Magnolol-Loaded Core–Shell Hydrogel Nanoparticles: Drug Release, Intracellular Uptake, and Controlled Cytotoxicity for the Inhibition of Migration of Vascular Smooth Muscle Cells

Abstract

Encapsulation and release behavior of a water-insoluble drug, magnolol, using a core-shell polysaccharide-based nanoparticle, manipulating the cellular internalization and controlled cytotoxic effect of magnolol-loaded nanoparticles over the A10 vascular smooth muscle cells (VSMCs) was reported. A magnolol-polyvinylpyrrolidone (PVP) core phase was prepared, followed encapsulating by an amphiphilic carboxymethyl-hexanoyl chitosan (CHC) shell to form a magnolol-loaded core-shell hydrogel nanoparticles (termed magnolol-CHC nanoparticles). The resulting magnolol-CHC nanoparticles were employed for evaluation of drug release and controlled cytotoxic inhibition of VSMCs migration in vitro. A sustained release of the magnolol from the nanoparticles was determined. The magnolol-CHC nanoparticles exhibited outstanding cellular uptake efficiency, and under a cytotoxic evaluation, an increased antiproliferative effect and effective inhibition of VSMC migration as a result of efficient intracellular delivery of the encapsulated magnolol in comparison to free magnolol was achieved. We then envision a potential intracellular medication strategy with improved biological and therapeutic efficacy using the magnolol-CHC nanoparticles illustrated in this work.

Magnolol restores the activity of meropenem against NDM-1-producing Escherichia coli by inhibiting the activity of metallo-beta-lactamase

“…Compared with the above inhibitors, magnolol has the advantages of abundant sources and easy preparation 26 , 27 . The high hydrophobicity and low solubility of magnolol may be the major obstacles to its bioavailability and clinical efficacy 28 , 29 . However, we revealed that the concentrations required to restore antimicrobial activity could be achieved in bacteria.…”

Self-assembled polysaccharide nanostructures for controlled-release applications

“…This hyperplasia of intima results in a narrowing of the lumen of the injured blood vessel and eventual re-occlusion of the vessel. Magnolol, 4-allyl-2-(5-allyl-2-hydroxy-phenyl)phenol, a strong antioxidant with approximately 1000 times greater activity than α-tocopherol, has been found to be effective in inhibiting the proliferation of VSMCs [40].…”

“…Conventional liposomal drug carriers were found to have low drug encapsulation efficiency, poor storage stability, rapid clearance from the blood stream, nonspecific uptake by the mononuclear phagocytic system, poor control over release of the drug from the liposome, and rapid drug loss profiles in vivo [40]. To overcome these drawbacks, Wang et al [40] prepared CHC (17, Figure 6)-based nanoparticles containing magnolol and found an increased antiproliferative effect and effective inhibition of VSMC migration (in comparison with free magnolol), as a result of efficient intracellular delivery of the encapsulated magnolol. They prepared a magnolol-polyvinylpyrrolidone core phase and encapsulated it in an amphiphilic CHC shell, to obtain magnolol-loaded core-shell nanoparticles with average hydrodynamic diameters in the range of 235-420 nm.…”

Protein-Protein and Protein-Ligand Docking

“…When heated with strong bases such as lithium carbonate, trisodium phosphate or sodium metasilicate, it generates a precipitate due to the ring opening and subsequent crosslinking of chains. Yen-Jen et al studied its effect as a drug deliverer and intracellular acceptor [40].…”