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Antitumoral melatonin-loaded nanostructured lipid carriers
Lorena Bonilla-Vidal1,2, Marta Świtalska3, Marta Espina1,2
1Department of Pharmacy, Pharmaceutical Technology & Physical Chemistry, University of Barcelona, Barcelona, 08028, Spain.
Abstract:
Aim: Cancer constitutes the second leading cause of death worldwide, with conventional therapies limited by significant side effects. Melatonin (MEL), a natural compound with antitumoral properties, suffers from instability and low solubility. To overcome these issues, MEL was encapsulated into nanostructured lipid carriers (MEL-NLC) containing rosehip oil to enhance stability and boost its antitumoral activity.Methods: MEL-NLC were optimized by a design of experiments approach and characterized for their physicochemical properties. Stability and biopharmaceutical behavior were assessed, along with interaction studies and in vitro antitumoral efficacy against various cancer cell lines.Results: Optimized MEL-NLC exhibited desirable physicochemical characteristics, including small particle size and sustained MEL release, along with long-term stability. In vitro studies demonstrated that MEL-NLC selectively induced cytotoxicity in several cancer cell lines while sparing healthy cells.Conclusion: MEL-NLC represent a promising alternative for cancer, combining enhanced stability and targeted antitumoral activity, potentially overcoming the limitations of conventional treatments.
Insights
Melatonin (MEL) was encapsulated into nanostructured lipid carriers (MEL-NLC) to improve its stability and antitumoral efficacy. These MEL-NLCs demonstrated selective cancer cell killing while sparing healthy cells, offering a promising alternative cancer treatment.
Area of Science:
- Nanotechnology in Medicine
- Cancer Therapeutics
- Pharmacology
Background:
- Cancer is a leading global cause of death with limited conventional therapy options.
- Melatonin (MEL), a natural compound, shows antitumoral properties but is limited by instability and poor solubility.
- Developing stable and effective drug delivery systems for natural compounds is crucial for cancer treatment.
Purpose of the Study:
- To enhance the stability and antitumoral activity of melatonin (MEL) by encapsulating it into nanostructured lipid carriers (MEL-NLC).
- To investigate the physicochemical properties, stability, and in vitro antitumoral efficacy of MEL-NLC.
- To evaluate MEL-NLC as a potential alternative cancer therapy.
Main Methods:
- Optimization of MEL-NLC using a design of experiments approach.
- Characterization of MEL-NLC for physicochemical properties, stability, and drug release kinetics.
- In vitro assessment of MEL-NLC cytotoxicity against various cancer cell lines and healthy cells.
Main Results:
- Optimized MEL-NLC showed favorable physicochemical characteristics, including small particle size and sustained melatonin release.
- MEL-NLC exhibited long-term stability, addressing a key limitation of free melatonin.
- In vitro studies confirmed selective cytotoxicity of MEL-NLC against cancer cells, with minimal impact on healthy cells.
Conclusions:
- MEL-NLC formulation enhances melatonin's stability and delivery for cancer treatment.
- The nanostructured lipid carrier system demonstrates targeted and selective antitumoral activity.
- MEL-NLC presents a promising, potentially less toxic, alternative to conventional cancer therapies.
