Kumar Astik, Sudevan Sachithra Thazhathuveedu, Nair Aathira Sujathan, Singh Ashutosh Kumar, Kumar Sunil, Jose Jobin, Behl Tapan, Mangalathillam Sabitha, Mathew Bijo, Kim Hoon
Department of Pharmaceutics, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682041, India.
Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682041, India.
Brain Sci. 2023 Jan 27;13(2):213. doi: 10.3390/brainsci13020213.
It is a very alarming situation for the globe because 55 million humans are estimated to be affected by Alzheimer's disease (AD) worldwide, and still it is increasing at the rapid speed of 10 million cases per year worldwide. This is an urgent reminder for better research and treatment due to the unavailability of a permanent medication for neurodegenerative disorders like AD. The lack of drugs for neurodegenerative disorder treatment is due to the complexity of the structure of the brain, mainly due to blood-brain barrier, because blood-brain drug molecules must enter the brain compartment. There are several novel and conventional formulation approaches that can be employed for the transportation of drug molecules to the target site in the brain, such as oral, intravenous, gene delivery, surgically implanted intraventricular catheter, nasal and liposomal hydrogels, and repurposing old drugs. A drug's lipophilicity influences metabolic activity in addition to membrane permeability because lipophilic substances have a higher affinity for metabolic enzymes. As a result, the higher a drug's lipophilicity is, the higher its permeability and metabolic clearance. AD is currently incurable, and the medicines available merely cure the symptoms or slow the illness's progression. In the next 20 years, the World Health Organization (WHO) predicts that neurodegenerative illnesses affecting motor function will become the second-leading cause of mortality. The current article provides a brief overview of recent advances in brain drug delivery for AD therapy.
这对全球来说是一个非常令人担忧的情况，因为据估计全球有5500万人受阿尔茨海默病（AD）影响，而且全球仍以每年1000万例的速度快速增长。由于像AD这样的神经退行性疾病没有永久性药物，这是一个对更好的研究和治疗的紧急提醒。神经退行性疾病治疗药物的缺乏是由于大脑结构的复杂性，主要是由于血脑屏障，因为药物分子必须进入脑区。有几种新颖的和传统的制剂方法可用于将药物分子输送到大脑中的靶位点，如口服、静脉注射、基因递送、手术植入脑室内导管、鼻腔和脂质体水凝胶，以及旧药重新利用。药物的亲脂性除了影响膜通透性外，还影响代谢活性，因为亲脂性物质对代谢酶具有更高的亲和力。因此，药物的亲脂性越高，其通透性和代谢清除率就越高。AD目前无法治愈，现有的药物只能缓解症状或减缓疾病进展。世界卫生组织（WHO）预测，在未来20年，影响运动功能的神经退行性疾病将成为第二大死亡原因。本文简要概述了AD治疗中脑药物递送的最新进展。
