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Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
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Nanodelivery of Parthenolide Using Functionalized Nanographene Enhances its Anticancer Activity.

A Karmakar1, Y Xu1, T Mustafa1

  • 1Center for Integrative Nanotechnology Sciences, University of Arkansas at Little Rock, AR 72204, USA.

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|January 10, 2015
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Carboxyl-functionalized nanographene successfully delivered the anticancer drug parthenolide (PTL), enhancing its efficacy and reducing toxicity in pancreatic cancer cells. This nanodelivery overcomes PTL's poor water solubility, improving its clinical potential.

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Area of Science:

  • Nanotechnology
  • Drug Delivery
  • Oncology

Background:

  • Anticancer drug development faces challenges with poor biocompatibility and water insolubility, leading to increased toxicity.
  • Parthenolide (PTL), a natural compound with anticancer properties, is limited by its poor water solubility.
  • Nanodelivery systems offer a promising strategy to enhance drug bioavailability and reduce systemic toxicity.

Purpose of the Study:

  • To investigate the use of carboxyl-functionalized nanographene (fGn) for delivering parthenolide (PTL).
  • To evaluate the enhanced anticancer efficacy and reduced toxicity of PTL delivered via fGn compared to a water-soluble analog (DMAPT).

Main Methods:

  • Complexation of PTL with carboxyl-functionalized nanographene (fGn).
  • In vitro evaluation of PTL-fGn complex efficacy on human pancreatic cancer cell line (Panc-1).
  • Assessment of apoptosis, ROS generation, and mitochondrial membrane disruption.

Main Results:

  • fGn delivery significantly enhanced the anticancer and apoptotic effects of PTL in Panc-1 cells, reducing the IC50 from 39 µM to 9.5 µM.
  • The PTL-fGn complex showed increased ROS formation and mitochondrial membrane disruption compared to PTL alone.
  • fGn delivery did not improve the efficacy of the water-soluble analog DMAPT, which had a higher IC50 than PTL-fGn.

Conclusions:

  • Carboxyl-functionalized nanographene effectively overcomes the hydrophobicity of PTL, enhancing its anticancer activity.
  • fGn-mediated delivery represents a viable strategy for improving the therapeutic effectiveness of PTL in cancer treatment.
  • This approach holds potential for developing more effective and less toxic chemotherapy agents.