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Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma
Gabriel Martínez-Razo1, Patrícia C Pires2,3,4, María Lilia Domínguez-López1
1Laboratorio de Toxicología Ambiental, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Unidad Profesional Zacatenco, Mexico City 07738, Mexico.
Abstract:
Melanoma is a highly lethal type of cancer that has had an increase in incidence in the last decades. Nevertheless, current therapies lack effectiveness and have highly disabling side effects, which calls for new therapeutic strategies. Norcantharidin (NCTD) is an acid derivative with potential antitumor activity isolated from natural blister beetles. However, its solubility limitations restrict its use. To address this issue, we developed an oil-in-water nanoemulsion using commonly available cosmetic ingredients, which increased NCTD solubility 10-fold compared to water. The developed nanoemulsion showed a good droplet size and homogeneity, with adequate pH and viscosity for skin application. In vitro drug release studies showed a sustained release profile, ideal for prolonged therapeutic effects. Accelerated stability studies proved that the formulation was reasonably stable under stress conditions, with particle separation fingerprints, instability index, particle size, and sedimentation velocity analyses being conducted. To assess the therapeutic potential of the developed formulation, in vitro studies were conducted on melanoma B16F1 cells; results showed an IC50 of 1.026 +/- 0.370 mg/kg, and the cells' metabolic activity decreased after exposure to the NCTD nanoemulsion. Hence, a new "easy-to-make" nanoformulation with therapeutic potential on melanoma cells was developed, as a possible adjuvant for future melanoma treatment.
Insights
Researchers developed a novel nanoemulsion to improve the solubility of Norcantharidin (NCTD), a potential melanoma treatment. This formulation demonstrated sustained drug release and significant antitumor activity against melanoma cells in vitro.
Area of Science:
- Pharmaceutical Sciences
- Oncology
- Nanotechnology
Background:
- Melanoma incidence is rising, and current treatments have limitations, necessitating novel therapeutic strategies.
- Norcantharidin (NCTD), a natural compound, shows antitumor potential but suffers from poor solubility, hindering its clinical application.
Purpose of the Study:
- To develop a stable and effective nanoemulsion formulation for Norcantharidin (NCTD) delivery.
- To evaluate the in vitro therapeutic potential of the NCTD nanoemulsion against melanoma cells.
Main Methods:
- An oil-in-water nanoemulsion was formulated using cosmetic ingredients to enhance NCTD solubility.
- Physicochemical properties (droplet size, pH, viscosity) and stability were assessed.
- In vitro drug release, cytotoxicity (IC50), and metabolic activity assays were performed on melanoma B16F1 cells.
Main Results:
- The nanoemulsion increased NCTD solubility 10-fold and exhibited suitable characteristics for skin application.
- Formulation stability was confirmed under accelerated stress conditions.
- The NCTD nanoemulsion demonstrated a sustained release profile and significant reduction in melanoma cell viability (IC50: 1.026 ± 0.370 mg/kg).
Conclusions:
- An easily prepared nanoemulsion effectively improved NCTD solubility and demonstrated promising in vitro antitumor activity.
- This nanoformulation holds potential as an adjuvant therapy for future melanoma treatment.
