title: Entrapment of curcumin into monoolein-based liquid crystalline nanoparticle dispersion for enhancement of stability and anticancer activity.
abstract: Despite the promising anticancer potential of curcumin, its therapeutic application has been limited, owing to its poor solubility, bioavailability, and chemical fragility. Therefore, various formulation approaches have been attempted to address these problems. In this study, we entrapped curcumin into monoolein (MO)-based liquid crystalline nanoparticles (LCNs) and evaluated the physicochemical properties and anticancer activity of the LCN dispersion. The results revealed that particles in the curcumin-loaded LCN dispersion were discrete and monodispersed, and that the entrapment efficiency was almost 100%. The stability of curcumin in the dispersion was surprisingly enhanced (about 75% of the curcumin survived after 45 days of storage at 40°C), and the in vitro release of curcumin was sustained (10% or less over 15 days). Fluorescence-activated cell sorting (FACS) analysis using a human colon cancer cell line (HCT116) exhibited 99.1% fluorescence gating for 5 μM curcumin-loaded LCN dispersion compared to 1.36% for the same concentration of the drug in dimethyl sulfoxide (DMSO), indicating markedly enhanced cellular uptake. Consistent with the enhanced cellular uptake of curcumin-loaded LCNs, anticancer activity and cell cycle studies demonstrated apoptosis induction when the cells were treated with the LCN dispersion; however, there was neither noticeable cell death nor significant changes in the cell cycle for the same concentration of the drug in DMSO. In conclusion, entrapping curcumin into MO-based LCNs may provide, in the future, a strategy for overcoming the hurdles associated with both the stability and cellular uptake issues of the drug in the treatment of various cancers.
authors: College of Pharmacy, Gachon University, Incheon, South Korea.
authors: Rengarajan
authors: R
authors: Baskaran
authors: College of Pharmacy Yeungnam University, Gyeongsan, South Korea.
authors: Thiagarajan
authors: T
authors: Madheswaran
authors: College of Pharmacy, Gachon University, Incheon, South Korea.
authors: Pasupathi
authors: P
authors: Sundaramoorthy
authors: College of Pharmacy, Gachon University, Incheon, South Korea.
authors: Hwan Mook
authors: HM
authors: Kim
authors: College of Pharmacy, Gachon University, Incheon, South Korea.
authors: Bong Kyu
authors: BK
authors: Yoo
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D003474:Curcumin / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D005989:Glycerides / Q000737:chemistry*; D045325:HCT116 Cells; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005989:Glycerides; C005953:monoolein; D003474:Curcumin
keywords: anticancer activity; cell cycle distribution; cellular uptake; curcumin; liquid crystalline nanoparticle; monoolein