Department of Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea; Juvic Inc., Yonsei Engineering Research Park, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
Department of Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
Carbohydr Polym. 2018 Jan 15;180:297-303. doi: 10.1016/j.carbpol.2017.10.044. Epub 2017 Oct 13.
A dissolving microneedle (DMN) patch encapsulated with ascorbic acid 2-glucoside (AA2G) in a needle-shaped hyaluronic acid (HA) backbone was fabricated and sterilized by electron beam (e-beam, 5-40kGy) and gamma ray (γ-ray, 5-30kGy). DMN structures maintained their morphologies and fracture force regardless of e-beam and γ-ray irradiation doses. Both e-beam (40kGy) and γ-ray (20 and 30kGy) met the product sterility requirements for cosmetics and vaccines; however, γ-ray irradiation significantly degraded the encapsulated AA2G, while e-beam maintained AA2G activity. Thus, an e-beam dose of 40kGy, which satisfied the sterility requirements without loss of AA2G, is suitable for terminal sterilization of DMNs. Moreover, we confirmed that the optimized irradiation (e-beam, 40kGy) did not affect dissolution rate and drug release profile of DMNs. Further, we confirmed that HA, the backbone polymer of DMNs, could be utilized as a stabilizer that inhibits degradation of encapsulated AA2G by irradiation. This detailed analysis can be developed further to optimize various biological drugs in transdermal drug delivery systems.
一种载有抗坏血酸 2-葡萄糖苷(AA2G)的可溶解微针(DMN)贴片,其以针状透明质酸(HA)为骨架,通过电子束(e 射线,5-40kGy)和伽马射线(γ射线,5-30kGy)进行了封装和消毒。DMN 结构无论接受何种剂量的 e 射线和γ射线辐射,其形态和断裂力都能得以保持。E 射线(40kGy)和γ射线(20 和 30kGy)均符合化妆品和疫苗的产品无菌要求;然而,γ射线辐照会显著降解包封的 AA2G,而 e 射线则能保持 AA2G 的活性。因此,40kGy 的 e 射线剂量既能满足无菌要求,又不会损失 AA2G,适用于 DMNs 的最终灭菌。此外,我们证实经过优化的辐照(e 射线,40kGy)不会影响 DMN 的溶解速率和药物释放特性。进一步的,我们证实了 DMN 的骨架聚合物透明质酸可以作为一种稳定剂,抑制辐照对包封 AA2G 的降解。这种详细的分析可以进一步发展,以优化各种用于透皮给药系统的生物药物。