Folate-functionalized nanoparticles for controlled ergosta-4,6,8(14),22-tetraen-3-one delivery

Add time:07/30/2019    Source:sciencedirect.com

To improve the therapeutic effect of Ergosta-4,6,8(14),22-tetraen-3-one (cas 19254-69-4) (ergone), a folate–decorated ergone–bovine serum albumin nanoparticles (abbreviated FA–ergone–BSANPs) was prepared. The properties were extensively studied by Zetasizer Nano Particle Size Analyzer and TEM, which indicated the prepared nanoparticles were spherical in shape and uniform in size with a zeta potential of −23.8 mV. The drug-loading capacity also has been determined with drug loading content of 2.73% and encapsulation efficiency of 61.8%. In vitro release studies proved the much slow drug release from the nanoparticles during circulating in the blood stream and the increase of drug release at the target sites. The FA–ergone–BSANPs showed enhanced cellular uptake, increased targeting capacity, and increased cytotoxicity against KB cells over-expressing folate receptor (FR), which indicated that its potent cell-killing activity is specific for cells that express the FR. In vivo experiment also confirmed that FA–ergone–BSANPs represent a FR-targeted chemotherapeutic that can produce potent activity against FR-positive tumors. In conclusion, this report has a great significance in pharmacology and clinical medicine as well as methodology. Further detailed dose-optimization studies will be required for better understanding in vivo pharmacokinetic and bio-distribution behaviors.

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