De Anindita, Venkatesh Nagasamy, Senthil M, Sanapalli Bharat Kumar Reddy, Shanmugham R, Karri Veera Venkata Satyanarayana Reddy
Department of Pharmaceutics, JSS College of Pharmacy, Ootacamund, JSS Academy of Higher Education & Research, Mysuru, Karnataka, India.
Department of Pharmaceutical Analysis, Sree Vidyanikethan College of Pharmacy, Tirupati, Jawaharlal Nehru Technological University Ananthapur, Andhra Pradesh, India.
Nanobiomedicine (Rij). 2018 Oct 11;5:1849543518805355. doi: 10.1177/1849543518805355. eCollection 2018 Jan-Dec.
Drug delivery to the brain is challenging because of the low permeability of blood-brain barrier, and therefore, optimum concentration of chemotherapeutics in the target area specifically for glioblastoma, an aggressive brain tumor, opens a new path of research. To achieve the goal, the oral alkylating agent temozolomide was incorporated into niosomes, and the surface was modified with chlorotoxin, a small 36 amino acid peptide discovered from the venom of scorpion . Active targeting using nanosized particles facilitates an increase in the accumulation of drugs in the cerebri by 3.04-folds. Temozolomide-loaded niosomes were prepared using conventional thin-film hydration method and characterized. Niosomes coated with chlorotoxin were produced with the size of 220 ± 1.45 nm with an entrapment efficiency of 79.09 ± 1.56%. Quantitative tissue distribution studies indicate enhanced permeation of the drug into the brain because of surface modification with less deposition in the highly perfused organs.
由于血脑屏障的低渗透性,将药物输送到大脑具有挑战性,因此,针对侵袭性脑肿瘤胶质母细胞瘤在靶区域实现化疗药物的最佳浓度,开辟了一条新的研究途径。为实现这一目标,将口服烷化剂替莫唑胺包裹于非离子表面活性剂囊泡中,并使用从蝎毒中发现的一种由36个氨基酸组成的小肽氯毒素对其表面进行修饰。利用纳米颗粒进行主动靶向可使药物在大脑中的蓄积量增加3.04倍。采用传统的薄膜水化法制备了载替莫唑胺的非离子表面活性剂囊泡并进行了表征。制备的包裹氯毒素的非离子表面活性剂囊泡大小为220±1.45 nm,包封率为79.09±1.56%。定量组织分布研究表明,由于表面修饰,药物在大脑中的渗透增强,在高灌注器官中的沉积减少。