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

Abstract

BLG (beta-lactoglobulin) and CBLG (cationic BLG developed by our lab) were evaluated as potential nutraceutical/drug carriers. The cationic corona conferred CBLG with superior integrity and drug retention under gastrointestinal conditions, at most 40-fold higher mucoadhesion, up to 30-fold greater transepithelial permeation and, at most 285% higher cellular uptake, compared to BLG. Furthermore, the more hydrophilic CBLG species exhibited better mucoadhesion, while the more hydrophobic one exhibited higher cellular uptake. Intriguingly, protein molecules were more cytotoxic and exhibited up to 175% higher tight junction-opening capacity than did protein nanoparticles, whereas the nanoparticles displayed up to 770% higher mucoadhesion, greater transepithelial permeation and elevated cellular uptake. Finally, all these surface properties and performances were significantly altered as CBLG bound to serum proteins. Possible mechanisms underlying these findings are discussed in detail. This research sheds some light on the development of protein-based nanoencapsulants and their performance upon oral administration.

β-Lactoglobulin Influences Human Immunity and Promotes Cell Proliferation

“…Currently, developing an efficient method for drug delivery, such as nanoparticles, is crucial and urgent. It is proven that LG nanotransporters do not impair digestion; yet, it can successfully transport functional proteins and even enhance a compound's bioavailability [59, 60]. Our study directly demonstrated the mechanism of cellular LG transportation.…”

Engineered β-Lactoglobulin Produced in E. coli: Purification, Biophysical and Structural Characterisation

“…Bovine β-lactoglobulin (BlgB) is a small protein (18.3 kDa) belonging to the lipocalin family. Due to BlgB ability to bind different classes of bioactive compounds, its application as a nutrients nanotransporter or drug carrier is currently an object of intensive studies [ 1 – 5 ]. Most of them are performed with commercially available natural lactoglobulin, but the use of recombinant protein seems to be a better alternative.…”

Interactions of salivary mucins and saliva with food proteins: a review

“…Broadly, neutral and negatively charged emulsions undergo reversible depletion flocculation whereas cationic emulsions show irreversible associative electrostatic interactions with mucin and salivary salts. Similarly, Teng et al (2016) found that cationic polymers interact readily with mucin and exhibited better mucoadhesion properties than unmodified BLG. Moreover, Singh and Ye (2013) showed depletion flocculation of a BLG-stabilized emulsion (20 wt% soybean oil, 1.0 wt% BLG) when mixed with an artificial saliva composition containing PGM.…”