Microradiopharmaceutical for Metastatic Melanoma.
Pharm Res
; 34(12): 2922-2930, 2017 Dec.
Article
in En
| MEDLINE
| ID: mdl-29063342
ABSTRACT
PURPOSE:
The purpose of this article was to develop, characterize and test (in vivo) dacarbazine microparticles that may be labeled with 99mTc and Ra-223 for both use diagnostic and therapy of metastatic melanoma.METHODS:
We developed by double emulsion solvent evaporation methodology the microparticle. The characterization has been done using, Dynamic Light Scattering (DLS) and Scanning Electron Microscopy (SEM). The labeling with 99mTc and Ra-223 has been done by the direct labeling process. Also the formulation has been tested pre-clinically using Balb/c mice inducted with melanoma, performing the the biodistribution and planar imaging. Cytotoxicity evaluation was also done in M3 V cell line. In order to understand the safety aspects of the microparticles, microbiological study (endotoxin and sterility) has been done. Finally, planar imaging was performed to evaluate the diagnosing aspect.RESULTS:
The results showed that a 559 nm microparticles was obtained with a spherical shape. The labeling process with 99mTc reached over 90% of efficacy. On the other hand, the labeling process with Ra-223 showed a 70% efficacy. The results in inducted animals demonstrated that the microparticles were able to reach the tumor with a high rate (20%). Also demonstrated a low recognition by the Mononuclear Phagocytic System. The cytotoxicity and the microbiological control, corroborates the safety aspect of these microparticles.CONCLUSION:
The planar image and the possible labeling with Ra-223, corroborates the use as a theragnostic agent for imaging and therapy of Metastatic Melanoma.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Radium
/
Technetium
/
Antineoplastic Agents, Alkylating
/
Dacarbazine
/
Melanoma
Limits:
Animals
Language:
En
Journal:
Pharm Res
Year:
2017
Document type:
Article
Affiliation country:
Brazil
Publication country:
EEUU
/
ESTADOS UNIDOS
/
ESTADOS UNIDOS DA AMERICA
/
EUA
/
UNITED STATES
/
UNITED STATES OF AMERICA
/
US
/
USA