Formulation, Characterization and Evaluation of Curcumin-Loaded PLGA Nanospheres for Cancer Therapy

Anticancer Res. 2009 Oct;29(10):3867-75.

Abstract

Background: Among the potent anticancer agents, curcumin has been found to be very efficacious against many different types of cancer cells. However, the major disadvantage associated with the use of curcumin is its low systemic bioavailability when administered orally due to its poor aqueous solubility. Our present work investigated the efficiency of encapsulation of curcumin in poly (lactic-coglycolic acid) (PLGA) nanospheres using solid/oil/water emulsion solvent evaporation method.

Materials and methods: The nanospheres were formulated and then characterized for percent yield, encapsulation efficiency, surface morphology, particle size, drug distribution studies, drug polymer interaction studies and in vitro drug release profiles.

Results: Our studies showed the successful formation of smooth and spherical curcumin-loaded PLGA nanospheres, with an encapsulation efficiency of 90.88+/-0.14%. The particle size distribution showed a range of 35 nm to 100 nm, with the mean particle size being 45 nm. Evaluation of these curcumin-loaded nanospheres was carried out in prostate cancer cell lines. Results showed robust intracellular uptake of the nanospheres in the cells. Cell viability studies revealed that the curcumin-loaded nanospheres were able to exert a more pronounced effect on the cancer cells as compared to free curcumin.

Conclusion: Our studies achieved successful formulation of curcumin loaded PLGA nanospheres, thus indicating that nanoparticle-based formulation of curcumin has high potential as an adjuvant therapy for clinical application in prostate cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Calorimetry, Differential Scanning
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Curcumin / administration & dosage*
  • Curcumin / chemistry*
  • Curcumin / pharmacokinetics
  • Drug Delivery Systems / methods*
  • Humans
  • Lactic Acid / administration & dosage*
  • Lactic Acid / chemistry
  • Lactic Acid / pharmacokinetics
  • Male
  • Microscopy, Confocal
  • NF-kappa B / metabolism
  • Nanospheres / administration & dosage*
  • Nanospheres / chemistry*
  • Particle Size
  • Polyglycolic Acid / administration & dosage*
  • Polyglycolic Acid / chemistry
  • Polyglycolic Acid / pharmacokinetics
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / pathology

Substances

  • Antineoplastic Agents
  • NF-kappa B
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Curcumin