Department of Pharmaceutics, SCES's Indira College of Pharmacy, New Pune Mumbai Highway, Tathawade, Pune, Maharashtra, 411033, India.
C. U. Shah College of Pharmacy, SNDT Women's University, Santacruz (W), Mumbai, Maharashtra, 400 049, India.
AAPS PharmSciTech. 2021 Apr 28;22(4):145. doi: 10.1208/s12249-021-01999-8.
Incorporation of permeation enhancers is one of the most widely employed approaches for delivering drugs across biological membranes. Permeation enhancers aid in delivering drugs across various physiological barriers such as brain capillary endothelium, stratum corneum, corneal epithelium, and mucosal membranes that pose resistance to the entry of a majority of drugs. Borneol is a natural, plant-derived, lipophilic, volatile, bicyclic monoterpenoid belonging to the class of camphene. It has been used under the names "Bing Pian" or "Long Nao" in Traditional Chinese Medicine for more than 1000 years. Borneol has been incorporated predominantly as an adjuvant in the traditional Chinese formulations of centrally acting drugs to improve drug delivery to the brain. This background knowledge and anecdotal evidence have led to extensive research in establishing borneol as a permeation enhancer across the blood-brain barrier. Alteration in cell membrane lipid structures and modulation of multiple ATP binding cassette transporters as well as tight junction proteins are the major contributing factors to blood-brain barrier opening functions of borneol. Owing to these mechanisms of altering membrane properties, borneol has also shown promising potential to improve drug delivery across other physiological barriers as well. The current review focuses on the role of borneol as a permeation enhancer across the blood-brain barrier, mucosal barriers including nasal and gastrointestinal linings, transdermal, transcorneal, and blood optic nerve barrier.
将渗透增强剂纳入其中是将药物递送至生物膜的最广泛应用的方法之一。渗透增强剂有助于将药物递送至各种生理屏障，如脑毛细血管内皮、角质层、角膜上皮和黏膜，这些屏障对大多数药物的进入构成阻力。龙脑是一种天然的、植物来源的亲脂性、挥发性、双环单萜，属于莰烯类。在中国传统医学中，它已经以“冰片”或“龙脑”的名称使用了 1000 多年。龙脑主要作为中枢作用药物的传统中药制剂中的辅助剂使用，以改善药物向大脑的递送。这一背景知识和传闻证据导致了广泛的研究，以确立龙脑作为血脑屏障渗透增强剂的作用。细胞膜脂质结构的改变和多种 ATP 结合盒转运蛋白以及紧密连接蛋白的调节是龙脑开放血脑屏障功能的主要因素。由于这些改变膜性质的机制，龙脑也显示出在改善其他生理屏障的药物递送方面有很大的潜力。本综述重点介绍了龙脑作为血脑屏障、黏膜屏障（包括鼻和胃肠道衬里）、透皮、透角膜和血视神经屏障的渗透增强剂的作用。
