Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS)
| Autor: | Dinesh P Asati, Gautam Mishra, Akash Chaurasiya, Roop K. Khar, Ajeet Kumar Singh, Anshumali Awasthi, Rama Mukherjee |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Chemistry
Pharmaceutical Biological Availability Pharmaceutical Science Antineoplastic Agents Absorption (skin) Aquatic Science Mass Spectrometry Excipients Surface-Active Agents chemistry.chemical_compound Drug Delivery Systems Microscopy Electron Transmission Exemestane Drug Discovery Electrochemistry Animals Self-microemulsifying drug delivery system Dissolution testing Microemulsion Particle Size Rats Wistar Solubility Chromatography High Pressure Liquid Ecology Evolution Behavior and Systematics Chromatography Ecology Aromatase Inhibitors General Medicine Hydrogen-Ion Concentration Rats Bioavailability Androstadienes chemistry Area Under Curve Drug delivery Thermodynamics Emulsions Female Agronomy and Crop Science Research Article |
| Zdroj: | AAPS PharmSciTech. 10:906-916 |
| ISSN: | 1530-9932 |
| Popis: | Limited aqueous solubility of exemestane leads to high variability in absorption after oral administration. To improve the solubility and bioavailability of exemestane, the self-microemulsifying drug delivery system (SMEDDS) was developed. SMEDDS comprises of isotropic mixture of natural or synthetic oil, surfactant, and cosurfactant, which, upon dilution with aqueous media, spontaneously form fine o/w microemulsion with less than 100 nm in droplet size. Solubility of exemestane were determined in various vehicles. Ternary phase diagrams were plotted to identify the efficient self-emulsification region. Dilution studies, droplet size, and zeta potential of the formulations were investigated. The release of exemestane from SMEDDS capsules was studied using USP dissolution apparatus in different dissolution media and compared the release of exemestane from a conventional tablet. Oral pharmacokinetic study was performed in female Wistar rats (n = 8) at the dose of 30 mg kg(-1). The absorption of exemestane from SMEDDS form resulted in about 2.9-fold increase in bioavailability compared with the suspension. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as exemestane by the oral route. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink