(W0930-11-74) Synergistic Effect of Bioenhancer for Increasing the Permeation of Lopinavir via Phospholipid Complexation

Purpose: The present study was initiated with the aim to prepare and evaluate phospholipid complex of lopinavir with bioenhancers for enhancement of bioavailability.

Methods: The prepared complex of Lopinavir withPhospholipon 90H® (lopinavir-phospholipid complex) using solvent evaporation methods and evaluated for physicochemical characterization such as microscopic study, particle size and zeta potential, FTIR, DSC and PXRD. Functional efficacy was assessed on the basis of dissolution and permeation study.

Results: Lopinavir content in the complex was found to be (94.09 ± 1.56). The SEM study showed that optimized lopinavir-phospholipid complex was appeared to be larger, opaque, irregularly-shaped and non-crystalline with a porous surface, possibly entrapping the lopinavir in Phospholipon 90H®. The prepared lopinavir-phospholipid complex along with bioenhancer (Piperin) showed a dramatic and a significant increase in the aqueous solubility over 1.5 and 10 fold, significantly faster release of lopinavir (82% w/w) at the end of 10 h of dissolution study as compared to pure lopinavir (50% w/w). The ex-vivo permeation study at the end of 3 h showed 1.42-fold increase in the permeation coefficient (k_p).

Conclusion: Use of bioenhancer along with phospholipid complexation is the efficient and promising strategy for the oral administration of lopinavir to overcome the barrier of poor aqueous solubility and hence bioavailability.