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Fluorescence-quenching of a Liposomal-encapsulated Near-infrared Fluorophore as a Tool for In Vivo Optical Imaging
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Thermosensitive liposomes encapsulating hypericin: Characterization and photodynamic efficiency.

Alice Abu Dayyih1, Mohamad Alawak1, Abdallah M Ayoub2

  • 1Department of Pharmaceutics and Biopharmaceutics, Philipps Universität Marburg, 35037 Marburg, Germany.

International Journal of Pharmaceutics
|October 21, 2021
PubMed
Summary
This summary is machine-generated.

Hypericin thermosensitive liposomes (Hyp-TSL) improve drug delivery and anti-tumor efficacy by releasing Hypericin (Hyp) in response to mild heat. This nanocarrier system enhances Hypericin bioavailability and cancer cell targeting, leading to improved therapeutic outcomes.

Keywords:
Cellular uptakeHypericinPhotodynamic therapyStimuli-responsive nanocarrierThermosensitive liposomes

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Area of Science:

  • Nanotechnology
  • Biomedical Engineering
  • Photodynamic Therapy

Background:

  • Hypericin (Hyp) exhibits potent photodynamic anti-tumor activity but suffers from poor water solubility, limiting its clinical application.
  • Stimuli-triggered nanocarriers offer enhanced bioavailability and targeted drug delivery compared to conventional methods.

Purpose of the Study:

  • To develop and optimize Hypericin thermosensitive liposomes (Hyp-TSL) for improved cancer therapy.
  • To evaluate the thermal sensitivity, drug release, cellular uptake, and anti-tumor efficacy of Hyp-TSL.

Main Methods:

  • Hyp-TSL were formulated using DPPC, DSPC, and DSPE-PEG2000, characterized for size, encapsulation efficiency, and colloidal stability.
  • Thermal sensitivity was assessed by monitoring liposomal integrity at varying temperatures.
  • Cellular uptake and reactive oxygen species generation were evaluated in MDA-MB-231 cells under hyperthermic conditions (42°C).
  • In vitro cytotoxicity was determined by measuring the half-maximal inhibitory concentration (IC50) after hyperthermic treatment.

Main Results:

  • Optimized Hyp-TSL showed a hydrodynamic diameter <100 nm, 94.5% encapsulation efficiency, and good stability.
  • Hyp-TSL demonstrated thermal sensitivity with a phase transition temperature of 41.1°C, leading to liposomal destruction above this temperature.
  • Hyperthermic treatment at 42°C significantly increased Hyp-TSL uptake and reactive oxygen species generation in cancer cells.
  • The IC50 of Hyp-TSL was reduced 3.8-fold at 42°C compared to 37°C, indicating enhanced anti-tumor efficacy.
  • Hemocompatibility studies confirmed Hyp-TSL safety for intravenous administration.

Conclusions:

  • Optimized Hyp-TSL effectively encapsulate Hypericin and release it in response to mild hyperthermia.
  • This stimuli-triggered delivery system enhances Hypericin's anti-tumor activity by improving cellular uptake and efficacy.
  • Hyp-TSL represent a promising nanocarrier for photodynamic therapy, improving drug bioavailability and therapeutic outcomes.