SYNTHESIS, IN-SILICO PHYSICOCHEMICAL PROPERTIES AND ANTIMICROBIAL STUDIES OF PYRAZOLINE LOADED NANOPARTICLESAbstract
Pyrazolines were prepared from the corresponding chalcones by using isonicotinylhydrazine as cyclizing agent. The synthesized compounds were characterized by spectral data and screened for antimicrobial activity. In-silico studies of physiochemical and drug-like properties revealed that these compounds have good bioavailability and drug-likeness properties. Compound PZ2 which exhibited good antimicrobial activity was incorporated into polymeric nanoparticles using PLGA polymer by solvent evaporation method. The prepared nanoparticles were characterized by particle size, entrapment efficiency (EE%), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and in-vitro release studies. Prepared nanoparticles were incorporated into different hydrogel systems, which were prepared by using Carbopol 934 and HPMC in different concentrations ratio 2:1, 1:1 & 1:2. Hydrogel formulations were evaluated for drug content, spreadability, viscosity and drug release studies. Hence, the studies confirmed that entrapment of pyrazolthe ine as antimicrobial drugs in nanoparticle systems has found to be an inventive alternative that improves therapeutic effectiveness and curtails undesirable side effects of the drugs. Further, incorporation of pyrazoline nanoparticles into hydrogel provides an additional benefit of advanced permeation features of antimicrobial constituents for transdermal application.
J. P. James, S. Priya * and D. Jyothi
Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Deralakatte, Mangalore, Karnataka, India.
03 July 2018
11 February 2019
09 March 2019
01 April 2019