Abstract

Objective: Self-microemulsifying drug delivery system (SMEDDS) of aceclofenac was developed to alleviate poor solubility and bioavailability issues.

Methods: The selection of components (oil, surfactant and co-surfactant) was based on saturated solubility studies and self emulsification ability. Pseudoternary phase diagrams were constructed to identify the self-emulsifying region. Isopropyl Myristate (IPM) was selected as oil phase; Cremophore as surfactant and Transcutol as co-surfactant (S/CoS mix) (in ratio of 1:1) respectively as optimized components for the SMEDDS formulation. The formulated liquid SMEDDS was evaluated for its self-emulsification time, phase separation, viscosity, cloud point and droplet size analysis. The liquid SMEDDS were converted to Solid SMEDDS by adsorption on solid carrier (Neusilin US2). Solid SMEDDS were further characterized for SEM, XRD, FTIR studies and evaluated for drug content, micrometric properties. Further Solid SMEDDS were compressed into tablet dosage form.

Results: In vitro drug release of liquid and Solid SMEDDS, optimized tablet batch was carried out in buffer (pH 7.4) at 37oC. The optimized formulation showed almost 100% drug release in 30 min and it was significantly higher than that of pure drug.

Conclusion: The study indicated the significance of aceclofenac SMEDDS as prospective carrier with enhanced dissolution characteristics for oral administration.

Keywords: Aceclofenac, solid-SMEDDS, neusilin, phase diagram, co-surfactant, cloud point, phase separation.

Graphical Abstract