Design of Curcumin Loaded PLGA Nanoparticles Formulation with Enhanced Cellular Uptake, and Increased Bioactivity in vitro and Superior Bioavailability in vivo

By P. Anand, Harish B. Nair, Bokyung Sung, A. Kunnumakkara, V. Yadav, R. Tekmal, Bharat B. Aggarwal. Biochemical Pharmacology, 2009

628 citations recorded by the source corpus.

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.

Subfields: Molecular Biology, Molecular Medicine, Pharmacology

View Paper: https://www.semanticscholar.org/paper/837ea783a02d5907d7b4e5ade867820a4968c108

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Citations in the corpus

A Review on Antibacterial, Antiviral, and Antifungal Activity of Curcumin (2014, background): “The optimum potential of curcumin is limited because of poor oral bioavailability and insufficient solubility in aqueous solvents leading to poor absorption, fast metabolism, and quick systemic elimination [5, 93].”
Curcumin, a component of golden spice: from bedside to bench and back. (2014, background): “Other effective formulation PLGA encapsulated curcumin also exhibited almost twice as high serum concentration of PLGA-curcumin than curcumin in animals (Anand et al., 2010).”
Curcumin nanoformulations: a review of pharmaceutical properties and preclinical studies and clinical data related to cancer treatment. (2014, background): “However, no in vitro release data were reported [77].”
Bactericidal Activity of Curcumin I Is Associated with Damaging of Bacterial Membrane (2015, background): “All previous studies on curcumin have indicated its membrane altering properties such as thinning and disruption of the membrane at high concentrations using artificial membranes only [26].”
Cellular Stress Responses, The Hormesis Paradigm, and Vitagenes: Novel Targets for Therapeutic Intervention in Neurodegenerative Disorders (2010, positive): “In primary cocultures of rat microglial and astroglial cells, dimethyl fumarate attenuated LPS-induced production of TNF a , IL-1 b , IL-6, and NO, in addition to inducing Nrf2-dependent genes (468).”
Targets of curcumin (2011, neutral): “These approaches include: the use of adjuvants such as piperine to suppress glucuronidation in the liver [253], the use of liposomal curcumin [259], curcumin nanoparticles [260], the use of curcumin phospholipid complex [261], and the use of structural analogs of curcumin [262].”