253) In the in vitro experiments, an IC₅₀ of 5.69 µg/mL has been achieved for 5-FU loaded PLGA-1, 3-diaminopropane-folic acid nanoparticles on HT-29 cancer cells and is significantly lower than that of 5-FU and 5-FU loaded PLGA nanoparticles which only have an IC₅₀ of 22.9 and 14.17 µg/mL, respectively. |
PMID:24437926 DOI:10.3109/10717544.2013.875603 |
2015 Drug delivery |
* Targeted delivery of 5-fluorouracil to HT-29 cells using high efficient folic acid-conjugated nanoparticles. |
- The incorporation of a high percentage of targeting molecules into drug delivery system is one of the important methods for improving efficacy of targeting therapeutic drugs to cancer cells. PLGA-based drug delivery carriers with folic acid (FA) as targeting molecule have a low targeting efficiency due to a low FA conjugation ratio. In this work, we fabricated a FA-conjugated PLGA system using a crosslinker 1, 3-diaminopropane and have achieved a high conjugation ratio of 46.7% (mol/mol). The as-prepared PLGA-based biomaterial was used to encapsulate therapeutic drug 5-fluorouracil (5-FU) into nanoparticles. In the in vitro experiments, an IC₅₀ of 5.69 µg/mL has been achieved for 5-FU loaded PLGA-1, 3-diaminopropane-folic acid nanoparticles on HT-29 cancer cells and is significantly lower than that of 5-FU and 5-FU loaded PLGA nanoparticles which only have an IC₅₀ of 22.9 and 14.17 µg/mL, respectively. The fluorescent microscopy images showed that nanoparticles with FA are largely taken up by HT-29 cancer cells and the targeting nanoparticles have more affinity to cancer cells than the pure drugs and untreated nanoparticles. Therefore, the 1, 3-diaminopropane can facilitate the conjugation of FA to PLGA to form a novel polymer and 5-FU loaded PLGA-1, 3-diaminopropane-folic acid nanoparticles can be a highly efficient system for specific delivery of drugs to cancer cells. |
(1)29 and | (20)4 treatment | (39)2 (FA) | (58)2 from |
(2)15 *null* | (21)3 (AA) | (40)2 (PA) | (59)2 hydrolysis |
(3)11 in | (22)3 (ALA) | (41)2 (PLGA) | (60)2 interactions |
(4)10 phenethyl | (23)3 (GABA) | (42)2 (PLGA), | (61)2 may |
(5)10 phosphatase | (24)3 (NEFA) | (43)2 (SA) | (62)2 nanoparticles |
(6)9 is | (25)3 changes | (44)2 (SLA) | (63)2 peptide |
(7)8 was | (26)3 decarboxylase | (45)2 (TA) | (64)2 proteins |
(8)6 (HA) | (27)3 etching | (46)2 (TCA) | (65)2 racemization |
(9)6 reactive | (28)3 levels | (47)2 A | (66)2 ratio |
(10)5 as | (29)3 metabolism | (48)2 BSA | (67)2 residues |
(11)5 bacteria | (30)3 on | (49)2 Ig-superfamily | (68)2 substances |
(12)5 group | (31)3 protein | (50)2 Schiff | (69)2 suppressive |
(13)5 or | (32)3 sequence | (51)2 biosynthesis | (70)2 synthetase |
(14)5 synthesis | (33)3 sequences | (52)2 by | (71)2 the |
(15)5 to | (34)3 status | (53)2 changes, | (72)2 therapy |
(16)4 binding | (35)3 were | (54)2 composition | (73)2 vitamin |
(17)4 derivatives | (36)2 (DHA) | (55)2 contents | |
(18)4 for | (37)2 (EDTA) | (56)2 cycle | |
(19)4 solution | (38)2 (EPA) | (57)2 extract |
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