Development, characterization and solubility enhancement of BCS class II drug phenytoin by solid phospholipid dispersion technique

Abstract

The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. Phenytoin is taking as a model drug; the present study adopted an innovative solid phospholipid nanoparticle (SPLN) line of attack, and it is parallelly equated with the industrialized methods (freeze-drying) which are used for the boosting of solubility and dissolution of Phenytoin. Phenytoin was articulated along with phospholipid and mannitol at a diverse ratio of phenytoin, PL, mannitol, in which 1:12:18 was the correct ratio for ideal preparation. Freeze-drying helps to prepare SPLNs in orbicular shape, which is amorphous in nature with ≤ 1µm diameter on average. While the amorphous matrix-like structure of solid phospholipid dispersion with larger particle size is obtained by freeze-drying technique. Formulating the formulation from this method improved the dissolution rate in a remarkable way. Tris buffer with pH 7.4acts as an apparent solubility dissolved concentration of phenytoin. The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. The decrease in the particle size or cumulating the drug surface area is the widely used practices to proliferate the solubility. The target of the present work was improvisation in solubility, dissolution of a poorly water-soluble drug, and its release by using solid phospholipid nanoparticles. Phenytoin is taking as a model drug. The solid phospholipid nanoparticles were primed by freeze-drying technique along with phospholipid and mannitol in diverse drug to excipients ratios (1:1, 1:2w: w). These preparations were assessed for compatibility study using FTIR, solubility enhancement study by XRD, entrapment efficiency, surface morphology by SEM, and in-vitro release study. As per the results, there is no influence of the excipients on the drug used. The solubility was increased by folds compared to in house prepared formulation.