title: Effect of nanoparticulate polybutylcyanoacrylate and methylmethacrylate-sulfopropylmethacrylate on the permeability of zidovudine and lamivudine across the in vitro blood-brain barrier.
abstract: Effect of size of nanoscaled polybutylcyanoacrylate (PBCA) and methylmethacrylate-sulfopropylmethacrylate (MMA-SPM) on the permeability of zidovudine (AZT) and lamivudine (3TC) across the blood-brain barrier (BBB) was investigated. Also, influence of alcohol on the permeability of AZT and 3TC incorporated with the two polymeric nanoparticles (NPs) was examined. The loading efficiency and the permeability of AZT and 3TC decreased with an increase in the particle size of the two carriers. By employing PBCA NPs, the BBB permeability of AZT and that of 3TC became, respectively, 8-20 and 10-18 folds. Application of MMA-SPM NPs leaded to about 100% increase in the BBB permeability of the two drugs. In the presence of 0.5% ethanol, 4-12% enhancement in the BBB permeability of the two drugs was obtained in the current carrier-mediated system.
authors.affiliation: Department of Chemical Engineering, National Chung Cheng University, Chia-Yi, Taiwan 62102, Republic of China. chmyck@ccu.edu.tw
authors.forename: Yung-Chih
authors.initials: YC
authors.lastname: Kuo
authors.forename: Hung-Hao
authors.initials: HH
authors.lastname: Chen
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D001812:Blood-Brain Barrier / Q000187:drug effects* / Q000378:metabolism; D002417:Cattle; D002478:Cells, Cultured; D004337:Drug Carriers; D004659:Enbucrilate / Q000494:pharmacology*; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D000431:Ethanol / Q000494:pharmacology; D019259:Lamivudine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008689:Methacrylates / Q000494:pharmacology*; D053758:Nanoparticles; D010316:Particle Size; D010539:Permeability; D015215:Zidovudine / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D019380:Anti-HIV Agents; D004337:Drug Carriers; D008689:Methacrylates; D019259:Lamivudine; D000431:Ethanol; D015215:Zidovudine; D004659:Enbucrilate