Preparation, characterization and evaluation of aspirin: benzoic acid cocrystals with enhanced pharmaceutical properties

Abstract

Background: The cocrystallization process in pharmaceuticals has gained widespread attention as a recent method of modifying physicochemical properties without altering the pharmacological characteristics of drugs. Cocrystallization provides a couple of benefits like it can be employed for a large number of APIs (acidic, basic, ionizable, or non-ionizable), and secondly, the availability of a large number of potential coformers increases the possibility of the cocrystals (CCs) that can be synthesized for an API. The main objective of this study was to investigate the effects of cocrystallization on drugs having poor aqueous solubility. Results: Aspirin (AN) and benzoic acid (BZ) were cocrystallized by using the solvent evaporation technique. CSD (Cambridge Structure Database) software and ΔpKa value method were used for the selection of the drug and coformer and for prediction of CC formation. The analysis of CCs was performed using DSC (differential scanning calorimetry), FT-IR (Fourier transformation infra-red spectroscopy) and XRD (X-ray diffraction) techniques. In vivo anti-inflammatory studies were conducted on 24 Wistar rats divided into four groups. Conclusions: Here, in this study, in vitro dissolution studies revealed an improved solubility profile of CCs compared to pure drug and marketed formulation viz. 87%, 31% and 60% respectively. The in vivo antiinflammatory studies exhibited improved anti-inflammatory activity compared to pure drug. So, on the basis of outcomes of this study, we concluded that cocrystallization process have a direct impact on the improvement of physicochemical characteristics of APIs having issues like solubility or stability without any modification and alteration of their pharmacological actions.

Lawsone Co-Crystals Loaded Antifungal Gel for Cutaneous Candidiasis

“…The creation of hydrogen bonding between lawsone and coformer, resulted in formation of the newer crystal structure with different crystalline properties. The formation of this new structure with enhanced pharmaceutical properties is in line with the studies carried out by Braham Dutt and coworkers [24]. The decrease in the particle size of the co-crystal, resulted in better interaction of drug with Candida albicans and enhanced antifungal activity even in the half the amount of the pure lawsone.…”

Formulation and Evaluation of Aspirin-PLGA Microsphere for the Dental Stem Cell Stimulation

“…Similar peaks were reported in the literature. 14,15 Whereas, no distinct and intense peak in the diffractogram of PLGA was observed demonstrating the amphorous nature. Aspirin peaks were not observed in the XRD pattern of the Aspirin microsphere, exhibiting that aspirin is uniformly dispersed in the polymer matrix, revealing the amorphous form.…”

“…Powder X-ray Diffraction (PXRD) 14,15 PXRD for the drug, polymer, physical mixture, and formulations were carried out using a D8 Advance BRUKER diffractometer. Samples were mounted on aluminum plates and measured at 2θ diffraction angle from 0 to 40° with a source of nickel-filtered and Cu-anode ceramic 14,15…”

“…In the present study, Aspirin exhibited endothermic peak at 144. 82°C (sharp) with 170.98 J/g of enthalpy of fusion (H) 14,15 represents its melting point (Figure 7). Another endothermic peak was also observed at 172.24°C, which may be partly superimposed to the melting one and is ascribable to the thermal degradation of aspirin, this confirms the crystalline nature of the drug.…”

Modification of Physicochemical Properties of Active Pharmaceutical Ingredient by Pharmaceutical Co-Crystals

“…Differential scanning calorimetry, Fourier transformation infrared spectroscopy and X-ray diffraction methods were used for the analysis of CCs. A total of 24 Wistar rats divided into four groups participated in in vivo anti-inflammatory studies [89]. Bwalya A. Witika et al prepared co-crystal of zidovudine (AZT) and lamivudine (3TC) that are antiviral agents used orally to manage HIV/AIDS infection.…”