Soy Protein Microparticles for Enhanced Oral Ibuprofen Delivery: Preparation, Characterization, and In Vitro Release Evaluation

Abstract

The objective of this work was to evaluate soy protein isolate (SPI) and acylated soy protein (SPA) as spray-drying encapsulation carriers for oral pharmaceutical applications. SPI acylation was performed by the Schotten-Baumann reaction. SPA, with an acylation rate of 41%, displayed a decrease in solubility in acidic conditions, whereas its solubility was unaffected by basic conditions. The drug encapsulation capacities of both SPI and SPA were tested with ibuprofen (IBU) as a model poorly soluble drug. IBU-SPI and IBU-SPA particles were obtained by spray-drying under eco-friendly conditions. Yields of 70 to 87% and microencapsulation efficiencies exceeding 80% were attained for an IBU content of 20 to 40% w/w, confirming the excellent microencapsulation properties of SPI and the suitability of the chemical modification. The in vitro release kinetics of IBU were studied in simulated gastrointestinal conditions (pH 1.2 and pH 6.8, 37°C). pH-sensitive release patterns were observed, with an optimized low rate of release in simulated gastric fluid for SPA formulations, and a rapid and complete release in simulated intestinal fluid for both formulations, due to the optimal pattern of pH-dependent solubility for SPA and the molecular dispersion of IBU in soy protein. These results demonstrate that SPI and SPA are relevant for the development of pH-sensitive drug delivery systems for the oral route.

Application of legume‐based materials in encapsulation technology: A review

“…This suggests that soy proteins are capable of conveying the probiotics' physiological activity to the intestine with higher functionality (González-Ferrero et al, 2018). The in vitro gastrointestinal digestion of SPI and acylated soy protein for oral ibuprofen release was studied by Castro et al (2018). The findings indicated that these proteins could be employed to increase the bioavailability of poorly soluble medications to speed up absorption in the gut (Castro et al, 2018).…”

“…The in vitro gastrointestinal digestion of SPI and acylated soy protein for oral ibuprofen release was studied by Castro et al (2018). The findings indicated that these proteins could be employed to increase the bioavailability of poorly soluble medications to speed up absorption in the gut (Castro et al, 2018). For in vitro release under stomach circumstances alone and in conjunction with intestinal conditions, flaxseed oil that has been encapsulated with the combination of SPI and modified starch was tested.…”

Design of sodium alginate/soybean extract beads loaded with hemp hurd and halloysite as novel and sustainable systems for methylene blue adsorption

“…The two thermal steps concerning the mass losses, from 200 to 300 C, could be related to the breaking of the alginate backbone as well as loss of OH groups due to the dehydration. [54,55] Above 300 C, SA is known to decarboxylate releasing CO 2 and other low molecular weight gases, while soy protein degradation occurred between 250 C and 450 C. [56] The presence of HH did not lead to further decomposition steps since the thermal decomposition of its main compounds (holocellulose, cellulose, hemicellulose, and lignin) occurred roughly in the same temperature ranges. The last thermal step (470-570 C) could then be related to the dehydroxylation of Al-OH groups.…”

Protein-Based Structures for Food Applications: From Macro to Nanoscale

“…These microgels can be a useful tool for tissue engineering. In addition, Anaya Castro et al (2018) produced SPI and acylated soy protein microparticles by spraydrying to encapsulate and release ibuprofen (a poorly soluble drug model). These authors obtained high microencapsulation efficiencies, confirming the excellent properties of these proteins to encapsulate and be used as pH-sensitive delivery systems for the oral route (Anaya Castro et al, 2018).…”