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

Abstract

To improve the therapeutic effect of ergosta-4,6,8(14),22-tetraen-3-one (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.

• Authors: Xuhua Liang, Yang Sun, Lusha Liu, Xuan Ma, Xiaoyun Hu, Jun Fan, Yingyong Zhao
• Journal: International journal of pharmaceutics (Int J Pharm) Vol. 441 Issue 1-2 Pg. 1-8 (Jan 30 2013) ISSN: 1873-3476 [Electronic] Netherlands
• PMID: 23262423 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier B.V. All rights reserved.

Chemical References

• Antineoplastic Agents
• Cholestenones
• Delayed-Action Preparations
• Folate Receptors, GPI-Anchored
• Serum Albumin, Bovine
• ergosta-4,6,8(14),22-tetraen-3-one

Topics

• Animals
• Antineoplastic Agents (administration & dosage, pharmacokinetics, pharmacology)
• Cholestenones (administration & dosage, pharmacokinetics, pharmacology)
• Delayed-Action Preparations
• Drug Delivery Systems
• Female
• Folate Receptors, GPI-Anchored (metabolism)
• Humans
• KB Cells
• Mice
• Mice, Inbred BALB C
• Nanoparticles
• Particle Size
• Serum Albumin, Bovine (chemistry)
• Tissue Distribution