Explicating the molecular level drug-polymer interactions at the interface of supersaturated solution of the model drug: Albendazole

Eur J Pharm Sci. 2021 Oct 10:106014. doi: 10.1016/j.ejps.2021.106014. Online ahead of print.ABSTRACTSupersaturation phenomenon addresses aqueous solubility of poorly water soluble drugs. However, supersaturation state of drugs tends to crystallize because of its thermodynamic instability thereby compromising the solubility and biopharmaceutical performance of drugs. The present study aims to investigate the supersaturation potential of albendazole (ABZ) and its precipitation via nucleation and crystal growth. We hypothesized the use of polymers as precipitation inhibitors and drug polymer interactions are characterized using conventional methods of Fourier transform infrared (FTIR), Nuclear magnetic resonance (NMR) and Polarized light microscopy (PLM). We used a new method of sum frequency generation (SFG) vibrational spectroscopic in exploring the drug polymer interactions at air-water interface, which we reported elsewhere in the case of rifaximin-polymer interactions (Singh et al., 2021). The supersaturation assay, saturation solubility studies and nucleation induction time analysis revealed polyvinyl alcohol (PVA) and polyvinyl pyrrolidone (PVP K30) as effective precipitation inhibitors thereby enhancing the ABZ equilibrium solubility and in vitro supersaturation maintenance of ABZ. Further, modification in the solid state of ABZ revealed influence of polymers on its precipitation behaviour. We conclude that PVA and PVP K30 act as nucleation and crystal growth inhibitor, ...
Source: European Journal of Pharmaceutical Sciences - Category: Drugs & Pharmacology Authors: Source Type: research