Preparation and pharmacological evaluation of physostigmine-loaded polyisobutylcyanoacrylate nanoparticles in rats.
The nanoparticles of physostigmine were prepared by an emulsion polymerization of polyisobutylcyanoacrylate. The drug content, release and particle size distribution of the nanoparticles were characterized. In vitro drug release profiles displayed a retardation by the nanoparticles in comparison to the aqueous solution. Pharmacological evaluation of physostigmine nanoparticles in vivo were carried out with Sprague-Dawley rats. The endogenous acetylcholine was sampled by on-line microdialysis and determined by a sensitive microbore HPLC/ED system in the striatum of rats. The choline oxidase and catalase immobilized enzyme reactors were used as the pre-column to erase choline. Accordingly, this chromatographic flow sequence could be utilized for the quantitative assay of acetylcholine without interference. The results indicate that the increase of acetylcholine (%) in the rats striatum by the nanoparticle was 2.3 times (AUC) higher than that of aqueous solution.
Tsai
T R
TR
School of Pharmacy, Kaohsiung Medical College, Taiwan, Republic of China.
Chuo
W H
WH
Lin
C W
CW
Cham
T M
TM
D000109:Acetylcholine / Q000378:metabolism; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage*; D003487:Cyanoacrylates / Q000008:administration & dosage*; D004337:Drug Carriers; D004659:Enbucrilate; D008297:Male; D017551:Microdialysis; D010830:Physostigmine / Q000008:administration & dosage*; D011108:Polymers / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley
D002800:Cholinesterase Inhibitors; D003487:Cyanoacrylates; D004337:Drug Carriers; D011108:Polymers; D010830:Physostigmine; D004659:Enbucrilate; D000109:Acetylcholine