Formulation and statistical optimization of self-microemulsifying drug delivery system of eprosartan mesylate for improvement of oral bioavailability

Abstract

The present investigation is aimed to design a statistically optimized self-microemulsifying drug delivery system (SMEDDS) of eprosartan mesylate (EM). Preliminary screening was carried out to find a suitable combination of various excipients for the formulation. A 3(2) full factorial design was employed to determine the effect of various independent variables on dependent (response) variables. The independent variables studied in the present work were concentration of oil (X 1) and the ratio of S mix (X 2), whereas the dependent variables were emulsification time (s), globule size (nm), polydispersity index (pdi), and zeta potential (mV), and the multiple linear regression analysis (MLRA) was employed to understand the influence of independent variables on dependent variables. Furthermore, a numerical optimization technique using the desirability function was used to develop a new optimized formulation with desired values of dependent variables. The optimized SMEDDS formulation of eprosartan mesylate (EMF-O) by the above method exhibited emulsification time, 118.45 ± 1.64 s; globule size, 196.81 ± 1.29 nm; zeta potential, -9.34 ± 1.2 mV, and polydispersity index, 0.354 ± 0.02. For the in vitro dissolution study, the optimized formulation (EMF-O) and pure drug were separately entrapped in the dialysis bag, and the study indicated higher release of the drug from EMF-O. In vivo pharmacokinetic studies in Wistar rats using PK solver software revealed 2.1-fold increment in oral bioavailability of EM from EMF-O, when compared with plain suspension of pure drug.

Self-nanoemulsfiying drug delivery system of bruceine D: a new approach for anti-ulcerative colitis

“…The release of BD from BD-SNEDDS in simulated intestinal fluid (pH 6.8) was significantly higher than that from BD suspension. Possible reasons include the following: 1) small droplet size of SNEDDS provided a large surface area for drug release into the aqueous phase; 2) BD might readily pass through dialysis membrane with the oil phase in SNEDDS; 63 3) release of BD from SNEDDS into the simulated gastric fluid (pH 1.2) was slower than that from suspension. This nature might allow BD-SNEDDS to survive in the harsh gastric environment and release in the intestine.…”

Enhancing Solubility of Candesartan Cilexetil by Co-milling; Preparation of Candesartan Cilexetil-glycyrrhizic Acid Composite

“…Determination of the dissolution rate in this study was according to method of the FDA [34] . The amount of milled products equivalent to 16 mg candesartan cilexetil and pure candesartan cilexetil were determined using a HTY-EU802 rotating paddle apparatus.…”

Lipid-based nanosystem of edaravone: development, optimization, characterization andin vitro/in vivoevaluation

“…To identify the self-emulsification region, a ternary phase diagram was plotted for the different ratios of an oil Capryol TM PGMC, surfactants Cremophor V R RH 40:Labrasol V R :TPGS 1000 in the ratio of 1:0.8:0.2, and a co-surfactant Transcutol P V R using Chemix V R School Software, trial version 3.6 (Oslo, Norway) (Dangre et al, 2016). In this mixture, the concentration of an oil, surfactant, and co-surfactant was varied from 0% to70% (w/w), 30% to 80% (w/w) and 0% to 30% (w/w), respectively.…”