A Novel Preparation Method for 5-Aminosalicylic Acid Loaded Eudragit S100 Nanoparticles

Abstract

In this study, solution enhanced dispersion by supercritical fluids (SEDS) technique was applied for the preparation of 5-aminosalicylic acid (5-ASA) loaded Eudragit S100 (EU S100) nanoparticles. The effects of various process variables including pressure, temperature, 5-ASA concentration and solution flow rate on morphology, particle size, 5-ASA loading and entrapment efficiency of nanoparticles were investigated. Under the appropriate conditions, drug-loaded nanoparticles exhibited a spherical shape and small particle size with narrow particle size distribution. In addition, the nanoparticles prepared were characterized by X-ray diffraction, Differential scanning calorimetry and Fourier transform infrared spectroscopy analyses. The results showed that 5-ASA was imbedded into EU S100 in an amorphous state after SEDS processing and the SEDS process did not induce degradation of 5-ASA.

Novel chewable colon targeted tablets of bumadizone calcium for treatment of ulcerative colitis: Formulation and optimization

“…The physical mixtures of the drug with the polymers( fig.1 a&b) resulted in the disappearance of such fusion peak, replaced by broad endothermic signals exhibiting reduced melting endotherm .The presence of endothermic signals in the physical mixtures confirmed that bumadizone crystals still exist in the physical mixtures .This was previously observed in the physical mixture of 5 aminosalicylic acid and piroxicam with Eudragit S100 [50,51] and diflunisal with Eudragit RL100 [52]. For confirmation X-ray diffraction measurements were carried out.…”

Impact of Microencapsulation on Two Probiotic Strains in Alginate Chitosan and Eudragit S100 Under Gastrointestinal and Normal Conditions

“…Retrospectively, a few studies have been conducted and accomplished worldwide. As a tangible example, Hu et al (2012) carried out the research in terms of application of EU S100 and acetone by SAS technique to create EU S100 nanoparticle, and they claimed, to achieve access to normal and integrated nanoparticles with 147 nm diameter in 15 MPa at 37°C. It appears that the results were fully appealing.…”

Solution-enhanced dispersion by supercritical fluids: an ecofriendly nanonization approach for processing biomaterials and pharmaceutical compounds

“…In addition, the increase in pressure augments the diffusion of SCF into the solvent, ensuing supersaturation that subsequently results in small-sized particles. [68][69][70] However, the changes in the pressure had no significant influence on the biological activity of the sensitive molecules such as enzymes. 71…”

“…In some instances, an increase in temperature results in severe aggregation of the particles with irregular surfaces due to collisions among the microparticles and vice versa. [68][69][70] To this end, the drug loading efficiency in the polymeric carriers is reduced during these conditions due to phase separation, which was articulated in a thermodynamics point of view.…”

“…However, the decrease in solution concentration, in turn, influences the loading efficiency of the drugs in the polymers. 68 In an attempt to explore the effect of organic non-solvent concomitantly with the solution concentration on the particle size and shape in SEDS, Chen et al demonstrated that the addition of DCM into the ethanolic solutions resulted in an initial concentration with a high degree of saturation yielding the small-sized particles with a spherical shape. 9,74 In this study, the authors described that the effect of solvent ratio was found to be prevailing on the particle sizes compared to that of the solution concentration.…”