Targeted delivery of tacrine into the brain with polysorbate 80-coated poly(n-butylcyanoacrylate) nanoparticles.
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.
Wilson
Barnabas
B
Department of Pharmaceutics, J.S.S. College of Pharmacy, Ootacamund, Tamil Nadu, India. b_wilson@rediffmail.com
Samanta
Malay Kumar
MK
Santhi
Kumaraswamy
K
Kumar
Kokilampal Perumal Sampath
KP
Paramakrishnan
Nallupillai
N
Suresh
Bhojraj
B
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
D002800:Cholinesterase Inhibitors; D004337:Drug Carriers; D011136:Polysorbates; D013501:Surface-Active Agents; D013619:Tacrine; D004659:Enbucrilate