Increasing the Stability of Pellets Containing Lycopene by Using Dual-Coating

Purpose

Lycopene (LYC) is a natural carotenoid, which has antioxidant, anti-inflammatory and anti-cancer properties. Nevertheless, its inherent instability has hindered oral formulation and administration due to sensitivity of LYC to environmental conditions.

Methods

We tested different methods of tomato extraction to provide an extract with the highest yield of extracted LYC and prepared double coated pellets to enhance the physiochemical properties of LYC and improve its efficacy. The pellets were prepared by extrusion-spheronization technique and were coated by Eudragit L 100 − 55 to protect LYC from gastric acidic pH. To increase the protection of LYC from environmental conditions and provide an opaque, thick layer on the pellets, a layer of sugar-coating was added around the film-coated pellets. Particle size, sphericity, morphology, dissolution, and stability of the pellets were analyzed.

Results

The highest yield of extracted LYC achieved by the mixture of ethyl acetate-acetone (1:1 v/v) applying for 5 h at 40 °C. The dissolution test of the pellets demonstrated that the dual-coating could protect LYC in the simulated gastric medium and release it in the simulated intestinal medium. The result of the stability test confirmed the efficiency of the additional sugar-coat to the film layer of the pellets since the amount of remaining LYC in dual-coated pallets was significantly higher than the film-coated pellets after six months of accelerated stability test.

Conclusion

The dual-coating of the pellets could protect LYC from environmental conditions and increase its stability. However, addition of substances to the formulation which might maximize the stability of LYC requires further study.

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Following excipients are mentioned in the study besides other: Eudragit L 100 − 55

Abdollahzadeh, R., Iranshahi, M., Akhgari, A. et al. Increasing the Stability of Pellets Containing Lycopene by Using Dual-Coating. J Pharm Innov 19, 50 (2024). https://doi.org/10.1007/s12247-024-09861-7

Read also our introduction article:

CPHI Milan 2024 – with a focus on excipients