188) 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. |
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)22 therapeutic | (17)3 mutation | (33)2 approaches | (49)2 information |
(2)11 and | (18)3 paradigm | (34)2 autosomal | (50)2 inhibitors |
(3)8 mechanism | (19)3 role | (35)2 candidate | (51)2 learning |
(4)8 method | (20)3 strain | (36)2 cardiac | (52)2 modulators |
(5)7 approach | (21)3 target | (37)2 clinical | (53)2 object |
(6)7 mutations | (22)3 targeted | (38)2 compounds | (54)2 oral |
(7)6 therapies | (23)3 targets | (39)2 data | (55)2 polymer |
(8)5 technique | (24)3 treatment | (40)2 described | (56)2 potent |
(9)4 strategies | (25)3 type | (41)2 dual | (57)2 prognostic |
(10)4 strategy | (26)3 words | (42)2 electroporation | (58)2 putative |
(11)4 surgical | (27)2 *null* | (43)2 finding | (59)2 recombinants |
(12)3 antibacterial | (28)2 anti-tumor | (44)2 findings | (60)2 results |
(13)3 drug | (29)2 antibiotic | (45)2 form | (61)2 therapeutical |
(14)3 homozygous | (30)2 anticancer | (46)2 genetic | (62)2 titanium |
(15)3 insights | (31)2 application | (47)2 imaging | (63)2 treatments |
(16)3 mechanisms | (32)2 applications | (48)2 in |
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