Original Article
Chitosan nanoparticles as a new delivery system for the anti-Alzheimer drug tacrine

https://doi.org/10.1016/j.nano.2009.04.001Get rights and content

Abstract

Tacrine-loaded chitosan nanoparticles were prepared by spontaneous emulsification. The particle size and zeta potential was determined by scanning probe microscopy and Zetasizer, respectively. The prepared particles showed good drug-loading capacity. The in vitro release studies showed that after the initial burst, all the drug-loaded batches provided a continuous and slow release of the drug. Coating of nanoparticles with Polysorbate 80 slightly reduced the drug release from the nanoparticles. Release kinetics studies showed that the release of drug from nanoparticles was diffusion-controlled, and the mechanism of drug release was Fickian. The biodistribution of these particles after intravenous injection in rats showed that of nanoparticles coated with 1% Polysorbate 80 altered the biodistribution pattern of nanoparticles.

From the Clinical Editor

In this paper, chitosan nanoparticles are investigated in a pre-clinical study as an optimized delivery system for tacrin, a drug with potential significance in Alzheimer's disease. The preparation showed optimal pharmacokinetic characteristics in a rat model.

Section snippets

Materials

The drug tacrine (9-amino-1,2,3,4-tetrahydroacridine) was purchased from Sigma (St. Louis, Missouri). Linseed oil was purchased from National Chemicals (Vadodara, India). Chitosan was a gift from Central Marine Fisheries Research Institute (Cochin, India). All other materials and reagents used in the study were analytical/high-performance liquid chromatography (HPLC) grade and used as purchased.

Preparation of chitosan nanoparticles

The chitosan nanoparticles containing the drug tacrine were prepared by the method of spontaneous

Nanoparticles

Chitosan nanoparticles of the drug tacrine with different drug-to-polymer ratios (1:1, 1:1.5, 1:2, 1:2.5, and 1:3) were prepared by spontaneous emulsification. Table 1 shows the process yield, percentage drug loading, and particle size of chitosan nanoparticles. Yields of production ranged between 77.50% ± 3.17% and 83.33 ± 1.46% depending on the drug-to-polymer ratio used. The nanoparticles prepared using a drug-to-polymer ratio of 1:1 showed the highest value. The drug-loading capacity

Preparation of chitosan nanoparticles

Chitosan nanoparticles of the drug tacrine with different drug-to-polymer ratios (1:1, 1:1.5, 1:2, 1:2.5, and 1:3) were prepared by spontaneous emulsification. Chitosan has many advantages for developing nanoparticles, including the ability to control the release of active agents and avoidance of the use of hazardous organic solvents while fabricating particles because of its solubility in aqueous acidic solution; it is a linear polyamine containing a number of free amine groups that are

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