Formulation and evaluation of domperidone oral proliposomal powders Article

Nalla, P, Bagam, S, Eedara, BB et al. (2015). Formulation and evaluation of domperidone oral proliposomal powders . 7(1), 108-118.

cited authors

  • Nalla, P; Bagam, S; Eedara, BB; Dhurke, R

abstract

  • The main objective of research work was to develop and characterize proliposomal powders of domperidone for improved solubility and oral bioavailability. Domperidone is a specific 5HT3 receptor antagonist used in the treatment of nausea and vomiting. It has low aqueous solubility and moreover after oral administration it undergoes extensive gastric and hepatic first pass metabolism. This results in very low oral bioavailability which may not decrease rate of vomiting. Proliposomal powders were developed using various ratios of hydrogenated soyphosphatidylcholine, cholesterol, and sodium cholate. The mean size of the vesicles was in the range of 390 to 520 nm. The entrapment efficiency of domperidone was found to be 44 to 90%. Values of Q60 observed for proliposome formulations were ranging from 69% to 92%. Photomicrographs obtained by SEM shows the transformation to amorphous state. XRD studies showed decrease in intensity of peak due to formation of some amorphous state. Ex- vivo studies data depicts increased permeation of formulation. The peak serum concentration of domperidone obtained from domperidone proliposomal powders with charge inducers (DOMPL-SC) was significantly higher in contrast to control (p<0.001) whereas the time to reach the peak concentration (Tmax) remained same. The extent of absorption assessed from AUC following oral administration of DOMPL-SC was significantly higher compared to control (p<0.001). There were no signs of instability such as agglomeration, crystallization seen even after 90 days of stability studies.

publication date

  • January 1, 2015

start page

  • 108

end page

  • 118

volume

  • 7

issue

  • 1