RETRACTED: Design of curcumin-loaded PLGA nanoparticles formulation with enhanced cellular uptake, and increased bioactivity in vitro and superior bioavailability in vivo

Abstract

Curcumin, a yellow pigment present in the spice turmeric (Curcuma longa), has been linked with antioxidant, anti-inflammatory, anti-proliferative, anticancer, antidiabetic, antirheumatic, and antiviral effects, but its optimum potential is limited by its lack of solubility in aqueous solvents and poor oral bioavailability. We employed a polymer-based nanoparticle approach to improve bioavailability. Curcumin was encapsulated with 97.5% efficiency in biodegradable nanoparticulate formulation based on poly (lactide-co-glycolide) (PLGA) and a stabilizer polyethylene glycol (PEG)-5000. Dynamic laser light scattering and transmission electron microscopy indicated a particle diameter of 80.9 nm. This curcumin, renamed from hereon “as curcumin (NP)”, was characterized for its biological activity. In vitro curcumin (NP) exhibited very rapid (2 h vs > 72 h) and more efficient cellular uptake then curcumin. Estrase staining revealed that curcumin (NP) was at least as potent as or more potent than curcumin in inducing apoptosis of leukemic cells and in suppressing proliferation of various tumor cell lines. When examined by electrophoretic gel shift mobility assay, curcumin (NP) was more active than curcumin in inhibiting TNF-induced NF-κB activation and in suppression of NF-κB-regulated proteins involved in cell proliferation (cyclin D1), invasion (MMP-9), and angiogenesis (VEGF). In mice, curcumin (NP) was more bioavailable and had a longer half-life than curcumin. Overall we demonstrate that curcumin-loaded PLGA nanoparticles formulation has enhanced cellular uptake, and increased bioactivity in vitro and superior bioavailability in vivo over curcumin.

Advanced targeted therapies in cancer: Drug nanocarriers, the future of chemotherapy

“…Anand et al [459] prepared curcumin-loaded biodegradable nanoparticles (80.9 nm) based on PLGA and PEG-5000 as stabilizer. The encapsulated curcumin had enhanced cellular uptake and bioactivity in vitro (antitumor, anti-invasive and antiangiogenic effects) compared to free curcumin, inducing apoptosis in leukemic cells and suppressing proliferation in different tumor cell lines.…”

A comparative study on the antioxidant and immunomodulatory properties of curcumin conjugated gold nanospheres and free curcumin

“…Till now a number of curcumin delivery strategies have been developed such as micelles (Ma et al, 2008), liposomal vesicles (Nguyen et al, 2016), nanoparticles (Bisht et al, 2007;Shaikh et al, 2009;Anand et al, 2010), nanoemulsions (Ganta and Amiji, 2009), phospholipid complexes (Maiti et al, 2007) and polymeric implants (Bansal et al, 2011) etc. to enhance its bioavailability.…”

Enhancement of Antibiotic Efficacy against Multi-drug Resistant Pseudomonas Aeruginosa Infections via Combination with Curcumin and 1-(1-Naphthylmethyl)-Piperazine

“…However, in an attempt to improve oral bioavailability of CUR researchers have investigated coupling the compound to nanocarriers. Thus, curcumin-loaded poly lactideco-glycolide and curcumin nanoparticles had superior bioactivity and bioavailability in addition to enhanced cellular uptake compared to curcumin alone [22]. In addition, encapsulation of curcumin with gelatin or starch improved the solubility and stability of the compound whilst retaining antimicrobial activity [23].…”