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Folate-tethered emulsion for the target delivery of retinoids to cancer cells

Title
Folate-tethered emulsion for the target delivery of retinoids to cancer cells
Author
김진기
Keywords
folic acid; folate receptor; all-trans retinoic acid; folate-tethered emulsion; ACUTE PROMYELOCYTIC LEUKEMIA; IN-VITRO; DRUG-DELIVERY; LIPOSOMAL DOXORUBICIN; BINDING-PROTEIN; KB CELLS; RECEPTOR; ACID; FORMULATION; VIVO
Issue Date
2008-08
Publisher
ELSEVIER SCIENCE BV
Citation
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, v. 68, No. 3, Page. 618-625
Abstract
Folic acid, conjugated to poly(ethylene glycol)-distearoylphosphatidylethanolamine (folate-PEG-DSPE), was used to target emulsions of all-trans retinoic acid (ATRA) to folate receptor-overexpressing tumor cells. Two kinds of ATRA-incorporated folate-tethered emulsions (ATRA-FTE2000/3400) were prepared using soybean oil, egg phosphatidylcholine and folate-PEG-DSPE with different PEG length. As a control, ATRA-incorporated non-tethered emulsion (ATRA-NTE) was prepared by using PEG2000-DSPE without folate instead of using folate-PEG-DSPE. The mean particle diameters of ATRA-FTE2000/3400 were about 100–130 nm. The cellular uptake in KB cells of fluorescence-labeled ATRA-FTE3400 was determined with HPLC (for ATRA) and confocal microscopy (for lipid emulsion). The growth inhibitory activity of ATRA was evaluated by MTT assay. The folate ligands in emulsion increased the cellular uptake of ATRA about 3-fold and 1.6-fold in ATRA-FTE3400 and ATRA-FTE2000, respectively. Growth inhibitory activity of ATRA-FTE3400 in KB cells was higher than that of ATRA-NTE at the same dose. Whereas the growth inhibitory effect in MCF-7 cells of ATRA was similar between ATRA-NTE and ATRA-FTE3400. The addition of free folate significantly reduced the uptake of ATRA regardless of the length of PEG attached to folate. Folate-tethered lipid emulsion showed effective and selective delivery to the folate receptor-abundant carcinomas, suggesting a potential for targeted delivery of anticancer agents.
URI
https://www.sciencedirect.com/science/article/pii/S0939641107002949http://repository.hanyang.ac.kr/handle/20.500.11754/80690
ISSN
0939-6411
DOI
10.1016/j.ejpb.2007.08.010
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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