[The inhibitive effects of 5-fluorouracil-loaded polylactic acid nanoparticles on human Tenon's capsule fibroblast in vitro].
OBJECTIVE
To investigate the inhibitive effects of 5-fluorouracil-loaded polylactic acid nanoparticles (5-FU-PLA-NPs) on human Tenon's capsule fibroblasts in vitro.


METHODS
This paper was experimental study. MTT assay was performed to estimate the effects of 0.1 mg/L, 1.0 mg/L, 10.0 mg/L, 100.0 mg/L, 1000.0 mg/L unloaded polylactic acid nanoparticles (PLA-NPs) on fibroblasts proliferation on 48 h, 72 h. MTT assay was performed to estimate the effects of 0.1 mg/L, 1.0 mg/L, 10.0 mg/L, 100.0 mg/L, 1000.0 mg/L original 5-FU and 5-FU-PLA-NPs on fibroblasts' proliferation on 7 consecutive days respectively. The inhibitory rate of the two drugs against the fibroblasts was calculated. Cells were exposed to 100 mg/L original 5-FU and 5-FU-PLA-NPs respectively for 7 days. Semi-quantitative RT-PCR was used to observe the mRNA expression of type III procollagen at the 1st day, 5th day and 7th day.


RESULTS
PLA-NPs had no cytotoxicity on the fibroblasts. Both 5-FU-PLA-NPs and original 5-FU could inhibit the proliferation of the fibroblasts and make the expression of type III procollagen mRNA lower in dose-dependent and time-dependent manner. The inhibitive effect of original 5-FU was more effective than 5-FU-PLA-NPs in the initial period, but the inhibitive effect of 5-FU-PLA-NPs was more effective than original 5-FU in long time.


CONCLUSIONS
PLA has good biocompatibility and safety, and can be used as a carrier of ophthalmic drugs. 5-FU-PLA-NPs shows slow-releasing function. 5-FU-PLA-NPs can be proposed as a potential controlled and targeted ophthalmic delivery system for the treatment of antifibrosis after glaucoma filtering surgery.
Lan
Yu-Qing
YQ
Department of Ophthalmology, Second Hospital Affiliated to Sun Yatsun University, Guangzhou 510020, China. lyqglp@163.com
Song
Xin
X
Xiao
Jian-Hui
JH
Zhuo
Ye-Hong
YH
Guo
Hui
H
Zhang
Chi
C
Huang
Kai-Hong
KH
D049109:Cell Proliferation; D002478:Cells, Cultured; D005123:Eye / Q000166:cytology; D005205:Fascia / Q000166:cytology / Q000187:drug effects*; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D005472:Fluorouracil / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D019344:Lactic Acid; D053758:Nanoparticles; D011091:Polyesters; D011108:Polymers
D011091:Polyesters; D011108:Polymers; D019344:Lactic Acid; C033616:poly(lactide); D005472:Fluorouracil