Acta Pharm. 63 (2013) 241-251
Short communication
Development of a self-microemulsifying drug delivery
system of domperidone: In vitro and in vivo characterization
RAMESH
JAKKI, MUZAMMIL AFZAL SYED, PRABHAKAR KANDADI and KISHAN VEERABRAHMA
Nanotechnology
Laboratory, Department of Pharmaceutics, University College of Pharmaceutical
Sciences, Kakatiya University, Warangal, Andhra Pradesh-506009, India
Accepted December 5, 2012
The main objective of this work was to prepare a self-micro emulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of domperidone, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. The in vitro self-micro emulsification properties and droplet size of SMEDDS were studied following their addition to water under mild agitation. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions (1:100, 1:500, 1:1000). The optimized formulation, SMEDDS-B used for in vitro dissolution and bioavailability assessment, contained oil (Labrafac CC, 25 %, m/m), surfactant (Tween 80, 55 %, m/m), and co-surfactant (Transcutol®, 20 %, m/m). The preliminary oral bioavailability of domperidone from SMEDDS was 1.92-fold higher compared to that of domperidone suspension in rats. The AUC0-24 and cmax values were 3.38 ± 0.81 µg h mL–1 and 0.44 ± 0.03 µg mL–1 for SMEDDS-B formulation in comparison with 1.74 ± 0.18 µg h mL–1 and 0.24 ± 0.02 µg mL-1 for domperidone suspension suggesting a significant increase (p < 0.05) in oral bioavailability of domperidone from SMEDDS.
Keywords: domperidone, SMEDDS, lipophilic drug delivery, particle
size, enhanced oral bioavailability