Photophysical characterization of anticancer drug valrubicin in rHDL nanoparticles and its use as an imaging agent.

J Photochem Photobiol B

Department of Cell Biology and Immunology, Center for Fluorescence Technologies and Nanomedicine, UNT Health Science Center, Fort Worth, TX, USA. Electronic address:

Published: February 2016

AI Article Synopsis

  • Nanoparticles like reconstituted high density lipoprotein (rHDL) are being used as targeted drug delivery systems in cancer therapy, enhancing the effectiveness of drugs while reducing side effects.
  • The anti-cancer drug valrubicin has poor water solubility, limiting its use, but encapsulating it in rHDL nanoparticles increases its fluorescence properties significantly, indicating deeper localization within the nanoparticles.
  • These enhanced fluorescence characteristics can help track the drug's distribution to cancer cells, showing potential for improved delivery in systemic therapies, such as intravenous treatments.

Article Abstract

Nanoparticles are target-specific drug delivery agents that are increasingly used in cancer therapy to enhance bioavailability and to reduce off target toxicity of anti-cancer agents. Valrubicin is an anti-cancer drug, currently approved only for vesicular bladder cancer treatment because of its poor water solubility. On the other hand, valrubicin carrying reconstituted high density lipoprotein (rHDL) nanoparticles appear ideally suited for extended applications, including systemic cancer chemotherapy. We determined selected fluorescence properties of the free (unencapsulated) drug vs. valrubicin incorporated into rHDL nanoparticles. We have found that upon encapsulation into rHDL nanoparticles the quantum yield of valrubicin fluorescence increased six fold while its fluorescence lifetime increased about 2 fold. Accordingly, these and potassium iodide (KI) quenching data suggest that upon incorporation, valrubicin is localized deep in the interior of the nanoparticle, inside the lipid matrix. Fluorescence anisotropy of the rHDL valrubicin nanoparticles was also found to be high along with extended rotational correlation time. The fluorescence of valrubicin could also be utilized to assess its distribution upon delivery to prostate cancer (PC3) cells. Overall the fluorescence properties of the rHDL: valrubicin complex reveal valuable novel characteristics of this drug delivery vehicle that may be particularly applicable when used in systemic (intravenous) therapy.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5531042PMC
http://dx.doi.org/10.1016/j.jphotobiol.2015.12.007DOI Listing

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