Characterization and biodistribution of bevacizumab TPGS-based nanomicelles: Preliminary studies.

TESAN F.; CERQUEIRA-COUTINHO C. ; SALGUEIRO J.; DE SOUZA ALBERNAZ M. ; PINTO S.R.; REZENDE DOS REIS S.R.; BERNARDES E.S.; CHIAPPETTA D.A.; ZUBILLAGA M.; SANTOS-OLIVEIRA R.

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY

EDITIONS SANTE

Año: 2016 vol. 36 p. 95 - 98

1773-2247

Bevacizumab is an FDA approved monoclonal antibody (anti VEGF) indicated in many cancers, mostly metastatic ones. D-a-tocopheryl polyethylene glycol succinate (TPGS) is the water-soluble form of vitamin E which usually forms micelles. This work aims to report preliminary results of the biodistribution of a TPGS based nano-micelle delivery system for bevacizumab in a gastric cancer xenograftmodel. Evaluation of the biodistribution of micelles/bevacizumab-99mTc was performed in Balb/c nude mice carrying MKN45 cell line xenograft. The nano-radiopharmaceutical (3.7 MBq/0.2 mL) was administered intraocularly and biodistribution was assesed 1 h post administration. The activity in each organand blood was determined by a gamma counter. Mean size was 10 ± 1 nm for pure TPGS and 11 ± 1 nm for bevacizumab-TPGS respectively. Biodistribution showed that the highest uptake was found in both lungs and liver. Kidneys had also an important uptake. The tumor accumulated moderate to low radiolabelednanomicelles, nevertheless tumor/blood ratio was very high.These preliminary results may help as a start point to continue evaluating the potential of radiolabeled bevacizumab-TPGS based nanomicelles to be used as a theranostic agent.