Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery

Abstract

The potential value of succinylated soy protein (SPS) as a wall material for the encapsulation of ibuprofen (IBU), a model hydrophobic drug, by spray-drying was investigated. A succinylation rate of 93% was obtained for soy protein isolate, with a molar ratio of 1/1.5 (NH 2 /succinic anhydride). The solubility profile at 37°C showed that this chemical modification decreased the solubility of the protein below its isoelectric point, whereas solubility increased in alkaline conditions. Various SPS/IBU ratios (90/10, 80/20, and 60/40) were studied and compared with the same ratio of soy protein isolate (SPI/IBU). High encapsulation efficiency was achieved (91-95%). Microparticles were spherical and between 4 and 8 μm in diameter. The spray-drying of protein/IBU solutions appeared to be beneficial, as it resulted in an amorphous solid dispersion of IBU within the microparticles, coupled with an increase in the thermal stability of IBU. In vitro release was evaluated in acidic (pH 1.2 in the presence of pepsin) and neutral (pH 6.8) conditions similar to those in the gastrointestinal (GI) tract. IBU was released significantly more slowly at pH 1.2, for both proteins. However, this slowing was particularly marked for SPS, for which rapid (within 2 h) and complete release was observed at pH 6.8. These results validate the hypothesis that SPS is suitable for use as a coating material for hydrophobic active pharmaceutical ingredients (APIs) due to its pH sensitivity, which should delay IBU release in the gastrointestinal tract.

Microencapsulation for Pharmaceutical Applications: A Review

“…In addition, liposomal encapsulation was superior to the microemulsion in terms of transdermal delivery of ibuprofen. 106 Bioactive amygdalin, abundant in bitter almonds, has been considered as cyanogenic glycoside chemical organic substance, which was initially developed as an API for treating cancer after being hydrolyzed to hydrogen cyanide (HCN). However, later HCN was revealed to damage normal cells.…”

“…Therefore, several microencapsulation technologies were conventionally applied to overcome these drawbacks such as spray drying, coacervation, microemulsion, extrusion, liposome, and other applications. − Interestingly, the most recent technology, liposomal encapsulation (ethanol-solvent injection), was compared to the microemulsion (spontaneous emulsification) in delivering ibuprofen transdermally, and liposomal encapsulation exhibited excellent permeability due to their interaction with the lipid bilayer and the protein. In addition, liposomal encapsulation was superior to the microemulsion in terms of transdermal delivery of ibuprofen …”