Fabrication, Characterization, and in Vitro Evaluation of Pegylated Glyceride Labrasol® Nanostructured Lipid Carrier Composites of Methotrexate: The Pathway to Effective Cancer Therapy

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.

Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization

“…On the other hand, changing the concentration of the Further, ZP of −35 to −25 mV is required for electrostatic stabilization for dispersed systems [34]. This result is attributed to the presence of Labrasol PEG chains that cover the particle surfaces that have a better effect on the zeta potential which is often the key factor in understanding how the dispersion and aggregation processes are applied [35]. As depicted (Figure 3B), decreasing the homogenization speed (F) and total lipid concentration (H) as well as increasing the percentage of the solid lipid ratio in the solid/liquid lipid mixture 9 of 23 (J), and the sonication time (G) had favorable effects on ZP (decreased).…”

“…Additionally, no burst AT release was noticed from the optimized AT-NLC formulation. This may be attributed to the presence of the PEG moiety of Labrasol at the surface of the NLCs causing a barrier for AT diffusion [35]. The relatively elevated cumulative release rate of AT-NLCs was presumably due to the disordered amorphous state of the AT that exhibited a higher dissolution rate and aqueous solubility [54].…”