Influence of the Impregnation Technique on the Release of Esomeprazole from Various Bioaerogels

Abstract

The presented study shows the possibility of using bioaerogels, namely neat alginate, pectin, chitosan aerogels, and alginate and pectin aerogels coated with chitosan, as drug delivery systems for esomeprazole. Two different techniques were used for the impregnation of esomeprazole: Supercritical impregnation, and diffusion via ethanol during the sol-gel synthesis. The prepared samples were characterized by employing N2 adsorption-desorption analysis, TGA/DSC, and FTIR. The achieved loadings were satisfactory for all the tested samples and showed to be dependent on the technique used for impregnation. In all cases, higher loadings were achieved when impregnation via diffusion from ethanol was used. Extensive release studies were performed for all impregnated samples. The in vitro dissolution profiles were found to be dependent on the carrier and impregnation method used. Most importantly, in all cases more controlled and delayed release was achieved with the bioaerogels compared to using pure esomeprazole.

Supercritical Fluid Technologies for the Incorporation of Synthetic and Natural Active Compounds into Materials for Drug Formulation and Delivery

“…Optimizing the drug release kinetics controlled by the diffusion mechanism and polymer degradation for a particular application is very important. Successful attempts have already been made to achieve the controlled release of AIs from biodegradable aerogels in simulated gastric and intestinal fluids [100,101]. In addition, the solubility of AIs with a hydrophobic character was significantly improved by their incorporation into aerogels [94,97,102].…”

“…Many studies have confirmed that embedding the AI in biodegradable polysaccharide aerogels is promising for oral drug delivery. Compared to crystalline AIs, these aerogels achieve more controlled release over a period of several hours to several days of testing [100,102,142]. Compared to the incorporation of AIs into aerogels, SC foaming often achieves long-term release of several days to 1-2 months due to the structural properties of polymer foams (PCL, PLA, PLGA), which is why their application is often focused on biomedical purposes (implant coatings, tissue engineering) [118,143].…”

Fabrication of Polymeric Hydrogels Containing Esomeprazole for Oral Delivery: In Vitro and In Vivo Pharmacokinetic Characterization

“…Esomeprazole has low water solubility and high permeability [ 29 ]. It has better pharmacokinetic (PK) profiling than omeprazole in the management of acid-related problems [ 30 ]. It has been studied that developed hydrogel preparations could be suitable carriers for the delivery of esomeprazole for the improvement of bioavailability [ 31 ].…”

Development, In-Vitro Characterization and Preclinical Evaluation of Esomeprazole-Encapsulated Proniosomal Formulation for the Enhancement of Anti-Ulcer Activity

“…EZL is low water-soluble and highly permeable [2]. It has superior pharmacokinetic profiling over omeprazole in monitoring acid-related ailments [3]. The fact that the stability of esomeprazole decreases with a decrease in pH of media means that the contact of EZL with the acidic content of the stomach leads to degradation of EZL and may reduce the bioavailability [4].…”