Development and evaluation of berberine-loaded bigel for the treatment of hyperpigmentation on B16F10 melanoma cell line

Abstract

Aim: The aim of this study was to optimize, develop, characterize and evaluate a topical nanobigel (BG) formulation containing Berberine (BRB) that exhibits anti-melanogenic properties. Materials & methods: The Berberine-loaded bigel (BRB@BG) formulation was prepared by homogenously mixing the optimized hydrogel and oleogel. BRB@BG was characterized in vitro and cytotoxicity study was conducted to evaluate its effects on murine skin melanoma B16F10 cell lines. Results: The optimized BRB@BG exhibited uniform texture with nanometric size, desirable spreadability and extrudability, suitable for topical applications. Cytotoxicity studies revealed that BRB@BG had a lower IC₅₀ value (4.84 μg/ml) on B16F10 cell lines compared with drug alone. Conclusion: In conclusion, the developed BRB@BG formulation showed good potential as safe and effective topical treatment for hyperpigmentation.

Plain language summary

Hyperpigmentation is a common skin disease in which the melanin content becomes abnormally high. The existing treatment options are associated with side effects and therefore research is being aimed to develop a topical nanoformulation based on natural compounds. Berberine (BRB) is one such natural compound that is known to inhibit the production of melanin in skin. This study was aimed to develop a bigel formulation of BRB that can be applied on skin, which can treat the hyperpigmentation and is safe. The developed nanomedicine was found to have all good properties of a topical formulation and was more effective than the drug alone. Various studies on animals were conducted to assess its safety and it was found that the formulation did not show any toxicity to the skin.

Article highlights

• Berberine, an isoquinoline alkaloid is reported to have antimelanogenic effect but is associated with poor oral bioavailability.

• Berberine-loaded bigel (BRB@BG) was prepared by homogenously mixing the optimized hydrogel and oleogel.

• The prepared BRB@BG was characterized using in vitro methods, TEM and trinocular microscopy.

• Cytotoxicity study was conducted to evaluate the effects of BRB@BG on the murine skin melanoma B16F10 cell lines.

• Safety of the developed formulation was performed using Draize test followed by histopathology and in ovo irritation studies.

• The developed formulation showed all desirable properties of an ideal topical formulation.

• The IC₅₀ values obtained after cytotoxicity studies was found to be lower than the plain drug showing better efficacy.

• The developed formulation showed no toxicity in any of the safety evaluation test.

Keywords: :

• berberine
• bigel
• cytotoxicity
• hydrogel
• hyperpigmentation
• oleogel

Supplemental material

Supplemental data for this article can be accessed at https://doi.org/10.1080/17435889.2024.2370759

Author contributions

Conceptualization: B Mangla, G Aggarwal; data curation: B Mangla, Z Ahamad, P Kumar; formal analysis: B Mangla, Z Ahamad; investigation: B Mangla, Z Ahamad, P Kumar; methodology: B Mangla, S Javed, W Ahsan; project administration: B Mangla, G Aggarwal; resources: B Mangla, S Javed, W Ahsan, G Aggarwal; software: B Mangla, G Aggarwal, S Javed, W Ahsan; supervision: B Mangla, G Aggarwal; validation: B Mangla, G Aggarwal, S Javed, W Ahsan; roles/writing – original draft: B Mangla, Z Ahamad, P Kumar, S Javed, W Ahsan; and Writing – review & editing: B Mangla, G Aggarwal, S Javed, W Ahsan.

Financial disclosure

The authors have no financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Competing interests disclosure

The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Writing disclosure

No writing assistance was utilized in the production of this manuscript.