Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

Drug Delivery

Tapan Kumar Shaw¹  Amal Kumar Bandyopadhyay¹  Biswajit Mukherjee¹  Murari Mohan Pal¹  Samrat Chakraborty¹  Dipika Mandal¹  Paramita Paul¹  Kazi Asraf Ali²  Goutam Dey³  Mahitosh Mandal³ 

[1] Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India;Dr. B. C. Roy College of Pharmacy and Allied Health Sciences, Dr. Meghnad Saha Sarani, Bidhan Nagar, Durgapur, West Bengal, Indi;School of Medical Science and Technology, Indian Institute of Technology Kharagpur, Kharagpur, West Bengal, India, an;

关键词: Blood–brain barrier;    nanoliposomes of Docetaxel;    glioma;    C6 cells;    brain distribution;   

DOI  :  10.1080/10717544.2016.1253798

来源: Taylor & Francis

【 摘 要 】

Docetaxel (DTX) is found to be very effective against glioma cell in vitro. However, in vivo passage of DTX through BBB is extremely difficult due to the physicochemical and pharmacological characteristics of the drug. No existing formulation is successful in this aspect. Hence, in this study, effort was made to send DTX through blood–brain barrier (BBB) to brain to treat diseases such as solid tumor of brain (glioma) by developing DTX-loaded nanoliposomes. Primarily drug-excipients interaction was evaluated by FTIR spectroscopy. The DTX-loaded nanoliposomes (L-DTX) were prepared by lipid layer hydration technique and characterized physicochemically. In vitro cellular uptake in C6 glioma cells was investigated. FTIR data show that the selected drug and excipients were chemically compatible. The unilamellar vesicle size was less than 50 nm with smooth surface. Drug released slowly from L-DTX in vitro in a sustained manner. The pharmacokinetic data shows more extended action of DTX from L-DTX in experimental rats than the free-drug and Taxotere®. DTX from L-DTX enhanced 100% drug concentration in brain as compared with Taxotere® in 4 h. Thus, nanoliposomes as vehicle may be an encouraging strategy to treat glioma with DTX.

【 授权许可】

CC BY