title: Exemestane loaded self-microemulsifying drug delivery system (SMEDDS): development and optimization.
abstract: The purpose of this research work was to formulate and characterize self-micro emulsifying drug delivery system containing exemestane. The solubility of exemestane was determined in various vehicles. Pseudo ternary phase diagram was used to evaluate the micro-emulsification existence area. SMEDDS formulations were tested for micro-emulsifying properties, and the resultant formulations loaded with exemestane (ME1, ME2, ME3, ME4 and ME5) were investigated for clarity, phase separation, globule size and shape, zeta potential, effect of various diluents and dilutions, thermodynamic and thermal stability. From the results it is concluded that increase in droplet size is proportional to the concentration of oil in SMEDDS formulation. Minor difference in the droplet size and zeta potential was observed by varying the diluents (deionized water and 0.1 N HCl) and dilutions (1:10, 1:50 and 1:100). Formulations, which were found to be thermodynamically stable (ME1, ME2, ME3 and ME4), were subjected to stability studies as per International Conference on Harmonization (ICH) guidelines. No significant variations were observed in the formulations over a period of 3 months at accelerated and long-term conditions. TEM photographs of microemulsions formulations further conformed the spherical shape of globules. Among the various SMEDDS formulations, ME4 offer the advantages of good clarity systems at high oil content and thus offer good solubilization of exemestane. Thus this study indicates that the SMEDDS can be used as a potential drug carrier for dissolution enhancement of exemestane and other lipophilic drug(s).
authors.affiliation: Dabur Research Foundation, Plot No. 22, Site -IV, Sahibabad, Ghaziabad, Uttar Pradesh 201010, India. ajeetrj@rediffmail.com
authors.forename: Ajeet K
authors.initials: AK
authors.lastname: Singh
authors.forename: Akash
authors.initials: A
authors.lastname: Chaurasiya
authors.forename: Manish
authors.initials: M
authors.lastname: Singh
authors.forename: Satish C
authors.initials: SC
authors.lastname: Upadhyay
authors.forename: Rama
authors.initials: R
authors.lastname: Mukherjee
authors.forename: Roop K
authors.initials: RK
authors.lastname: Khar
mesh_terms: D000730:Androstadienes / Q000737:chemistry*; D047072:Aromatase Inhibitors / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004655:Emulsions; D046529:Microscopy, Electron, Transmission; D009821:Oils / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D013816:Thermodynamics
chemical_list: D000730:Androstadienes; D047072:Aromatase Inhibitors; D004337:Drug Carriers; D004655:Emulsions; D009821:Oils; D013501:Surface-Active Agents; C056516:exemestane