Cationic β-lactoglobulin nanoparticles as a bioavailability enhancer: comparison between ethylenediamine and polyethyleneimine as cationizers.
Cationic β-lactoglobulin (CBLG) was synthesized by two strategies: extensive conjugation of ethylenediamine (EDA) and limited cationization with polyethyleneimine (PEI). Both methods provided CBLG with satisfactory water solubility and resistance to peptic digestion. Compared with EDA-derived CBLG (C-EDA), PEI-derived CBLG (C-PEI) exhibited a higher zeta potential (54.2 compared to 32.4mV for C-EDA), which resulted in significantly elevated mucoadhesion (439% and 118% higher than BLG and C-EDA, respectively) in a quartz crystal microbalance (QCM) study. In addition, PEI caused reduced conformational disruption on BLG compared to EDA as evidenced by FTIR measurement. This character, together with the steric hindrance provided by PEI, caused a phenomenal reduction in tryptic digestibility by at least 75% compared to C-EDA. In the presence of aqueous acetone, C-PEI aggregated spontaneously into nanoparticles with average size of 140 nm and narrow size distribution. These merits made C-PEI a useful material that provides desirable solubility and protection for orally administrated nutraceuticals or drugs.
Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States.
Zi
Z
Teng
Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States.
Ying
Y
Li
Institute of Food and Nutraceutical Science, School of Agriculture and Biology, Shanghai Jiao Tong University, Shanghai 200240, China.
Yuge
Y
Niu
School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.
Yuhong
Y
Xu
Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States; Institute of Food and Nutraceutical Science, School of Agriculture and Biology, Shanghai Jiao Tong University, Shanghai 200240, China.
Liangli
L
Yu
Department of Nutrition and Food Science, University of Maryland, 0112 Skinner Building, College Park, MD 20742, United States. Electronic address: wangqin@umd.edu.
Qin
Q
Wang
D001682:Biological Availability; D002412:Cations / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D005029:Ethylenediamines / Q000737:chemistry*; D007782:Lactoglobulins / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D011094:Polyethyleneimine / Q000737:chemistry*; D012995:Solubility
D002412:Cations; D004337:Drug Carriers; D005029:Ethylenediamines; D007782:Lactoglobulins; C031234:ethylenediamine; D011094:Polyethyleneimine
Cationic beta-lactoglobulin (CBLG); Ethylenediamine (EDA); Mucoadhesive properties; Nanoparticles; Polyethyleneimine (PEI); Protein digestion; Secondary structure