Utilization of a fattigation platform gelatin-oleic acid sodium salt conjugate as a novel solubilizing adjuvant for poorly water-soluble drugs via self-assembly and nanonization

In this study, gelatin and oleic acid sodium salt (OAS), a generally recognized as safe-listed material were chosen and conjugated to develop a natural solubilizing adjuvant using the fattigation platform technology to enhance solubility and dissolution rate of poorly water-soluble drugs according to self-assembly and nanonization principle when simply mixed with poorly water-soluble drugs. We synthesized the gelatin and OAS conjugates (GOC) at three different ratios (1:1, 1:3, 1:5; GOC 1, GOC 2, and GOC 3, respectively) via the 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide/N-hydroxysuccinimide reaction using a spray dryer. This amphiphilic micronized GOC was self-assembled into nanoparticles. The synthesis of new amphiphilic conjugates was identified through Fourier transform-infrared (FT-IR) spectroscopy. The powder properties of the GOCs, such as angle of repose, bulk density, and tapped density were varied with the oleic acid bonding ratio. Then, GOCs were utilized to investigate the enhanced solubility and release rate of various poorly water-soluble drugs such as cilostazol (CSZ), coenzyme Q10, ticagrelor, telmisartan, aprepitant and itraconazole as model drugs. Based on the solubility studies by concentration and type of GOCs, 3% GOC 2 was selected. When this GOC mixed with these model drugs by a physical mixture, the wet method and by hot melting, the solubility was highly enhanced compared to the pure control drug, ranging from 20-150,000 times. In case of CSZ, All ...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research