PMID- 31866565
OWN - NLM
STAT- MEDLINE
DCOM- 20201117
LR  - 20201117
IS  - 1879-0720 (Electronic)
IS  - 0928-0987 (Linking)
VI  - 143
DP  - 2020 Feb 15
TI  - Intratumoral distribution of YSNSG cyclopeptide in a mouse melanoma model using 
      microdialysis.
PG  - 105201
LID - S0928-0987(19)30474-9 [pii]
LID - 10.1016/j.ejps.2019.105201 [doi]
AB  - The YSNSG peptide is a synthetic cyclopeptide targeting alpha(v)beta(3) integrin with 
      antitumor activity. Previous study has determined main pharmacokinetic parameters 
      in plasma and in tissue in healthy animals using microdialysis. First we aim to 
      assess the impact of a 20 mg/kg dosage instead of 10 mg/kg in tumor growth 
      inhibition. Secondly we aim to investigate the YSNSG peptide distribution in two 
      different tumor regions in animals with melanoma. C57BL/6 mice were exposed at 
      Days 8, 10 and 12 after melanoma cells implantation (B16F1) to different dosage 
      of YSNSG peptide or control, respectively (n = 10 per group). Data analysis was 
      performed at D16, 20 and 24 with a Nonlinear Mixed-Effects (NLME) approach. For 
      pharmacokinetic study n = 8 mice (same disease condition) received YSNSG peptide 
      by intravenous after insertion of two microdialysis probes in central peripheral 
      region of tumor, respectively. Plasma and tissue samples were collected during 
      2 h. A non-compartmental analysis was performed to determine main pharmacokinetic 
      parameters. There was a significant tumor growth inhibition in mice receiving 
      20 mg/kg vs Control (p < 0.02). Main plasma parameters were half-life elimination 
      25.8 +/- 8.2 min, volume of distribution 11.9 +/- 0.4 mL, clearance 19.8 +/- 9.4 mL/h 
      and area under the curve 1,173.6 microg.min/mL. Penetration rate of the YSNSG peptide 
      from plasma to tumor tissue were 3.3 +/- 2.1% and 3.4 +/- 2.7% in central and 
      peripheral, respectively. Contrary to subcutaneous distribution in healthy 
      animals the distribution of the YSNSG peptide into tumoral tissue is low but 
      seems non-heterogeneous between central and peripheral tumor region.
CI  - Copyright (c) 2019 Elsevier B.V. All rights reserved.
FAU - Slimano, Florian
AU  - Slimano F
AD  - MEDyC Research Unit, UMR CNRS/URCA n degrees 7369, SFR CAP-Sante, Reims University, 51, 
      rue Cognacq-Jay, 51100 Reims, France; Department of Pharmacy, CHU Reims, Avenue 
      du General Koenig, and Faculty of Pharmacy, Reims University, 51, rue 
      Cognacq-Jay, 51100 Reims, France. Electronic address: 
      florian.slimano@univ-reims.fr.
FAU - Djerada, Zoubir
AU  - Djerada Z
AD  - Department of Pharmacology and Toxicology, CHU Reims, Avenue du General Koenig, 
      51100 Reims, France; EA3801, SFR CAP-Sante, Faculty of Medicine, Reims 
      University, 51, rue Cognacq-Jay, 51100 Reims, France.
FAU - Guerin, Juline
AU  - Guerin J
AD  - MEDyC Research Unit, UMR CNRS/URCA n degrees 7369, SFR CAP-Sante, Reims University, 51, 
      rue Cognacq-Jay, 51100 Reims, France.
FAU - Bellouch, Morad Id
AU  - Bellouch MI
AD  - MEDyC Research Unit, UMR CNRS/URCA n degrees 7369, SFR CAP-Sante, Reims University, 51, 
      rue Cognacq-Jay, 51100 Reims, France.
FAU - Brassart-Pasco, Sylvie
AU  - Brassart-Pasco S
AD  - MEDyC Research Unit, UMR CNRS/URCA n degrees 7369, SFR CAP-Sante, Reims University, 51, 
      rue Cognacq-Jay, 51100 Reims, France.
FAU - Dukic, Sylvain
AU  - Dukic S
AD  - MEDyC Research Unit, UMR CNRS/URCA n degrees 7369, SFR CAP-Sante, Reims University, 51, 
      rue Cognacq-Jay, 51100 Reims, France; Department of Pharmacy, CHU Reims, Avenue 
      du General Koenig, and Faculty of Pharmacy, Reims University, 51, rue 
      Cognacq-Jay, 51100 Reims, France.
LA  - eng
PT  - Journal Article
DEP - 20191219
PL  - Netherlands
TA  - Eur J Pharm Sci
JT  - European journal of pharmaceutical sciences : official journal of the European 
      Federation for Pharmaceutical Sciences
JID - 9317982
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Peptides, Cyclic)
RN  - 0 (YSNSG cyclopeptide)
SB  - IM
MH  - Administration, Intravenous
MH  - Animals
MH  - Antineoplastic Agents/blood/*pharmacokinetics/therapeutic use
MH  - Disease Models, Animal
MH  - Female
MH  - Melanoma/blood/drug therapy/*metabolism/pathology
MH  - Mice, Inbred C57BL
MH  - Microdialysis
MH  - Peptides, Cyclic/blood/*pharmacokinetics/therapeutic use
MH  - Tumor Burden/drug effects
OTO - NOTNLM
OT  - Cyclopeptide
OT  - Integrin antagonist
OT  - Intratumoral distribution
OT  - Melanoma
OT  - Microdialysis
OT  - Pharmacokinetic
OT  - YSNSG
EDAT- 2019/12/24 06:00
MHDA- 2020/11/18 06:00
CRDT- 2019/12/24 06:00
PHST- 2019/08/27 00:00 [received]
PHST- 2019/12/16 00:00 [revised]
PHST- 2019/12/17 00:00 [accepted]
PHST- 2019/12/24 06:00 [pubmed]
PHST- 2020/11/18 06:00 [medline]
PHST- 2019/12/24 06:00 [entrez]
AID - S0928-0987(19)30474-9 [pii]
AID - 10.1016/j.ejps.2019.105201 [doi]
PST - ppublish
SO  - Eur J Pharm Sci. 2020 Feb 15;143:105201. doi: 10.1016/j.ejps.2019.105201. Epub 
      2019 Dec 19.