Khambhla Ekta, Shah Viral, Baviskar Kalpesh
Department of Pharmaceutics, National Institute of Pharmaceutical, Education and Research-Ahmedabad (NIPER-A), Thaltej, Ahmedabad, Gujarat, India.
Curr Pharm Des. 2016;22(19):2913-22. doi: 10.2174/1381612822666160401145951.
The current epoch has witnessed a lifestyle impregnated with stress, which is a major cause of several neurological disorders. High morbidity and mortality rate due to neurological diseases and disorders have generated a huge social impact. Despite voluminous research, patients suffering from fatal and/or debilitating CNS diseases such as brain tumors, HIV, encephalopathy, Alzheimer's, epilepsy, Parkinson's, migraine and multiple sclerosis outnumbered those suffering from systemic cancer or heart diseases. The brain being a highly sensitive neuronal organ, has evolved with vasculature barriers, which regulates the efflux and influx of substances to CNS. Treatment of CNS diseases/disorders is challenging because of physiologic, metabolic and biochemical obstacles created by these barriers which comprise mainly of BBB and BCFB. The inability of achieving therapeutically active concentration has become the bottleneck level difficulty, hampering the therapeutic efficiency of several promising drug candidates for CNS related disorders. Parallel maturation of an effective CNS drug delivery strategy with CNS drug discovery is the need of the hour. Recently, the focus of the pharmaceutical community has aggravated in the direction of developing novel and more efficient drug delivery systems, giving the potential of more effective and safer CNS therapies. The present review outlines several hurdles in drug delivery to the CNS along with ideal physicochemical properties desired in drug substance/formulation for CNS delivery. The review also focuses on different conventional and novel strategies for drug delivery to the CNS. The article also assesses and emphasizes on possible benefits of biomaterial based formulations for drug delivery to the CNS.
当前时代见证了充满压力的生活方式,而压力是多种神经疾病的主要成因。神经疾病和障碍导致的高发病率和死亡率产生了巨大的社会影响。尽管进行了大量研究,但患有致命性和/或使人衰弱的中枢神经系统疾病(如脑肿瘤、艾滋病、脑病、阿尔茨海默病、癫痫、帕金森病、偏头痛和多发性硬化症)的患者数量超过了患有全身性癌症或心脏病的患者。大脑作为一个高度敏感的神经器官,进化出了血管屏障,该屏障调节物质进出中枢神经系统。由于这些主要由血脑屏障(BBB)和血脑脊液屏障(BCFB)构成的屏障所造成的生理、代谢和生化障碍,中枢神经系统疾病/障碍的治疗具有挑战性。无法达到治疗活性浓度已成为瓶颈级别的难题,阻碍了几种有前景的中枢神经系统相关疾病候选药物的治疗效果。与中枢神经系统药物研发并行发展有效的中枢神经系统药物递送策略是当务之急。最近,制药界的关注点更加集中在开发新型且更高效的药物递送系统上,这为更有效、更安全的中枢神经系统治疗带来了潜力。本综述概述了药物递送至中枢神经系统的几个障碍,以及药物/制剂用于中枢神经系统递送所需的理想物理化学性质。该综述还聚焦于药物递送至中枢神经系统的不同传统和新型策略。本文还评估并强调了基于生物材料的制剂用于药物递送至中枢神经系统可能带来的益处。