Cationic β-Lactoglobulin Nanoparticles as a Bioavailability Enhancer: Protein Characterization and Particle Formation

Abstract

Cationic β-lactoglobulin (CBLG) was developed as a bioavailability enhancer for poorly absorbed bioactives. At most 11 anionic amino acid residues of β-lactoglobulin (BLG) were substituted by ethylenediamine (EDA), resulting in a highly positive surface charge (zeta potential up to 39 mV at pH 7.0) and significantly increased surface hydrophobicity. These changes conferred CBLG with desirable water solubility and improved mucoadhesion by at most 252%, according to quartz crystal microbalance (QCM) study. Furthermore, CBLG inherited the unique resistance to gastric digestion from BLG, while the digestion under simulated intestinal condition was significantly improved. The latter was possibly due to the formation of aspartic acid-EDA conjugates, together with the randomization of protein conformation related with decreased percentage of β-sheet. Compared to BLG, CBLG formed smaller (75-94 nm), more uniform nanoparticles by the acetone-desolvation method. These merits made CBLG a useful material that provides desirable solubility, controlled release, and enhanced absorption to nutraceuticals or drugs.

Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity

“…This corroborates with earlier studies, which have shown similar trend of increasing zeta potential along with increase in liquid lipid concentration (Nayak et al, 2010). In all the formulations, zeta potential was high enough to stabilize the nanoparticles against aggregation (Teng et al, 2013). Addition of either artemether or lumefantrine has no effect on the zeta potential of the nanoparticles.…”

Characterization of resveratrol–milk protein interaction

“…b-Lactoglobulin (BLG) is a 162-residue globular protein, makes up approximately 60% of bovine whey protein (Matalanis et al, 2011;Teng et al, 2013). Because of its flexibility and amphiphilic nature, BLG serves as a natural carrier for various nutrients (Lefèvre and Subirade, 2003;Papiz et al, 1986;Kontopidis et al, 2004).…”

Cationic beta-lactoglobulin nanoparticles as a bioavailability enhancer: Effect of surface properties and size on the transport and delivery in vitro

“…These values were over 15 and 40 times higher than that of BLG nanoparticles (0.254), and they were considerably higher than that achieved by other biopolymers such as chitosan (Chayed & Winnik, 2007). According to our previous report, CBLG molecules also displayed higher mucoadhesion than did BLG (Teng, Li, Luo, Zhang, & Wang, 2013). However, it was noteworthy that the C-EDA and C-P600 nanoparticles showed 770% and 475% higher mucoadhesion than did their constituent molecules, although the former exhibited less positive surface charges than did the latter (Table 1).…”

“…CBLG was synthesized via an EDC-aided coupling reaction, and nanoparticles were prepared with BLG and CBLG by organic solvent desolvation, as previously described (Teng, Li, Luo, Zhang, & Wang, 2013). In brief, the coupling process was initiated by incubating BLG and cationizer (EDA or PEI) at pH 4.75 in the presence of EDC, and it was terminated after 4 h by adding sodium acetate buffer.…”