Highly stable and fast-dissolving ascorbic acid-loaded microneedles.

Autor: Leelawattanachai J; National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand., Panyasu K; National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand., Prasertsom K; National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand., Manakasettharn S; National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand., Duangdaw H; Department of Chemical Engineering, Faculty of Engineering, Mahidol University, Nakhon Pathom, Thailand., Budthong P; Department of Pharmaceutical Sciences, Faculty of Pharmacy, Srinakharinwirot University, Nakhon Nayok, Thailand., Thepphornbanchakit N; Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand., Chetprayoon P; Toxicology and Bio Evaluation Service Center (TBES), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand., Muangnapoh K; National Metal and Material Technology Center (MTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand., Srinives S; Department of Chemical Engineering, Faculty of Engineering, Mahidol University, Nakhon Pathom, Thailand., Waraho-Zhmayev D; Biological Engineering Program, Faculty of Engineering, King Mongkut's University of Technology Thonburi, Bangkok, Thailand., Triampo D; Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Mahidol University, Nakhon Pathom, Thailand.
Jazyk: angličtina
Zdroj: International journal of cosmetic science [Int J Cosmet Sci] 2023 Oct; Vol. 45 (5), pp. 612-626. Date of Electronic Publication: 2023 May 18.
DOI: 10.1111/ics.12865
Abstrakt: Objectives: Ascorbic acid has many benefits to the skin. Numerous attempts to promote its topical delivery show great challenges since its chemical instability and poor skin impermeability. Microneedle delivery is a simple, safe, painless and effective means to deliver therapeutic or nourishing molecules into the skin. The purpose of this study was twofold: (a) to develop a new formulation of ascorbic acid-loaded microneedles to enhance ascorbic acid stability by investigating an optimal amount of polyethyleneimine as an additive to the dextran-based microneedle formulation and (b) to assess microneedle properties in terms of dissolving rate, skin penetration ability, biocompatibility and antimicrobial activity.
Methods: The microneedles formulated with ascorbic acid and varied polyethyleneimine concentrations were fabricated and subsequently tested for ascorbic acid stability using 2,2-diphenyl-1-picrylhydrazyl assay. The dissolution rate and skin penetration depth were investigated in porcine skin and the reconstructed human full-thickness skin model respectively. The skin irritation tests were done according to the Organisation for Economic Co-operation and Development Test Guideline No. 439. An antimicrobial disc susceptibility test was performed against Escherichia coli, Staphylococcus aureus and Staphylococcus epidermidis.
Results: Among varied amounts of 0%, 1.5%, 3.0% and 4.5% (w/v), the 3.0% polyethyleneimine showed the most desirable characteristics, including well-preserved shape integrity after demoulding, significantly improved stability of ascorbic acid (p < 0.001) from 33% to 96% antioxidant activity after 8 weeks of storage at 40°C, increased dissolving rate (p < 0.001) by being completely dissolved within 2 min after the skin insertion, passing skin penetration and biocompatibility tests as well as having a broad spectrum of antimicrobial property.
Conclusion: With a safety profile and enhanced properties, the new formulation of ascorbic acid-loaded microneedles shows outstanding potential as commercially available cosmetics and healthcare products.
(© 2023 Society of Cosmetic Scientists and Societe Francaise de Cosmetologie.)
Databáze: MEDLINE
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