Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain

Drug Delivery

Tapash Chakraborty¹  Malay Kumar Das¹  Laboni Mondal²  Biswajit Mukherjee²  Sanchari Bhattacharya²  Lopamudra Dutta²  Mita Chatterjee Debnath³  Raghuvir H. Gaonkar³ 

[1] Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, India;Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India;Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, Kolkata, Indi;

关键词: Nanosize lipid carrier;    blood–brain barrier;    gamma scintigraphy;    pharmacokinetics;    biodistribution;   

DOI  :  10.1080/10717544.2018.1435749

来源: publisher

【 摘 要 】

Delivering highly water soluble drugs across blood–brain barrier (BBB) is a crucial challenge for the formulation scientists. A successful therapeutic intervention by developing a suitable drug delivery system may revolutionize treatment across BBB. Efforts were given here to unravel the capability of a newly developed fatty acid combination (stearic acid:oleic acid:palmitic acid = 8.08:4.13:1) (ML) as fundamental component of nanocarrier to deliver highly water soluble zidovudine (AZT) as a model drug into brain across BBB. A comparison was made with an experimentally developed standard phospholipid-based nanocarrier containing AZT. Both the formulations had nanosize spherical unilamellar vesicular structure with highly negative zeta potential along with sustained drug release profiles. Gamma scintigraphic images showed both the radiolabeled formulations successfully crossed BBB, but longer retention in brain was observed for ML-based formulation (MGF) as compared to soya lecithin (SL)-based drug carrier (SYF). Plasma and brain pharmacokinetic data showed less clearance, prolonged residence time, more bioavailability and sustained release of AZT from MGF in rats compared to those data of the rats treated with SYF/AZT suspension. Thus, ML may be utilized to successfully develop drug nanocarrier to deliver drug into brain across BBB, in a sustained manner for a prolong period of time and may provide an effective therapeutic strategy for many diseases of brain. Further, many anti-HIV drugs cannot cross BBB sufficiently. Hence, the developed formulation may be a suitable option to carry those drugs into brain for better therapeutic management of HIV.

【 授权许可】

CC BY