Abstract
In the present study, ketoprofen-p-aminobenzoic acid (KP-PABA) co-crystal was prepared, to advance solubility and dissolution rate of drug, by solvent evaporation technique employing central composite experimental design. The optimized batch as recommended by the experimental design was characterized by FTIR, DSC, XRD, SEM, and NMR studies and further, evaluated for in-vitro and in-vivo anti-inflammatory and analgesic activities. The solubility and % drug release of different batches of co-crystal was found to be between 34.20–60.11 µg/ml and 68.11–93.45%, respectively. Physical characterization by X-ray diffraction spectra and differential scanning calorimetric studies confirmed the crystallinity of prepared co-crystal. The IC50 value of optimized batch of co-crystal formulation and pure drug was observed as 248.79 µg/ml and 524.40 µg/ml, respectively, displaying that co-crystal formulation possesses more percentage protection against protein denaturation than the drug ketoprofen. The results of in-vivo anti-inflammatory activity carried out by rat paw edema method revealed that the optimized batch of co-crystal preparation provided a significant % inhibition in paw volume in contrast to standard drug in wistar rats. Hence, the crystalline molecular complex of ketoprofen with p-aminobenzoic acid was documented that set out an improvement in solubility and also in anti-inflammatory activity of the drug in wistar rats.
Highlights
Co-crystal are described as a multicomponent crystalline material possessing two or more molecules that are connected by noncovalent interactions in the same crystal lattice [1,2]
Ketoprofen - p-amino benzoic acid (KP-PABA) co-crystal was prepared by the solvent evaporation method as reported earlier [34]
Ketoprofen and PABA were used in stoichiometrically equal ratio and after carefully weighing were dissolved in10mL of acetic acid gel
Summary
Co-crystal are described as a multicomponent crystalline material possessing two or more molecules (i.e., drug and coformer) that are connected by noncovalent interactions in the same crystal lattice [1,2]. Co-crystal have the ability to improve the drug dissolution, bioavailability, hygroscopicity, solubility, processability and physical/chemical stability of the compound as compared to active pharmaceutical ingredient (API) [3, 4]. Co-crystallization is an advanced method to improve pharmaceutical solid dosage form. The preference of a method to produce cocrystal is crucial and depends on different factors for example thermal stability, alteration in solubility of coformers and API in particular solvents, tendency to form stable polymorphs or solvates and availability of a sufficient amount of the substance [5]. The difference between pKa value of API and coformer (i.e., ∆pKa) depicts the co-crystal formation capability of a coformer with a given API [6, 7].
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