Synthesis of calcium phosphate-binding liposome for drug delivery

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4148-50. doi: 10.1016/j.bmcl.2009.05.117. Epub 2009 Jun 10.


Metastatic bone disease is often associated with bone pain, pathologic fractures, and nerve compression syndromes. Effective therapies to inhibit the progression of bone metastases would have important clinical benefits. Therefore, we developed a novel calcium phosphate-binding liposome for a bone-targeting drug delivery system. We synthesized a novel amphipathic molecule bearing a bisphosphonate (BP) head group to recognize and bind to hydroxyapatite (HA). We demonstrated that the liposomes having BP moieties show high affinity for HA. Doxorubicin-loaded liposomes adsorbed on the surface of HA significantly reduce the number of viable human osteosarcoma MG63 cells. This shows that the liposomes can be excellent carriers for anticancer drugs because they specifically target bone tissue. This calcium phosphate-binding liposome system could be used with many drugs for bone-related diseases such as osteoporosis, rheumatoid arthritis, and multiple myeloma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacology
  • Arthritis, Rheumatoid / drug therapy
  • Bone Neoplasms / drug therapy
  • Bone and Bones / drug effects
  • Calcium Phosphates / chemistry*
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical / methods
  • Doxorubicin / pharmacology
  • Drug Delivery Systems
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Humans
  • Liposomes / chemistry*
  • Multiple Myeloma / drug therapy
  • Neoplasm Metastasis
  • Osteoporosis / drug therapy
  • Protein Binding


  • Antineoplastic Agents
  • Calcium Phosphates
  • Liposomes
  • Doxorubicin
  • calcium phosphate