶向神经系统疾病。为了克服这一缺点,使用两亲性嵌段共聚物的治疗方法——使用聚合物胶束——由于其在药物靶向、递送和成像等方面的广泛应用而获得了发展。聚合物胶束是两亲性嵌段共聚物在水溶液中自发组装时产生的纳米载体。这些纳米颗粒的疏水核-亲水壳结构使疏水药物更容易装载到核中,因此,这些药物的溶解度得到了提高。基于胶束的药物递送载体可以通过网状内皮系统摄取靶向大脑,并产生长期循环效应。PMs还可以与靶向配体结合,靶向配体增加其被特定细胞的摄取,从而减少脱靶效应。在本综述中,我们主要关注用于脑递送的聚合物胶束,以及胶束制剂的制备方法、机制和正在进行的脑递送临床试验的制剂。
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来源期刊
Current drug delivery
Current drug delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.10
自引率
4.20%
发文量
170
期刊介绍: Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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