Blood Compatible Nanostructured Lipid Carriers for the Enhanced Delivery of Azidothymidine to Brain

Non nucleoside anti retroviral drug exhibit low brain permeability. As a result, unchallenged HIV viral replication can lead to HIV-encephalitis and antiretroviral drug resistance. The objective of this study was to develop and evaluate nano lipid carriers for enhanced brain delivery of the potent and frequently used HIV non nucleoside reversetrascriptase, azidothymidine using a well characterized human brain cell line (C6) representative of the blood-brain barrier. Nano lipid carriers (NLCs) were prepared by solvent diffusion method followed by ultrasonication and analyzed for azidothymidine encapsulation efficiency, particle size, morphology, zeta potential and drug release. Cell viability experiments demonstrate that NLCs exhibit no toxicity in C6 cells at a concentration corresponding to 100 g/100 L of azidothymidine. Spherical NLCs with an average particle size of 170–500 nm were formulated. Delivery of azidothymidine by NLCs led to a significantly higher accumulation by the brain cells. These data suggest that NLCs could be a promising drug delivery system to enhance brain uptake of azidothymidine and potentially other non nucleotide class of anti retroviral drugs.