title: 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.
authors.affiliation: Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States.
authors.forename: Zi
authors.initials: Z
authors.lastname: Teng
authors.affiliation: Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States; Department of Nutritional Sciences, University of Connecticut, 3624 Horsebarn Road Ext., Unit 4017, Storrs, CT 06269, United States.
authors.forename: Yangchao
authors.initials: Y
authors.lastname: Luo
authors.affiliation: Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States.
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States. Electronic address: wangqin@umd.edu.
authors.forename: Qin
authors.initials: Q
authors.lastname: Wang
mesh_terms: D001682:Biological Availability; D018938:Caco-2 Cells; D002412:Cations; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D004847:Epithelial Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007421:Intestine, Small / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D007782:Lactoglobulins / Q000737:chemistry / Q000493:pharmacokinetics*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D013499:Surface Properties
chemical_list: D002412:Cations; D004337:Drug Carriers; D007782:Lactoglobulins
keywords: Beta-lactoglobulin (BLG); Cationic polymers; Delivery systems; Encapsulation; Mucoadhesion; Nanoparticles; Surface properties