title: Targeted delivery of tacrine into the brain with polysorbate 80-coated poly(n-butylcyanoacrylate) nanoparticles.
abstract: The purpose of the present study was to investigate the possibility of targeting an anti-Alzheimer's drug tacrine in the brain using polymeric nanoparticles. Rats obtained 1mg/kg of tacrine by intravenous injection in the form of three preparations: (1) a simple solution in phosphate buffered saline, (2) bound to poly(n-butylcyanoacrylate) nanoparticles, and (3) bound to poly(n-butylcyanoacrylate) nanoparticles coated with 1% polysorbate 80 (Tween 80). After 1h of post injection the rats were killed by decapitation and tacrine concentration in brain, liver, lungs, spleen and kidneys was analyzed by HPLC. A higher concentration of drug tacrine was observed in liver, spleen and lungs with the nanoparticles in comparison to the free drug. The accumulation of drug tacrine in the liver and spleen was reduced, when nanoparticles were coated with 1% polysorbate 80. In the brain a significant increase in tacrine concentration was observed in the case of poly(n-butylcyanoacrylate) nanoparticles coated with 1% polysorbate 80 compared to the uncoated nanoparticles and the free drug. In conclusion, the present study demonstrates that the brain concentration of intravenously injected tacrine can be enhanced by binding to poly(n-butylcyanoacrylate) nanoparticles, coated with 1% the nonionic surfactant polysorbate 80.
authors.affiliation: Department of Pharmaceutics, J.S.S. College of Pharmacy, Ootacamund, Tamil Nadu, India. b_wilson@rediffmail.com
authors.forename: Barnabas
authors.initials: B
authors.lastname: Wilson
authors.forename: Malay Kumar
authors.initials: MK
authors.lastname: Samanta
authors.forename: Kumaraswamy
authors.initials: K
authors.lastname: Santhi
authors.forename: Kokilampal Perumal Sampath
authors.initials: KP
authors.lastname: Kumar
authors.forename: Nallupillai
authors.initials: N
authors.lastname: Paramakrishnan
authors.forename: Bhojraj
authors.initials: B
authors.lastname: Suresh
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism; D001921:Brain / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D004337:Drug Carriers; D004355:Drug Stability; D004659:Enbucrilate / Q000737:chemistry*; D007275:Injections, Intravenous; D007700:Kinetics; D053758:Nanoparticles; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013619:Tacrine / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D002800:Cholinesterase Inhibitors; D004337:Drug Carriers; D011136:Polysorbates; D013501:Surface-Active Agents; D013619:Tacrine; D004659:Enbucrilate