Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 441, Issue 1-2, Pages 1-8Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2012.12.018
Keywords
Ergosta-4,6,8(14),22-tetraen-3-one (ergone); Nanoparticles; Folate receptor; Targeted therapeutics; Slow release capacity; Anticancer
Categories
Funding
- National Natural Science Foundation of China [81001622]
- Project of As a Major New Drug to Create a Major National Science and Technology Special [20082X09101-2-016]
- Doctoral Initiate Foundation of Xi'an University of Arts and Science [90506]
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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. (C) 2012 Elsevier B. V. All rights reserved.
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