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Microneedling-enhanced dermal delivery of catechin and curcuminoid polyphenols from gel, patch and ointment formulations

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Polyphenols exhibit a wide range of biological and pharmacological activities, yet their dermal delivery is often limited by skin permeability and formulation-dependent constraints. In this work, the potential of roller microneedling as a physical strategy to improve dermal delivery of representative polyphenols—epicatechin, epigallocatechin gallate (EGCG), and curcumin—was investigated using common topical dosage forms, namely polymeric gel, patch, and ointment. Standardized skin permeation parameters were first obtained using excised porcine skin under conditions of stratum corneum saturation. The microneedling procedure was characterized, and its effect on polyphenol transdermal permeation from each formulation type was evaluated using Franz diffusion cells. Maximum steady-state permeation fluxes varied from 13.2 μg/cm2/h (curcumin) to 708 μg/cm2/h (epicatechin). Roller microneedling produced well-defined microchannels across the stratum corneum, with a mean interchannel distance of 2.3 mm, without compromising skin integrity, and significantly enhanced polyphenol permeation from all tested vehicles. Depending on the compound and formulation, microneedling increased permeation fluxes and/or reduced lag times, with particularly relevant effects observed for gel-delivered curcumin and ointment-delivered EGCG. Moreover, the polyphenols exhibited a robust antioxidant activity (equivalent to micromolar ascorbic acid) after transdermal permeation, including following microneedle-assisted delivery, supporting the compatibility of microneedling and the formulation vehicles with polyphenol functionality. Overall enhancement factors were consistent, yielding approximately twofold increases in both permeation flux and antioxidant activity. These findings demonstrate that roller microneedling is a practical, low-invasive approach to enhance the dermal delivery of polyphenols from conventional topical formulations, offering a versatile strategy that complements formulation-based optimization for therapeutic and cosmetic applications.

Descrição

Article number - 108928.
Acknowledgments and Funding: This work was supported by Fundação para a Ciência e Tecnologia (FCT-Portugal) through the project PTDC/BIA-MIB/31864/2017. The research was also supported by FCT/MCTES through national funds to the research units: LSRE-LCM, UID/50020/2025 (DOI: 10.54499/UID/50020/2025); and ALiCE, LA/P/0045/2020 (DOI: 10.54499/LA/P/0045/2020).

Palavras-chave

Alginate Curcuminoids Drug delivery Flavonoids Medical devices Pluronic F-127

Contexto Educativo

Citação

Violante, C., Marques-da-Silva, D., & Lagoa, R. (2026). Microneedling-enhanced dermal delivery of catechin and curcuminoid polyphenols from gel, patch and ointment formulations. Journal of Drug Delivery Science and Technology, 127, Artigo 108928. https://doi.org/10.1016/j.jddst.2026.108928

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