Coamorphisation of acetyl salicylic acid and curcumin for enhancing dissolution, anti-inflammatory effect and minimizing gastro toxicity

Abstract

ObjectiveThe study was aimed to develop coamorphous mixture of acetyl salicylic acid (ASA) and curcumin (CU) for enhancing dissolution, anti-inflammatory effect and minimizing gastro toxicity. SignificanceDeveloped coamorphous of ASA and CU enhanced solubility and anti-inflammatory efficacy while minimizing the gastro toxicity at low dose level. MethodsThe coamorphous were developed by solvent evaporation method at various weight ratios of drugs: PVP K 30 and optimized. The mixtures were characterized for saturation solubility, amorphism (PXRD, DSC, FTIR), SEM, in vitro dissolution. The anti-inflammatory and gastro protective activities were performed to assess the bioavailability and gastro toxicity of the ASA and CU coamorphous mixture respectively. ResultsSolubility study revealed ~5.5 and ~3076 fold rise in solubility of ASA and CU than their pure form. Solid state characterization of the coamorphous mixture suggested complete amorphisation of the ASA and CU at 1:3 weight ratio. FTIR study confirmed the hydrogen bond formation suggested the enhancement of solubility and leads to bioavailability. DSC, PXRD and SEM confirmed the amorphism. Adequate release of ASA and CU suitable for ensuring oral bioavailability and efficacy and also be expected to be a suitable formulation for oral administration of mixture. Significant inhibition (5 fold) of paw edema and protective index (>75) of SD revealed enhancement of anti-inflammatory activity and reduction of gastro toxicity. ConclusionCoamorphous mixture of ASA and CU at low dose level is a promising approach for combination therapy in inflammation.