title: 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.
authors.affiliation: Department of Pharmaceutics, Kamla Nehru College of Pharmacy, Butibori, Nagpur, Maharashtra, 441108, India. pankaj_dangre@rediffmail.com.|Department of Pharmaceutics, Suresh GyanVihar University, Mahal, Jagtpura, Jaipur, Rajasthan, 302025, India. pankaj_dangre@rediffmail.com.
authors.forename: Pankaj
authors.identifier: 0000-0003-4750-9384
authors.initials: P
authors.lastname: Dangre
authors.affiliation: Department of Pharmaceutics, Suresh GyanVihar University, Mahal, Jagtpura, Jaipur, Rajasthan, 302025, India.
authors.forename: Ritu
authors.initials: R
authors.lastname: Gilhotra
authors.affiliation: Department of Pharmaceutics, Modern College of Pharmacy (For Ladies), Moshi, Pune, Maharashtra, 421105, India.
authors.forename: Shashikant
authors.initials: S
authors.lastname: Dhole
mesh_terms: D000179:Acrylates / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry; D007093:Imidazoles / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D010316:Particle Size; D051381:Rats; D012995:Solubility; D013876:Thiophenes / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D000179:Acrylates; D004655:Emulsions; D005079:Excipients; D007093:Imidazoles; D013876:Thiophenes; C068373:eprosartan
keywords: Bioavailability; Eprosartan mesylate; Factorial design; Optimization; Self-microemulsifying drug delivery system