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Research Article

Quality-by-design-based development of ultradeformable nanovesicular transgelosome of standardized Piper longum extract for melanoma

    Debadatta Mohapatra

    Phytomedicine Research Laboratory, Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi, 221005, Uttar Pradesh, India

    ,
    Dulla Naveen Kumar

    Nanomedicine Research Laboratory, Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi, 221005, Uttar Pradesh, India

    ,
    Singh Shreya

    Phytomedicine Research Laboratory, Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi, 221005, Uttar Pradesh, India

    ,
    Dhananjay Panigrahi

    Dr. Reddy's Laboratories, Integrated Product Development, Bachupally (V&M), Medchal District, Telangana, 500090, India

    ,
    Ashish Kumar Agrawal

    Nanomedicine Research Laboratory, Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi, 221005, Uttar Pradesh, India

    &
    Alakh N Sahu

    *Author for correspondence: Tel.: +91 945 113 7862;

    E-mail Address: ansahu.phe@iitbhu.ac.in

    Phytomedicine Research Laboratory, Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi, 221005, Uttar Pradesh, India

    Published Online:https://doi.org/10.2217/nnm-2023-0069

    Background: Melanoma is the most aggressive and deadly form of skin cancer. The stratum corneum of the skin is a major obstacle to dermal and transdermal drug delivery. Ultradeformable nanovesicular transferosome has the capacity for deeper skin penetration and its incorporation into hydrogel forms a transgelosome that has better skin permeability and patient compliance. Method: Here, the quality-by-design-based development and optimization of nanovesicular transgelosome of standardized Piper longum fruit ethanolic extract (PLFEE) for melanoma therapy are reported. Results: Compared with standardized PLFEE-loaded plain gel, the transgelosome displayed optimal pharmaceutical properties and improved ex vivo skin permeability and in vivo tumor regression in B16F10 melanoma-bearing C57BL/6 mice. Conclusion: The results reflect the potential of transgelosome for melanoma therapy.

    Plain language summary

    Melanoma is a deadly form of skin cancer that originates from melanocytes in the skin. Skin is a major barrier to drug delivery. Transferosome is a liquid nanoformulation that has the capacity for deeper skin penetration. The transferosome was prepared from standardized Piper longum fruit ethanolic extract (PLFEE) and loaded into gel to form a transgelosome for improved skin application and patient compliance. Compared with extract-loaded plain gel, the transgelosome showed good pharmaceutical properties with better activity in melanoma (B16F10)-bearing female C57BL/6 mice. The therapeutic activity of the standard anticancer drug dacarbazine was improved with the prepared PLFEE transgelosome.

    Graphical abstract

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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