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Optimization of brain targeted gallic acid nanoparticles for improved antianxiety-like activity

Nagpal, Kalpana, Singh, S.K., Mishra, D.N.
International journal of biological macromolecules 2013 v.57 pp. 83-91
brain, corticosterone, drugs, gallic acid, locomotion, mice, nanoparticles, nitrites, particle size
Ligand coated nanoparticles may improve brain uptake of drugs. To formulate brain targeted nanoparticles of gallic acid (GA) for improving its antianxiety-like activity. The nanoparticles were prepared and optimized to minimize particle size and maximize percent drug entrapment efficiency using two factor three level (3²) central composite design. Pure GA, optimized ligand coated nanoparticles of GA (cGANP) and corresponding uncoated nanoparticles (GANP) were administered to Swiss albino mice for seven consecutive days and evaluated in vivo for their antianxiety-like activity. Behavioral studies revealed that cGANP significantly improved antianxiety-like activity in mice. The plasma nitrite level decreased with GA, GANP and cGANP (most pronounced for cGANP) treated group as compared to saline treated control group while no change in plasma corticosterone levels was observed in any treatment. The treatments (except alprazolam) did not show any significant effect on locomotor activity of mice. The antianxiety-like activity may be attributed to decreased plasma nitrite level and effect was improved by enhanced brain uptake of GA via ligand coated nanoparticles. Thus antianxiety-like activity of GA was significantly improved formulating it as ligand coated nanoparticles. On the other hand, no significant difference was observed between antianxiety-like activity by administration of pure GA and GANP.