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.

Self-Assembly of Organic Nanomaterials and Biomaterials: The Bottom-Up Approach for Functional Nanostructures Formation and Advanced Applications

“…For example, the successful incorporation of active compounds and drugs into LCNs has been exploited for the delivery of drugs through the blood-brain barrier (BBB), thus evidencing several advantages, like: Controlled drug release, improved colloidal stability (and drug bioavailability), reduced chemical and physiological degradation (in vivo) and reduction of side effects [47,48]. Moreover, entrapment of the curcumin into specific dispersion of monoolein-based liquid crystalline nanoparticle (with almost 100% encapsulation efficiency) evidenced enhancement of the colloidal stability of curcumin in the nano-formulation (about 75% of the curcumin is able to survive after 45 days of storage at T = 40 • C), while the in vitro release of curcumin was sustained (10% or less over 15 days) [49].…”

Curcumin’s Nanomedicine Formulations for Therapeutic Application in Neurological Diseases

“…Incorporation of drugs into LCNs for delivery processes through the BBB evidenced several advantages like controlled drug release, improved drug bioavailability, reduced chemical and physiological degradation, in vivo, and reduction of side effects [228,229]. Recently, entrapment of CUR into monoolein-based liquid crystalline nanoparticle dispersion (with almost 100% encapsulation efficiency) evidenced enhancement of the colloidal stability of CUR in the nanoformulation (about 75% of the CUR survived after 45 days of storage at 40 • C), while the in vitro release of CUR was sustained (10% or less over 15 days) [230]. Moreover, the release of CUR in bulk mesophases and in inverse hexagonal (HII) liquid crystals and the radical scavenging activity of LCNPs were also recently investigated [228].…”

A novel approach of encapsulating curcumin and succinylated derivative in mannosylated-chitosan nanoparticles

“…Furthermore, CS is biocompatible and has been used to formulate drug delivery systems that improve the cellular uptake of several therapeutics (Aibani, Rai, Patel, Cuddihy, & Wasan, 2021). Of relevance to the current work is that CS polymeric nanoparticles have been shown to be essential in protecting CUR from degradation, promoting cellular uptake, thereby potentiating its therapeutic activity (Baskaran, Madheswaran, Sundaramoorthy, Kim, & Yoo, 2018). Furthermore, conjugation of CS with mannose (mannosylated-CS) and formulation as nanoparticles has been shown to prompt effective uptake of the nanoparticles by cancer tissue (Shi et al, 2017).…”