Folate-functionalized nanoparticles for controlled ergosta-4,6,8(14),22-tetraen-3-one delivery.
Int J Pharm
; 441(1-2): 1-8, 2013 Jan 30.
Article
en En
| MEDLINE
| ID: mdl-23262423
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.
Texto completo:
1
Colección:
01-internacional
Asunto principal:
Colestenonas
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Sistemas de Liberación de Medicamentos
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Nanopartículas
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Antineoplásicos
Límite:
Animals
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Female
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Humans
Idioma:
En
Revista:
Int J Pharm
Año:
2013
Tipo del documento:
Article
País de afiliación:
China