Fabrication of Curcumin Micellar Nanoparticles with Enhanced Anti-Cancer Activity.
Although curcumin is effective in killing cancer cells, its low water solubility and inadequate bioavailability remain major limitations to its therapeutic application. Formulating curcumin micellar nanoparticles (Cur-NPs) encapsulated with a biodegradable polymer can significantly improve curcumin's solubility, stability, and bioavailability in vitro. In this study, differently sized Cur-NPs coated with polyvinyl alcohol (PVA) were engineered. The particle size, encapsulation efficiency, in vitro release, stability, cytotoxicity, and cellular uptake of these Cur-NPs were characterized in several cancer cell lines. The results showed that, relative to solubilized curcumin, Cur-NPs demonstrated higher cytotoxicity against cancer cells. To our knowledge, this study is the first to demonstrate that the extent of the anti-cancer potency and cellular uptake of Cur-NPs is directly correlated to particle size, where Cur-NPs with the smallest size (28 nm) were the most potent. Confocal microscopy revealed the subcellular localization of the smaller Cur-NPs (28 nm) to be in both the nucleus and cytoplasm, while the larger particles (200 nm) were only localized in the cytoplasm.
Wing-Hin
WH
Lee
Mary
M
Bebawy
Ching-Yee
CY
Loo
Frederick
F
Luk
Rebecca S
RS
Mason
Ramin
R
Rohanizadeh
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D003474:Curcumin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D006801:Humans; D061986:MCF-7 Cells; D008823:Micelles; D055616:Microtechnology; D053758:Nanoparticles / Q000737:chemistry / Q000627:therapeutic use; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D010316:Particle Size; D012995:Solubility; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D003474:Curcumin