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

Authors

  • 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.

DOI:

https://doi.org/10.22159/ajpcr.2019.v12i6.33377

Keywords:

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

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.

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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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Published

07-06-2019

How to Cite

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, June 2019, pp. 229-37, doi:10.22159/ajpcr.2019.v12i6.33377.

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Original Article(s)