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The major therapeutic limitation of curcumin and indole-incorporated curcumin analog is its low bioavailability. We hypothesized that nano-encapsulation of indole-incorporated curcumin analog and curcumin as a biodegradable polymeric nanoparticle may enhance its bioavailability with extended drug retention time. Indole-incorporated curcumin analog and curcumin loaded PLGA nanoparticles were synthesized by solvent evaporation technique. Physicochemical characterizations and anti-cancer potential of the nanoparticles were evaluated in human colon cancer cell line SW480. The synthesized NPs had a size range of 50-150 nm diameter. The nano-formulation preserved the drug from degradation in wide ranges of pH environments. The nanoparticles treatment against SW480 cancer cell line triggered nuclear fragmentation, cell cycle blockade, inhibition of apoptosis and metastatic biomarkers. These drug-loaded nanoparticles may be potent nano-formulations against colon cancer because of its ability to tolerate extreme pH environments, thus having potential of oral drug-delivery., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Significance: Efficient targeted therapy with minimal side-effects is the need of the hour. Locally altered redox state is observed in several human ailments, such as inflammation, sepsis, and cancer. This has been taken advantage of in designing redox-responsive nanodrug carriers. Redox-responsive nanosystems open a door to a multitude of possibilities for the control of diseases over other drug delivery systems. Recent Advances: The first-generation nanotherapy relies on novel properties of nanomaterials to shield the drug and deliver it to the diseased tissue or organ. The second generation is based on targeting the drug or diagnostic material to the diseased cell-specific receptors, or to a particular organ to improve the efficacy of the drug. The third and the latest generation of nanocarriers, the stimuli-responsive nanocarriers exploit the disease condition or environment to specifically deliver the drug or diagnostic probe for the best diagnosis and treatment. Several different kinds of stimuli such as temperature, magnetic field, pH, and altered redox state-responsive nanosystems have educed immense promise in the field of nanomedicine and therapy., Critical Issues: We describe the evolution of nanomaterial since its inception with an emphasis on stimuli-responsive nanocarriers, especially redox-sensitive nanocarriers. Importantly, we discuss the future perspectives of redox-responsive nanocarriers and their implications., Future Directions: Redox-responsive nanocarriers achieve a near-to-zero premature release of the drug, thus avoiding off-site toxicity associated with the free drug. This bears great potential for the development of more effective drug delivery with better pharmacokinetics and pharmacodynamics.

Aim: Our hypothesis was to prove that surface modifiers themselves can be used as stabilizers and that their entrapment efficiency is directly influenced by the type of stabilizers used., Materials & Methods: Particle size and the polydispersity index of the nanoparticles (NPs) were measured by dynamic light scattering, whereas the morphology of the NPs was studied by scanning electron microscopy. Percentage nanoparticle yield, entrapment efficiency and drug loading capacity were measured by ultraviolet absorbance. The physical rigidity, robustness and drug releasing capability of these NPs were also assessed., Conclusion: Physiochemical characterization and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay suggest that polysorbate 80 has the dual capability of being a stabilizer and a surface modifier in addition to having better drug entrapment properties than Pluronic® 188. Disulfiram, the drug that was loaded on these NPs, is also observed for the first time to show significant anticancer potential against hepatocellular carcinoma (Hep3B) cell lines.