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Published on: December 1, 2016
Radachlorin-Containing Microparticles for Photodynamic Therapy
Sergey Petrovich Krechetov1, Anastasia Maksimovna Miroshkina2, Maria Nikolaevna Yakovtseva1
1Phystech School of Biological and Medical Physics, Moscow Institute of Physics and Technology, Dolgoprudny, Russia.
Abstract:
Reducing the undesirable systemic effect of photodynamic therapy (PDT) can be achieved by incorporating a photosensitizer in microparticles (MPs). This study is devoted to the preparation of biocompatible biodegradable MPs with the inclusion of the natural photosensitizer Radachlorin (RС) and an assessment of the possibility of their use for PDT. RC-containing MPs (RС MPs) with poly(lactic-co-glycolic acid) copolymer (PLGA) matrix were prepared by a double emulsion solvent evaporation methods. The size and morphology of RC MPs were surveyed using scanning electron microscopy, confocal laser scanning microscopy, and dynamic light scattering. The content of RC, its release from RC MPs, and singlet oxygen generation were evaluated by the optical spectroscopy. Cellular uptake and cytotoxic photodynamic effect of RC MPs were investigated with in vitro assays. The average diameter of the prepared RC MPs was about 2-3 μm. The RC MPs prepared by the water/oil/oil method had a significantly higher inclusion of RC (1.74 μg/mg) then RC MPs prepared by the water/oil/water method (0.089 μg/mg). Exposure of the prepared RC MPs to PDT light radiation was accompanied by the singlet oxygen generation and a cytotoxic effect for tumor cells. The release of the RC from the RC MPs was prolonged and lasted at least two weeks. PLGA RC MPs were found to cause a photoactivated cytotoxic effect for tumor cells and can be used for local application in PDT of tumors.
Insights
Biodegradable microparticles containing Radachlorin (RC) offer a targeted approach to photodynamic therapy (PDT). These RC-loaded microparticles demonstrate sustained release and potent photoactivated cytotoxicity against tumor cells.
Area of Science:
- Biomaterials Science
- Photodynamic Therapy
- Drug Delivery Systems
Background:
- Photodynamic therapy (PDT) faces challenges with systemic side effects.
- Microparticles (MPs) can encapsulate photosensitizers to improve PDT efficacy and localization.
- Radachlorin (RC) is a natural photosensitizer with potential therapeutic applications.
Purpose of the Study:
- To prepare biocompatible, biodegradable MPs incorporating the natural photosensitizer Radachlorin (RC).
- To evaluate the potential of these RC-loaded MPs for targeted photodynamic therapy.
- To characterize the physical properties, drug release, and in vitro efficacy of the developed MPs.
Main Methods:
- Preparation of RC-containing MPs (RC MPs) using poly(lactic-co-glycolic acid) (PLGA) via double emulsion solvent evaporation.
- Characterization of RC MPs size, morphology, and RC content using SEM, CLSM, DLS, and optical spectroscopy.
- In vitro assessment of cellular uptake, prolonged RC release, singlet oxygen generation, and photocytotoxic effect on tumor cells.
Main Results:
- PLGA RC MPs were successfully prepared with an average diameter of 2-3 μm.
- The water/oil/oil method yielded significantly higher RC loading (1.74 μg/mg) compared to water/oil/water (0.089 μg/mg).
- RC MPs exhibited sustained RC release over two weeks, generated singlet oxygen upon light exposure, and demonstrated a photoactivated cytotoxic effect on tumor cells.
Conclusions:
- PLGA-based RC MPs are effective in delivering Radachlorin for photodynamic therapy.
- These MPs show potential for localized PDT applications, reducing systemic toxicity.
- The developed RC MPs offer a promising strategy for enhanced tumor treatment via PDT.
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