Nanomedicine-based combination of gambogic acid and retinoic acid chlorochalcone for enhanced anticancer efficacy in osteosarcoma

Biomed Pharmacother. 2016 Oct:83:79-84. doi: 10.1016/j.biopha.2016.06.001. Epub 2016 Jun 23.

Abstract

In this study, gambogic acid (GA) and retinoic acid chlorochalcone (RACC) co-loaded glycol chitosan nanoparticle was successfully developed and studied for its therapeutic efficacy against osteosarcoma cancer cells. The GA/RACC loaded glycol chitosan nanoparticles (RGNP) was nanosized and exhibited a controlled release of drug in either pH 7.4 and pH 5.0. Owing to the strong positive charge on the RGNP surface, efficiency cellular uptake was observed in cancer cells. Moreover, a synergistic combination of GA and RACC were effectively suppressed the tumor growth progression. The half maximal inhibitory concentration (IC50) values in MG63 cells were 0.89μg/ml and 0.35μg/ml for GA and RGNP after 24h. The results clearly suggest the synergist effect of GA and RACC in effectively inhibiting the cancer cell proliferation. The RGNP as expected induced a remarkably higher apoptosis of cancer cells with ∼28%. Overall, combination of GA and RACC encapsulated in a nanocarrier could be an effective strategy to treat osteosarcoma. Future studies will focus on the in vivo evaluation of GA/RACC-loaded polymeric nanoparticles.

Keywords: Apoptosis; Gambogic acid; Nanoparticles; Osteosarcoma; Retinoic acid chlorochalcone.

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cyclohexanones / chemistry
  • Cyclohexanones / pharmacology
  • Cyclohexanones / therapeutic use*
  • Drug Liberation
  • Endocytosis / drug effects
  • Humans
  • Kinetics
  • Nanomedicine / methods*
  • Nanoparticles / chemistry
  • Nanoparticles / ultrastructure
  • Osteosarcoma / drug therapy*
  • Osteosarcoma / pathology
  • Treatment Outcome
  • Tretinoin / analogs & derivatives*
  • Tretinoin / chemistry
  • Tretinoin / pharmacology
  • Tretinoin / therapeutic use
  • Xanthones / chemistry
  • Xanthones / pharmacology
  • Xanthones / therapeutic use*

Substances

  • Antineoplastic Agents
  • Cyclohexanones
  • Xanthones
  • retinoic acid chlorochalcone
  • Tretinoin
  • gambogic acid