Transdermal drug delivery system of domperidone sustained-release coated microsphere gels: In vitro characterization and in vivo evaluation

Abstract

Domperidone (DMP) is an effective peripheral D2 dopamine receptor antagonist. It is commonly used in the treatment of nausea and vomiting caused by Parkinson's disease. An oral preparation, which is rapidly absorbed after administration, and reaches a peak plasma concentration within 15–30 min, is commonly used. However, owing to the “first-pass effect” of liver metabolism and intestinal wall metabolism, the oral bioavailability of domperidone is low, and the action period is long. Therefore, in the present study, spray drying and emulsion solvent evaporation were combined to prepare a coated microsphere preparation with sustained release effect, and a gel matrix was selected to prepare a sustained-release coated microsphere gel for transdermal drug delivery. The pharmacokinetic results showed that the transdermal sustained-release coated microsphere gel effectively increased the Tmax, Cmax, T1/2, and AUC compared with those of an oral DMP group (P < 0.05), and the relative bioavailability was 3.2 times that of the oral DMP group. This indicates that the preparation was able to ameliorate the problems associated with a traditional oral DMP formulation. Therefore, the present study may provide a theoretical basis for the transdermal delivery of DMP sustained-release microspheres.