Exemestane Loaded Self-Microemulsifying Drug Delivery System (SMEDDS): Development and Optimization |
| |
Authors: | Ajeet K Singh Akash Chaurasiya Manish Singh Satish C Upadhyay Rama Mukherjee Roop K Khar |
| |
Institution: | (1) Dabur Research Foundation, Plot No. 22, Site -IV, Sahibabad, Ghaziabad, Uttar Pradesh, 201010, India;(2) Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar-62, New Delhi, India |
| |
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). |
| |
Keywords: | aromatase inhibitors exemestane microemulsion SMEDDS |
本文献已被 PubMed SpringerLink 等数据库收录! |
|