CJ Mbah1*, P Harry2 and KM Ezealisiji2
1Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
2Faculty of Pharmaceutical Sciences, University of Port-Harcourt, Nigeria
*Corresponding Author: CJ Mbah, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria.
Received: March 21, 2018; Published: April 19, 2018
Citation: CJ Mbah., et al. “Prediction of Skin Permeability of Praziquantel: pH-Permeability Relationship”. Acta Scientific Pharmaceutical Sciences 2.5 (2018).
Skin permeability of drugs determines the rate and extent these agents cross the tissue and be absorbed into the systemic circulation to reach their sites of action. Praziquantel, is clinically used for the treatment of all types of schistosomiasis.
The purpose of the present study was to predict the probable pH effect on the permeability of praziquantel through the skin using data obtained from the effect of pH on the partition coefficient of praziquantel.
The partition coefficient was determined by shake-flask method at room temperature using chloroform-buffer system. A highly effective mathematical model equation was used to estimate the permeability coefficient. The maximum flux through the skin was obtained by multiplying the estimated permeability coefficient and aqueous solubility of the drug. A cubic equation that defined relationship between activation energy and logarithm of partition coefficient was utilized to calculate the activation energy involved in the partitioning of the drug in chloroform-buffer system. The diffusion coefficient through the membrane was estimated using an equation relating permeability coefficient, skin-vehicle partition coefficient and the average thickness of the stratum corneum. The results show pH of the buffer solutions to have varying effect on the partition coefficient of the drug. A non-linear curve was observed when logarithm of partition coefficient was plotted against the pH of buffer solution. The results obtained from the study also showed that the estimated permeability coefficient increased 2.5- fold at pH 2.0 and 3.2-fold at pH 8.0 respectively when compared to distilled water. This leads to the conclusion that the skin permeability of praziquantel is most favoured at slightly high basic pH value (pH 8.0).
Keywords: Praziquantel; Partition Coefficient; pH; Skin Permeability Coefficient
Copyright: © 2018 CJ Mbah., et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.