Formulation and evaluation of maline based solid super-saturable self-emulsifying drug delivery system for risperidone

Abstract

Objective: Solid super-saturable self-emulsifying drug delivery system of risperidone was formulated utilizing maline; a type of a deep eutectic choline based ionic liquid (DEIL), as oil phase in order to enhance the drug's solubility, dissolution, and intestinal penetration, and therefore its bioavailability.
Method: Maline was prepared using 1:1 molar ratio choline chloride and malonic acid. The SEDDs was formulated using maline as oil phase, tween80 or tween 20 as surfactant, and PEG600 or PG as co-surfactant in comparsion to conventional one using oleic acid as oil phase. Soluplus was utilized as drug precipitation inhibitor. For SEDDs solidification Aerosil 200 adsorbant was used as a carrier.
Results: The mean droplet size of the optimized formulation 210.3 nm with polydispersity of 0.357, zeta potential -3.47, drug content 100.21±0.47%. The optimum solid supersaturable SEDDs formula (SSM) showed excellent flow properties with Carr’s Index of 8.77%, Hausner ratio of 1.09, and angle of repose at 38.72○. The FTIR, DSC and XRD results showed a good drug excipient compatability.Ex vivo permeation test on isolated sheap intestine revealed an inhancement in the risperidone amount permeated from the optimum formulation comparable to that of the pure drug and marketed tablet and even the conventional solid S-SEDDs formula.
Conclusion: The developed Maline based solid super-saturable self-emulsifying drug delivery system of risperidone can be considered as an innovative, economically feasible alternative to existing risperidone formulations and a promising method for enhancing the oral bioavailability of poor soluble drugs.