Significant delivery of tacrine into the brain using magnetic chitosan microparticles for treating Alzheimer's disease.
Alzheimer's disease (AD) is a progressive degenerative disorder of the brain characterized by a slow, progressive decline in cognitive function and behavior. As the disease advances, persons have a tough time with daily tasks like using the phone, cooking, handling money or driving the car. AD affects 15 million people worldwide and it has been estimated that AD affects 4.5 million Americans. Tacrine is a reversible cholinesterase inhibitor used for treating mild to moderate AD. In the present study, an attempt was made to target the anti-Alzheimer's drug tacrine in the brain by using magnetic chitosan microparticles. The magnetic chitosan microparticles were prepared by emulsion cross-linking. The formulated microparticles were characterized for process yield, drug loading capacity, particle size, in vitro release, release kinetics and magnetite content. The particle size was analyzed by scanning electron microscope. The magnetite content of the microparticles was determined by atomic absorption spectroscopy. For animal testing, the microparticles were injected intravenously after keeping a suitable magnet at the target region. The concentrations of tacrine at the target and non-target organs were analyzed by HPLC. The magnetic chitosan microparticles significantly increased the concentration of tacrine in the brain in comparison with the free drug.
Wilson
Barnabas
B
Department of Pharmaceutics, J.S.S College of Pharmacy, Rocklands, Ootacamund, Tamil Nadu 643001, India. b_wilson@rediffmail.com <b_wilson@rediffmail.com>
Samanta
Malay Kumar
MK
Santhi
Kumaraswamy
K
Sampath Kumar
Kokilampal Perumal
KP
Ramasamy
Muthu
M
Suresh
Bhojraj
B
D000544:Alzheimer Disease / Q000188:drug therapy*; D000818:Animals; D001672:Biocompatible Materials / Q000008:administration & dosage; D048271:Chitosan / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000295:instrumentation / Q000379:methods*; D052203:Ferrosoferric Oxide / Q000008:administration & dosage / Q000493:pharmacokinetics; D007275:Injections, Intravenous / Q000379:methods; D008280:Magnetics / Q000379:methods; D008297:Male; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000008:administration & dosage* / Q000648:ultrastructure; D051381:Rats; D017208:Rats, Wistar; D013619:Tacrine / Q000008:administration & dosage*
D001672:Biocompatible Materials; D002800:Cholinesterase Inhibitors; D013619:Tacrine; D048271:Chitosan; D052203:Ferrosoferric Oxide