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Abstract
Topical delivery of local anesthetics has been an area of interest for researchers considering the barrier properties of skin and unfavorable physicochemical properties of drugs. In the present study, efforts have been made to modify the in vivo efficacy of eutectic mixture of lidocaine and prilocaine by exploiting the phospholipid modified microemulsion based delivery systems. The strategic QbD (D-optimal mixture design) enabled systematic optimization approach, after having obtained the isotropic area of interest by ternary phase diagram, has resulted into the system with most desirable attributes. Latter include nano-scale, globular structures with an average size of 40.6 nm, as characterized by TEM and DLS. The optimized microemulsion systems in gel dosage forms revealed the better permeability over commercial cream (CC) through abdominal rat skin. Enhancement in the flux from MOPT-NMP gel was 3.22-folds for prilocaine and 4.94-folds for lidocaine, in comparison to that of CC. This enhanced skin permeability is very well reflected in the in vivo studies, wherein intensity and duration of action was augmented significantly. The skin compliance of the optimized formulation was revealed in histopathological studies. The overall benefit relating to efficacy and safety-compliance could be correlated to the uniqueness of the carriers, composed of phospholipids and other components. Hence, the developed phospholipid-microemulsion based gel formulation has been proposed as more useful alternative for the topical delivery of lidocaine and prilocaine.
Acknowledgements
Authors are thankful to M/s Ipca Labs Ltd. Ratlam, India for generously providing the gift samples of lidocaine and Prilocaine, where to M/s Gattefosse, Hauptstrasse, Germanyand M/s Phospholipid GmbH, Nattermannallee, Germany, for the ex gratis supply of Labrasol®, Lauroglycol 90® and phospholipids, respectively.
Declaration of interest
The authors report no declarations of interest. Financial grants obtained from University Grants Commission (UGC), New Delhi, to one of us (Poonam Negi) are gratefully acknowledged.