Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy

• Published in: Nano biomedicine and engineering 2014-06, Vol.6 (2), p.47-59
• Main Authors: Chidambaram, Moorthi, Krishnasamy, Kathiresan
• Format: Article
• Language: English
• Subjects: curcumin; piperine; polymeric nanoparticle; quercetin; silibinin
• ISSN: 2150-5578; 2150-5578
• DOI: 10.5101/nbe.v6i2.p47-59

Curcumin, a functional food polyphenol reported to inhibit cancer cell proliferation, invasion, angiogenesis and metastasis through interaction with multiple molecular targets. However, the clinical usefulness of curcumin in the treatment of cancer is limited due to poor solubility in water at acidic and neutral pH, hydrolytic degradation in alkaline pH and metabolism in the liver and intestine, resulting in decreased or absence of therapeutic efficacy. Hence, the present study was aimed to overcome the limitations of curcumin in the treatment of cancer by codelivery of nanosized curcumin and bioenhancer using acid degradable polymeric nanoparticles. Modified nanoprecipitation method was used to prepare void, curcumin-piperine, curcumin-quercetin and curcumin-silibinin encapsulated polymeric nanoparticles. Prepared nanoformulations were evaluated for particle size, polydispersity index, zeta potential, surface morphology, drug content, encapsulation efficiency, drug loading, in vitro release, stability at elevated storage conditions, toxicity on normal liver cells, anticancer activity on various cancer cell lines and on cancer induced rats. Prepared curcumin-bioenhancer encapsulated polymeric nanoparticles were (a) spherical in shape with size 95% release of curcumin and bioenhancers within 45 minutes in gastric fluid; (c) proved non-toxic to normal liver cells; (d) extremely stable at elevated storage conditions; and (e) demonstrated enhanced anticancer activity against various cancer cell lines and mammary cancer in rats than the pure curcumin. Study concludes that the prepared curcumin-bioenhancer encapsulated polymeric nanoformulations significantly overcome the limitations of curcumin in the treatment of cancer and synergistically enhance its anticancer activity. However, out of three polymeric nanoformulations, curcumin-silibinin polymeric nanoformulation showed superior anticancer activity.