Abstract
Formulation of promising anticancer herbal drug curcumin as a nanoscale-sized curcumin (nanocurcumin) improved its delivery to cells and organisms both in vitro and in vivo. We report on coupling nanocurcumin with upconversion nanoparticles (UCNPs) using Poly (lactic-co-glycolic Acid) (PLGA) to endow visualisation in the near-infrared transparency window. Nanocurcumin was prepared by solvent-antisolvent method. NaYF4:Yb,Er (UCNP1) and NaYF4:Yb,Tm (UCNP2) nanoparticles were synthesised by reverse microemulsion method and then functionalized it with PLGA to form UCNP-PLGA nanocarrier followed up by loading with the solvent-antisolvent process synthesized herbal nanocurcumin. The UCNP samples were extensively characterised with XRD, Raman, FTIR, DSC, TGA, UV-VIS-NIR spectrophotometer, Upconversion spectrofluorometer, HRSEM, EDAX and Zeta Potential analyses. UCNP1-PLGA-nanocurcumin exhibited emission at 520, 540, 660 nm and UCNP2-PLGA-nanocurmin showed emission at 480 and 800 nm spectral bands. UCNP-PLGA-nanocurcumin incubated with rat glioblastoma cells demonstrated moderate cytotoxicity, 60–80% cell viability at 0.12–0.02 mg/mL marginally suitable for therapeutic applications. The cytotoxicity of UCNPs evaluated in tumour spheroids models confirmed UCNP-PLGA-nanocurcumin therapeutic potential. As-synthesised curcumin-loaded nanocomplexes were administered in tumour-bearing laboratory animals (Lewis lung cancer model) and showed adequate contrast to enable in vivo and ex vivo study of UCNP-PLGA-nanocurcumin bio distribution in organs, with dominant distribution in the liver and lungs. Our studies demonstrate promise of nanocurcumin-loaded upconversion nanoparticles for theranostics applications.
Highlights
Cancer is a major global health issue that needs novel approaches in addition to conventional surgical resection, chemotherapy, or radiotherapy [1]
We report on synthesis and characterisation of biofunctional nanocomplexes of NaYF4 : Yb,Er and NaYF4 :Yb,Tm upconversion nanoparticles surface-coated with PLGA and nanocurcumin
UCNP1-PLGA-nanocur and UCNP2-PLGA-nanocur composites were prepared by facile molecular interaction approach
Summary
Cancer is a major global health issue that needs novel approaches in addition to conventional surgical resection, chemotherapy, or radiotherapy [1]. UCNPs demonstrate unique optical properties, including high penetration into biological tissues due to so called near-infrared transparency window, high resistance to photobleaching, absence of autofluorescence, multicolour emission with a narrow line width, high luminescence lifetime, low irradiation damage, and increased signal-to-noise ratio and photochemical stability [4]. Drug delivery of curcumin accompanied by PLGA could increase therapeutic efficacies to promote sustained drug delivery and drug release targeting, minimize the non-specific consumption by undesirable tissues and to enhance the aqueous solubility [10,24,25]. In vivo biodistribution of these nanocomplexes was investigated in small animals
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