Self-assembling nanoparticles for the release of bisphosphonates in the treatment of human cancers

摘要

The present invention describe nanocomplexes also called auto-assembling nanoparticles comprising biphosphonates, lipid nanovectors and inorganic nanovectors.;In particular the invention describes zoledronic acid complexed with calcium phosphate base nanoparticles; said particles in their turn mixed with lipidic particles e.g. liposomes.;Said nanocomplexes are useful, and showed to be efficient in vivo, as pharmaceutical formulations of biphosphonates for the treatment or prevention of tumor growth and/or metastasis. Tumors can be solids and/or haematological such as prostate, lung, head/neck, colon, liver, breast, pancreas, kidneys, bladder, male and female urogenital tract, bones, multiple myeloma, primitive and secondary tumors of the central nervous system and lymphomas.

主权项

1. A nanocomplex, which is a self-assembling nanoparticle, comprising a core portion comprising bisphosphonate complexed with an inorganic nanovectors and an outer portion comprising a lipid and a hydrophilic polymer, wherein the outer portion envelopes the core portion to form the nanocomplex and wherein the nanocomplex is stabilized by non-covalent interactions between the core portion and the outer portion and has a mean diameter between 10 nm and 500 nm; wherein the nanocomplex is assembled by first complexing biphosphonate with the inorganic nanovectors to form the core portion and then subsequently contacting the formed core portion with a lipid nanovector comprising the lipid and the hydrophilic polymer, wherein the inorganic nanovectors comprises nanoparticles of a Ca, Mg, Sr or Zn inorganic salt.