Soy Protein Microparticles for Enhanced Oral Ibuprofen Delivery: Preparation, Characterization, and In Vitro Release Evaluation
- 64 Downloads
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.
KEY WORDSvegetal protein microencapsulation oral route modified release pH sensitivity
We would like to thank the Mexican Council of Science CONACyT for providing financial support, Yannick Thebault and Cédric Charvillat from CIRIMAT for SEM and XRD analyses, and Christine Rey-Rouch from LGC for TGA analyses.
- 2.Bosselmann S, Williams RO III. Route-specific challenges in the delivery of poorly water-soluble drugs. Formulating poorly water soluble drugs. Berlin: Springer; 2012. p. 1–26.Google Scholar
- 17.Hadzieva J, Mladenovska K, Crcarevska MS, Dodov MG, Dimchevska S, Geškovski N, et al. Lactobacillus casei encapsulated in soy protein isolate and alginate microparticles prepared by spray drying. Food Technol Biotechnol. 2017;55(2):173–86. 10.17113/ftb.55.02.17.4991.CrossRefPubMedPubMedCentralGoogle Scholar
- 23.Liu Y, Wang X, Liu Y, Di X. Thermosensitive in situ gel based on solid dispersion for rectal delivery of ibuprofen. AAPS PharmSciTech. 2017; https://doi.org/10.1208/s12249-017-0839-5.
- 25.Tamilvanan S, Sa B. In vitro and in vivo evaluation of single-unit commercial conventional tablet and sustained-release capsules compared with multiple-unit polystyrene microparticle dosage forms of ibuprofen. AAPS PharmSciTech. 2006;7(3):E126–E34. https://doi.org/10.1208/pt070372.CrossRefPubMedCentralGoogle Scholar
- 26.International A. Official methods of analysis of AOAC International. Official methods of analysis of AOAC International. 1995;Volume II.Google Scholar
- 31.Sharif HR, Williams PA, Sharif MK, Abbas S, Majeed H, Masamba KG, et al. Current progress in the utilization of native and modified legume proteins as emulsifiers and encapsulants—a review. Food Hydrocoll. 2017; https://doi.org/10.1016/j.foodhyd.2017.01.002.
- 33.Nielsen PM, Petersen D, Dambmann C. Improved method for determining food protein degree of hydrolysis. J Food Sci. 2001;66(5):642–6. https://doi.org/10.1111/j.1365-2621.2001.tb04614.x.CrossRefGoogle Scholar
- 48.Duarte I, Temtem M, Gil M, Gaspar F. Overcoming poor bioavailability through amorphous solid dispersions. Ind Pharm. 2011;30:4–6.Google Scholar