Improved oral bioavailability of poorly water‑soluble vorinostat by self‑microemulsifying drug delivery system. Beni-Suef University Journal of Basic and Applied Sciences, 11: 99. ISSN 2314-8543 (2022)
Abstract
Background: Vorinostat is a histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) with anticancer
properties. However, it is plagued by low water solubility, low permeability (BCS class IV drug), and suboptimal
pharmacokinetics. The purpose of the present study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of vorinostat. Capryol 90, labrasol, and polyethylene glycol (PEG 400)
were selected as oil phase, surfactant, and co-surfactant, respectively. The vorinostat self-microemulsifying drug delivery systems were tested for self-microemulsifying time, phase separation, effect of pH, droplet size, zeta potential, dilution study, Fourier-transform infrared (FT-IR) spectroscopy analysis, and field emission scanning electron microscopy(FESEM). A rat model in vivo pharmacokinetic study was conducted for the optimized formulation against vorinostat pure drug powder.
Results: The results from the characterization studies showed that the optimized formulation (F7) self microemulsification time was 1.4 ± 0.05 min and no precipitation or phase separation was observed. The mean droplet size, polydispersity index (PDI), and zeta potential of the optimized formulation (F7) were found to be 272.9 ± 82.7 nm, 0.415, and − 57.2 mV, respectively. The pharmacokinetic parameters of the optimized formulation (F7) showed a 1.6-fold increase in maximum concentration (Cmax) and a 3.6-fold increase in area under the curve (AUC (0−∞)), in comparison with pure drug in suspension.Conclusions: The findings suggest that SMEDDS formulation could be an effective method for increasing the oral bioavailability of vorinostat, which is poorly water soluble.
| Item Type: | Article |
|---|---|
| Keywords: | Vorinostat, Self-microemulsion, Surfactant, Interface, In vivo pharmacokinetic study, Oral bioavailability |
| Taxonomy: | By Niche > Health Innovation > Medical Care By Niche > Health Innovation > Medical Care > Technological Innovations By Niche > Health Innovation > Public Health Research |
| Local Content Hub: | Niche > Health Innovation |
| Depositing User: | Wan Rohani Wan Chin (Hospital UiTM) |
| Date Deposited: | 26 Jun 2023 09:22 |
| Last Modified: | 26 Jun 2023 09:22 |
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