Jagruti Prajapati
Ramanbhai Patel College of Pharmacy, India
Title: Brain targeting and bioavailability enhancement: Agomelatine microemulsion via intranasal administration
Biography
Biography: Jagruti Prajapati
Abstract
“Agomelatine” is melatonin receptor (MT1 & MT2) agonist and 5HT2c antagonist, widely used for major depressive episode, absolute bioavailability is <5%. The aim of present study is to develop Agomelatine microemulsion for intranasal delivery, to improve bioavailability. Preformulation study (Purity& Compatibility) was established by Melting point, λmax by UV–Visible spectrophotometry, FTIR, XRD, DSC. Solubility study of drug was conducted in various oils, non-ionic surfactants and co-surfactants. Ternary phase diagrams were constructed to evaluate the microemulsion regions for 1:1, 1:2, 1:3, 2:1, 3:1 of Smix (Chemix). A single isotropic region was found in pseudo-ternary phase diagrams. Microemulsion was formulated by water titration method. Smix ratio 1:1 was selected based on ternary phase diagram and conductivity measurement. In preliminary study, the concentration of oil and Smix were optimized on the bases of globule size. Reported dose of drug is successfully loaded in 0.1ml of ME prepared using optimized oil and Smix concentration range. Microemulsion of Agomelatine was optimized by mixture design of experiment. Prepared microemulsion was characterized by globule size (15 nm), viscosity (80 cps), zeta potential (-47mv) and TEM, Confocal Microscopy Study. In vitro drug release study of pure drug and Agomelatine Microemulsion was performed, in which Agomelatine microemulsion shows 100% Cumulative Drug Release which follows higuchi model. In vivo study (Pharmacokinetic and Pharmacodynamic) was also performed. Pharmacodynamic study was done by Forced Swim test. Pharmacokinetic study revealed that Bioavailability of Agomelatine Microemulsion was increased. Stability study of the same was also performed for heating-cooling cycle, freeze-thaw cycle and centrifugation.