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2018-11-29T04:34:50Z
2018-11-29T04:34:50Z
2008-08
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, v. 68, No. 3, Page. 618-625
0939-6411
https://www.sciencedirect.com/science/article/pii/S0939641107002949
https://repository.hanyang.ac.kr/handle/20.500.11754/80690
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.
This work is financially supported by the Ministry of Education and Human Resources Development (MOE), the Ministry of Commerce, Industry and Energy (MOCIE) and the Ministry of Labor (MOLAB) through the fostering project of the Lab of Excellency.
en_US
ELSEVIER SCIENCE BV
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
Folate-tethered emulsion for the target delivery of retinoids to cancer cells
Article
3
68
10.1016/j.ejpb.2007.08.010
618-625
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Kim, Sung-Hoon
Kim, Jin-Ki
Lim, Soo-Jeong
Park, Jeong-Sook
Lee, Mi-Kyung
Kim, Chong-Kook
2008212687
E
COLLEGE OF PHARMACY[E]
DEPARTMENT OF PHARMACY
jinkikim