Potential of microemulsified entacapone drug delivery systems in the management of acute Parkinson's disease

Abstract

A B S T R A C T Objective:To design solid self-microemulsifying drug delivery system (S-SMEDDS) of entacapone and evaluate for its anti-Parkinson's potentials. Methods: Solubility studies were performed in various vehicles i.e., oils, surfactants and co-surfactants and pseudo-ternary phase diagrams were plotted to understand the microemulsion formation region. Liquid self-microemulsifying drug delivery systems (SMEDDS) were developed using gingelly and rice bran oil as lipid vehicles, Tween 80 and Span 20 as surfactants and glycerin, propylene glycol as co-surfactants. They were characterized by Fourier transform infrared spectroscopy, pH, viscosity, zeta potential, polydispersibility index and droplet size analysis and evaluated for drug content, in-vitro release, in-vitro diffusion and ex-vivo permeation. Optimized liquid SMEDDS were converted into S-SMEDDS by adsorption and melt granulation procedures. Characterization by differential scanning calorimetry, SEM, micrometrics, reconstitution property, moisture content and evaluation by drug content, drug release kinetics and shelf-life were performed for S-SMEDDS. Parkinsonism was induced and pharmacodynamic potentials of S-SMEDDS were evaluated. Results: S-SMEDDS formulation AG8 had shown the highest drug release of 90.92% within 60 min. Pharmacodynamic studies also proved the efficiency of entacapone S-SMEDDS against Parkinsonism. Conclusions: Entacapone S-SMEDDS is an effective drug delivery system that offers more predictable and extensive drug release with enhanced shelf-life in the treatment of acute Parkinsonism.

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

“…Finally, the temperature of the cold trap was maintained at -53º until completion of the drying process. The resultant powder of EENS was further used for subsequent evaluation studies [29][30][31] .…”

“…Prior to size determination, lyophilized NS was redispersed in distilled water. Data obtained were mean average values of 3 independent samples that are prepared under the same formulation conditions [30,32] .…”

“…SEM studies were performed using an SEM (Jeol JSM-6360, Japan) at 20 kV accelerating voltage and high vacuum. Before analysis, lyophilized EENS were first placed on two-sided carbon tape and then, sputtered with gold-palladium alloy up to 3-5 nm of thickness [30,33] .…”

QbD Based Approach to Enhance the In-Vivo Bioavailability of Ethinyl Estradiol in Sprague-Dawley Rats

“…Each spectrum of samples was collected from an average of 21 single scans at 4 cm −1 resolution in the absorption area of 800-4000 cm −1 . 32…”

“…F rel of lyophilized EENPs after oral administration was computed according to the following formula with the EEAQD as a reference, (1) All data were expressed as mean ± SD and the level of significance was taken as P< 0.05. 32…”