Synthesis and evaluation of a hematoporphyrin derivative in a folate receptor-targeted solid-lipid nanoparticle formulation.
Anticancer Res
; 24(1): 161-5, 2004.
Article
in En
| MEDLINE
| ID: mdl-15015592
ABSTRACT
PURPOSE:
This study was aimed at the synthesis, formulation and in vitro evaluation of folate receptor (FR)-targeted solid-lipid nanoparticles (SLNs) as a carrier for a lipophilic derivative of the photosensitizer hematoporphyrin (Hp), in FR-overexpressing tumor cells. MATERIALS ANDMETHODS:
FR-targeted hematoporphyrin-stearylamine (HpSa) SLN composed of TrioleinEgg-phosphatidylcholine (EPC)Tween-80 (T-80) (642510), with 0.5 mole % of folate-polyethyleneglycol-cholesterol (FPC) or polyethyleneglycol-distearoylphosphatidylethanolamine (PEG-DSPE), were prepared by ethanol injection method. Stability of the SLN was monitored by changes in particle size at 4 degrees C and drug retention at various time points. Cellular uptake and IC50 values of the FR-targeted formulations were determined in vitro in the FR (+) KB cells.RESULTS:
Stable targeted SLNs were prepared by ethanol injection encapsulating greater than 95 percent of 5 mole % of HpSa, having a mean diameter < 200 nm. In vitro cytotoxicity assay on the FR-targeted SLN gave IC50 of 1.57 microM in KB cells and non-targeted SLNs gave an IC50 of 5.17 microM. FR selectivity was confirmed by fluorescence microscopy.CONCLUSION:
FR-targeted SLNs incorporating the lipophilic drug HpSa were capable of specific receptor binding in cultured KB cells, which warrants further investigation.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Carrier Proteins
/
Receptors, Cell Surface
/
Amines
/
Hematoporphyrins
Limits:
Humans
Language:
En
Journal:
Anticancer Res
Year:
2004
Document type:
Article
Affiliation country:
United States