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Diclofenac Loaded Biodegradable Nanoparticles as Antitumoral and Antiangiogenic Therapy
Gerard Esteruelas1,2, Eliana B Souto3,4, Marta Espina1,2
1Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08007 Barcelona, Spain.
Abstract:
Cancer is identified as one of the main causes of death worldwide, and an effective treatment that can reduce/eliminate serious adverse effects is still an unmet medical need. Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), has demonstrated promising antitumoral properties. However, the prolonged use of this NSAID poses several adverse effects. These can be overcome by the use of suitable delivery systems that are able to provide a controlled delivery of the payload. In this study, Diclofenac was incorporated into biodegradable polymeric nanoparticles based on PLGA and the formulation was optimized using a factorial design approach. A monodisperse nanoparticle population was obtained with a mean size of ca. 150 nm and negative surface charge. The release profile of diclofenac from the optimal formulation followed a prolonged release kinetics. Diclofenac nanoparticles demonstrated antitumoral and antiangiogenic properties without causing cytotoxicity to non-tumoral cells, and can be pointed out as a safe, promising and innovative nanoparticle-based formulation with potential antitumoral effects.
Insights
Biodegradable polymeric nanoparticles effectively delivered diclofenac, a non-steroidal anti-inflammatory drug (NSAID), showcasing antitumoral and antiangiogenic effects without harming healthy cells. This innovative formulation offers a safer approach to cancer treatment.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Cancer is a leading global cause of death, necessitating novel treatments with reduced side effects.
- Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), exhibits antitumoral potential but is limited by adverse effects from prolonged use.
- Controlled drug delivery systems can mitigate NSAID-related toxicity and enhance therapeutic efficacy.
Purpose of the Study:
- To develop and optimize biodegradable polymeric nanoparticles for controlled diclofenac delivery.
- To evaluate the antitumoral, antiangiogenic, and cytotoxic effects of the diclofenac-loaded nanoparticles.
Main Methods:
- Diclofenac was encapsulated in poly(lactic-co-glycolic acid) (PLGA) nanoparticles.
- A factorial design approach was employed for formulation optimization.
- Nanoparticle characterization included size, surface charge, and drug release kinetics.
- In vitro antitumoral, antiangiogenic, and cytotoxicity assays were performed.
Main Results:
- Optimized nanoparticles were monodisperse with a mean size of approximately 150 nm and a negative surface charge.
- The formulation exhibited prolonged diclofenac release kinetics.
- Diclofenac nanoparticles demonstrated significant antitumoral and antiangiogenic activities.
- No cytotoxicity was observed in non-tumoral cells.
Conclusions:
- Biodegradable PLGA nanoparticles provide a safe and effective delivery system for diclofenac.
- The optimized formulation shows potential as an innovative therapeutic strategy for cancer treatment with reduced adverse effects.
