FABRICATION, CHARACTERIZATION, AND IN VITRO EVALUATION OF PEGYLATED GLYCERIDE LABRASOL® NANOSTRUCTURED LIPID CARRIER COMPOSITES OF METHOTREXATE: THE PATHWAY TO EFFECTIVE CANCER THERAPY

  • RADHARANI PANDA Department of Pharmaceutical Technology, Division of Pharmaceutics, Jadavpur University, Kolkata, West Bengal, India.
  • KETOUSETUO KUOTSU Department of Pharmaceutical Technology, Division of Pharmaceutics, Jadavpur University, Kolkata, West Bengal, India.

Abstract

Objective: The objective of the current study is to optimize and evaluate the potential of polyethylene glycolylated (PEG) glyceride Labrasol® nanostructured lipid carrier (NLC) composites of methotrexate (MTX) to achieve enhanced sustained release delivery in cancer treatment.


Materials and Methods: MTX-NLC was successfully prepared by hot melt emulsification and probe sonication method for spatial and controlled release of this therapeutic agent.


Results: The solubility screening of MTX and lipids resulted in the selection of Monostearin as solid lipid, PEGylated glyceride Labrasol® and olive oil as liquid lipids for the formulation of MTX-loaded NLC composites. Particle size, zeta potential, and polydispersity index of both the composites were confirmed using dynamic light scattering, whereby Labrasol® MTX-NLC showed high entrapment efficiency and drug loading. A spherical particle shape with smooth surface of all the composites was confirmed from the scanning electron microscope and transmission electron microscopy analysis. Labrasol® MTX-NLC showed remarkably increased cytotoxic response, augmented cellular uptake, and low half maximal inhibitory concentration value in MCF-7 cells. In vitro release study confirmed that encapsulation of MTX in PEGylated glyceride Labrasol® MTX-NLC resulted in enhanced sustained release of MTX for a period of 48 h.


Conclusion: The present study establishes that PEGylated glyceride Labrasol® MTX-NLC can be considered as a promising anticancer delivery system, thereby improving antitumor efficacy of the drug.

Keywords: Methotrexate, Nanostructured lipid carrier,, Polyethylene glycolylated glyceride,, In vitro release,, MCF-7 cells,, Half maximal inhibitory concentration value,, Cellular uptake.

Author Biography

RADHARANI PANDA, Department of Pharmaceutical Technology, Division of Pharmaceutics, Jadavpur University, Kolkata, West Bengal, India.

Research Scholar,

Division of Pharmaceutics,

Department of Pharmaceutical Technology,

Jadavpur University,

Kolkata-700032, West Bengal, India.

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RADHARANI PANDA, and KETOUSETUO KUOTSU. “FABRICATION, CHARACTERIZATION, AND IN VITRO EVALUATION OF PEGYLATED GLYCERIDE LABRASOL® NANOSTRUCTURED LIPID CARRIER COMPOSITES OF METHOTREXATE: THE PATHWAY TO EFFECTIVE CANCER THERAPY”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 12, no. 6, Apr. 2019, pp. 229-37, https://innovareacademics.in/journals/index.php/ajpcr/article/view/33377.
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