Abstract
BackgroundThe synthesis of bioactive nanoparticles with precise molecular level control is a major challenge in bionanotechnology. Understanding the nature of the interactions between the active components and transport biomaterials is thus essential for the rational formulation of bio-nanocarriers. The current study presents a single molecule of bovine serum albumin (BSA), lysozyme (Lys), or myoglobin (Mb) used to load hydrophobic drugs such as quercetin (Q) and other flavonoids.ResultsInduced by dimethyl sulfoxide (DMSO), BSA, Lys, and Mb formed spherical nanocarriers with sizes less than 70 nm. After loading Q, the size was further reduced by 30%. The adsorption of Q on protein is mainly hydrophobic, and is related to the synergy of Trp residues with the molecular environment of the proteins. Seven Q molecules could be entrapped by one Lys molecule, 9 by one Mb, and 11 by one BSA. The controlled releasing measurements indicate that these bioactive nanoparticles have long-term antioxidant protection effects on the activity of Q in both acidic and neutral conditions. The antioxidant activity evaluation indicates that the activity of Q is not hindered by the formation of protein nanoparticles. Other flavonoids, such as kaempferol and rutin, were also investigated.ConclusionsBSA exhibits the most remarkable abilities of loading, controlled release, and antioxidant protection of active drugs, indicating that such type of bionanoparticles is very promising in the field of bionanotechnology.
Highlights
The synthesis of bioactive nanoparticles with precise molecular level control is a major challenge in bionanotechnology
Scanning transmission electron microscopy (STEM) micrographs show that the native bovine serum albumin (BSA), Lys, and Mb molecules were cross-linked, and formed loose aggregates (Figures 2A, A’, and A’’)
After adding 1.5 × 10-4 mol/L Q solution prepared with 10% dimethyl sulfoxide (DMSO), spherical and compact Q loaded protein (BSA, Lys, or Mb) nanoparticles (D-BSA-Q, D-Lys-Q, or D-Mb-Q) occurred (Figures 2C, C’, and 2C’’), but their size decreased compared with the system without Q, the D-BSA-Q aggregates, which markedly decreased in size
Summary
The synthesis of bioactive nanoparticles with precise molecular level control is a major challenge in bionanotechnology. Nanotoxicology research has indicated that [1] pharmacological properties and the biodegradability, biocompatibility, and nontoxicity should be considered in such new systems Synthetic macromolecules, such as the amphiphilic hyperbranched multiarm copolymers (HPHEEP-star-PPEPs) [2], poly(2ethyl-2-oxazoline)-b-poly(D,L-lactide) [3], and polyethylene glycol [4], are often investigated; replacing these synthetic materials with natural proteins, which are more likely to be accepted by people, has become the focus of many research studies [5,6,7,8,9]. I.e., desolvation with ethanol and solidification with glutaraldehyde, BSA can form nanoparticles [7]. The molecular sizes obtained from such a process are often larger than 70 nm; such particles cannot be used to entrap hydrophobic drugs, thereby restricting the development of bio-nanocarriers
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