Design and Development of Immediate Release Pellets Formulation Containing Co Amorphous Mixture of Aceclofenac: In-Vitro and In-Vivo Study

Abstract

Purpose

Aceclofenac is a nonsteroidal anti-inflammatory drug (NSAID) belonging to BCS Class II, has a constraint over its therapeutic benefits owing to its poor aqueous solubility.

Methods

In this study, co-amorphous mixtures of Aceclofenac (ACE) with Aspartame (ASPA) of various molar ratios at specific milling times were produced through ball milling (BM) technique. The characterization was done using FTIR, DSC and PXRD. The pellets formulation was prepared by extrusion spheronization method using 3² full factorial design. The optimized formulation was evaluated for in-vitro and in-vivo performance.

Results

Amongst the co amorphous mixtures and pure ACE studied for solubility, ACE: ASPA (1:1) showed the significant increase in solubility and was further formulated as pellets. Solid-state characterization of mixture revealed amorphization of ACE after 120 min of ball milling. In-vitro dissolution study data of F4 pellets formulation revealed (99.00 ± 3.59%) significant increase (P < 0.005) compared to pure drug (50.12 ± 2.52%) and other formulations. The in-vivo studies reveal a significant increase in percent inhibition of inflammation (61.7%) of the prepared formulation (p < 0.05) as compared to the marketed formulation (53.19%), and pure drug (46.8%).

Conclusion

Therefore, the prepared pellets of co-amorphous mixture of aceclofenac and aspartame, boost the solubility and stability of aceclofenac which has a potential to be a promising approach in the management of pain.

Graphical Abstract