ENHANCED AQUEOUS SOLUBILITY AND IN VITRO DISSOLUTION OF THE ANTI-HYPERLIPIDEMIC AGENT USING SYNTHESIZED SOLID DISPERSION CARRIER

Abstract

Objective: To improve ATN's solubility, permeability, and dissolution rate of pentaerythritol-eudragit®RS100 co-processed excipients (CE) and their potential as a solid dispersion carrier (ATN-CE-SD). Methods: The ATN-CE-SD was prepared using the solvent evaporation technique. The pure ATN, physical mixture, CE carrier, and optimized ATN-CE-SD was physicochemically characterized using Scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, solubility, and in vitro dissolution was used to evaluate solid dispersions. Results: Physical and chemical analysis showed that ATN-CE-SD formed via the involvement of weak intermolecular forces of attraction between CE carrier and ATN. The prepared solid dispersion showed the drug content around ~ 96.94 % w/w, indicating that the solvent evaporation method improved the encapsulation of ATN and, thus, enhanced its drug content. Compared to pure ATN (~ 0.11 mg/ml), ATN-CE-SD (1:2) significantly increased the aqueous solubility by around ~ 25-fold (~ 2.78 mg/ml), indicating solid dispersion improves the solubility of ATN. ATN-CE-SD enhanced the rate of dissolution of ATV (~ 65 %) compared to pure ATN (~ 25 %) and PM (~ 34 %). Likewise, ATN-CE-SD (1:2) improved the rate and extent of ATN (~ 60 %) across the biological membrane compared to pure ATN (~ 22 %) and PM (~ 32 %). The ATN-CE-SD (1:2) improved the dissolution efficiency by around ~ (57.31%) compared to pure ATN (~ 7.02%) and PM (~ 20.43%). According to the study, co-processed excipients could serve as a promising solid dispersion carrier and improve ATN's water solubility, permeability, and dissolution rate. Conclusion: Based on the results, it is possible to use synthetic solid dispersion carriers as alternatives to improve the low water solubility and permeability of ATN.