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Merck

Development of novel nanoparticle for bone cancer.

Journal of biomedical nanotechnology (2014-05-09)
Beatriz Ferreira de Carvalho Patricio, Marta de Souza Albernaz, Michelle Alvares Sarcinelli, Samira Marques de Carvalho, Ralph Santos-Oliveira, Gilberto Weissmüller
ABSTRACT

Bone metastasis is responsible for up to 99% of bone tumors. As no cure has yet to be discovered, available treatments simply strive to improve quality of life. One of such treatments is the use of EDTMP (ethylenediamine-tetramethylenephosphonic acid) labeled with Samarium-153, which has been shown to improve survival in 70-80% of patients treated. A major disadvantage of this radiopharmaceutical is its superficial delivery, resulting in the need for multiple doses. The current work describes novel polymeric nanoparticles of EDTMP and evaluation of their biodistribution in vivo. Nanoparticles were prepared using a double emulsion-solvent evaporation method and characterized by AFM (atomic force microscopy). Nanoparticles (200-500 nm) were then labeled with Technetium-99m for biodistribution analysis in healthy Wistar rats. Polymeric nanoparticles of EDTMP were observed to accumulate at bone tissue for long periods of time (150 min), resulting in prolonged release of EDTMP at the target site. This finding suggests that this novel pharmaceutical formulation of EDTMP provides better targeted delivery than free EDTMP and may be a more optimal treatment for management of bone metastasis pain.

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