PMID- 23135527
OWN - NLM
STAT- MEDLINE
DCOM- 20130328
LR  - 20181202
IS  - 1432-0843 (Electronic)
IS  - 0344-5704 (Linking)
VI  - 71
IP  - 2
DP  - 2013 Feb
TI  - Pharmacokinetic study and effectiveness evaluation of slow-release 
      PLGA-5-fluorouracil microsphere.
PG  - 351-9
LID - 10.1007/s00280-012-2016-6 [doi]
AB  - PURPOSE: The aim was to develop a slow-release poly-lactic-co-glycolic acid 
      (PLGA)-5-fluorouracil microsphere, study the pharmacokinetic characteristics as 
      well as to evaluate the effectiveness and safety of this preparation on 
      colorectal tumor in vivo. METHODS: The PLGA-5-fluorouracil microsphere was 
      prepared based on a spray-drying method, and the drug loading of 5-fluorouracil 
      (the percentage of 5-fluorouracil content in the whole microsphere), in vitro 
      5-fluorouracil release profile and pharmacokinetic characteristics were carried 
      out through high-performance liquid chromatography. The inhibiting effect on 
      tumor growth and safety was examined using in vivo subcutaneously (s.c.) 
      inoculated colorectal tumor models of nude mice. RESULTS: The size of the 
      microsphere was less than 100 mum, drug loading was 20 % and drug release time 
      lasted as long as 30 days. Slow-release PLGA-5-fluorouracil microsphere had 
      longer half-life time (t (1/2)), larger apparent volume of distribution (V ( d )) 
      and smaller area under the curve (AUC) compared with 5-fluorouracil. 
      PLGA-5-fluorouracil microsphere significantly restrained tumor growth and this 
      effect correlated with decreased expression of vascular endothelial growth factor 
      in tumor cells. Body weight measurement and blood analysis did not suggest 
      significant adverse effects on the mice during the study. CONCLUSIONS: The 
      slow-release PLGA-5-fluorouracil microsphere developed here was suitable for 
      regional use; it has pharmacokinetic advantages and appears safe and effective in 
      controlling the tumor growth. This preparation shows promise in reducing local 
      recurrence of colorectal cancer after resection, but needs further investigation.
FAU - Li, Jingquan
AU  - Li J
AD  - General Surgery Department, The 309th Hospital of the PLA, No A17, Heishanhu 
      road, Haidian district, Beijing 100091, China. jingquanli2012@163.com
FAU - Pu, Yongdong
AU  - Pu Y
FAU - Wang, Shiliang
AU  - Wang S
FAU - Ding, Manzhi
AU  - Ding M
FAU - Chen, Dianliang
AU  - Chen D
FAU - Zhu, Mudan
AU  - Zhu M
LA  - eng
PT  - Journal Article
DEP - 20121108
PL  - Germany
TA  - Cancer Chemother Pharmacol
JT  - Cancer chemotherapy and pharmacology
JID - 7806519
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Vascular Endothelial Growth Factor A)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - U3P01618RT (Fluorouracil)
SB  - IM
MH  - Animals
MH  - Delayed-Action Preparations
MH  - Female
MH  - Fluorouracil/*administration & dosage/adverse 
      effects/*pharmacokinetics/therapeutic use
MH  - HCT116 Cells
MH  - Humans
MH  - Immunohistochemistry
MH  - Lactic Acid/*administration & dosage
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - *Microspheres
MH  - Polyglycolic Acid/*administration & dosage
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Vascular Endothelial Growth Factor A/analysis
EDAT- 2012/11/09 06:00
MHDA- 2013/03/30 06:00
CRDT- 2012/11/09 06:00
PHST- 2012/07/25 00:00 [received]
PHST- 2012/10/21 00:00 [accepted]
PHST- 2012/11/09 06:00 [entrez]
PHST- 2012/11/09 06:00 [pubmed]
PHST- 2013/03/30 06:00 [medline]
AID - 10.1007/s00280-012-2016-6 [doi]
PST - ppublish
SO  - Cancer Chemother Pharmacol. 2013 Feb;71(2):351-9. doi: 10.1007/s00280-012-2016-6. 
      Epub 2012 Nov 8.