INVESTIGATING EFFECTS OF PERMEATION ENHANCERS ON PERCUTANEOUS ABSORPTION OF LOXAPINE SUCCINATE

Abstract

Objective: The objective of the present work is to explore and screen the potential of selected permeation enhancers in increasing the (Loxapine succinate) LX penetration in the presence of adhesives.

Methods: LX was utilized as a model drug for its possible delivery via the transdermal route. Urea (U)(5,7.5 and 10% w/v), oleic acid (OA) (0.1, 0.5 and 1% w/v), peppermint oil (PO) (0.3,0.5 and 1% w/v), dimethyl sulphoxide (DMSO) (2.5,5 and 7.5 % w/v), propylene glycol (PG) (5,7.5 and 10 % w/v) and ginger oil (GO) (0.3,0.5 and 1% w/v) were explored for their effects on permeation enhancement. Franz-type, six diffusion cell assembly was utilized for the permeation studies across excised pig ear skin section. Flux rate, permeation coefficient of LX and enhancement ratio obtained using different PEs were used as parameters for evaluating the best possible combination of adhesive along with PE for LX permeation.

Results: Results showed that flux of LX improved from 119 µg/cm²/h to 178.84±4.136µg/cm²/h with 10 % w/v U. 1% w/v OA, increased the flux up to 442.61 µg/cm²/h. Incorporation of 1 % w/v PO increased flux up to 505.55±6.195 µg/cm²/h with ER of 4.22. The use of 7.5 % w/v DMSO raised the flux value to 456.41±6.186 µg/cm²/h with ER of 3.81. The patches consisting of GO (1% w/v) provided flux 574.10±5.165 µg/cm²/h and ER up to 4.79. The use of 10 % w/v PG raised the flux value to 414.5±5.189 µg/cm²/h with ER of 3.45.

Conclusion: It can be concluded by the investigation done in the research that GO provides the maximum possible flux in comparison to other permeation enhancers.