Don Trong-Ming, Chen Michelle, Lee I-Chi, Huang Yi-Cheng
Department of Chemical and Materials Engineering, Tamkang University, No. 151 Yingzhuan Rd., Tamsui Dist., New Taipei City 251301, Taiwan.
Department of Food Science, National Taiwan Ocean University, No.2, Beining Rd., Zhongzheng Dist., Keelung City 20224, Taiwan.
Int J Biol Macromol. 2022 May 15;207:90-99. doi: 10.1016/j.ijbiomac.2022.02.127. Epub 2022 Feb 24.
Dissolving microneedles made from natural polymers recently have gained much attention as an efficient transdermal drug delivery system (TDDS). For the first time, ulvan, a sulfated polysaccharide extracted from Ulva lactuca, was applied to fabricate dissolving microneedles through a two-step casting method. The ulvan microneedles (UMNs) made from 4% ulvan solution were in a pyramidal shape with an average height of 655 μm and an aspect ratio of 2.63. The in vitro skin insertion study showed the UMNs could totally penetrate into the porcine skin to the dermis layer and rapidly dissolved as the needle height was reduced by 90.3% after post-insertion of only 2 min. The rapid dissolution of UMNs in situ thus could release the loaded model drugs of rhodamine 6G (R6G) and bovine serum albumin-fluorescein isothiocyanate conjugate (FITC-BSA) in the skin tissue. The in vitro drug release profiles through porcine skin revealed the UMNs markedly enhanced the cumulative release of FITC-BSA. In addition, the UMNs had good biocompatibility towards normal cells of HaCaT and NIH3T3. Briefly, this study demonstrates the rapidly dissolving UMNs could effectively carry the drug into skin and thus can be developed as a potential TDDS in the pharmaceutical and cosmeceutical fields.
近年来，由天然聚合物制成的可溶解微针作为一种高效的经皮给药系统（TDDS）备受关注。首次将从石莼中提取的硫酸化多糖——岩藻依聚糖，通过两步浇铸法应用于制备可溶解微针。由4%岩藻依聚糖溶液制成的岩藻依聚糖微针（UMNs）呈金字塔形状，平均高度为655μm，纵横比为2.63。体外皮肤插入研究表明，UMNs能够完全穿透猪皮至真皮层，并在插入仅2分钟后针高降低90.3%时迅速溶解。UMNs在原位的快速溶解因此能够在皮肤组织中释放负载的罗丹明6G（R6G）和牛血清白蛋白 - 异硫氰酸荧光素共轭物（FITC - BSA）模型药物。通过猪皮的体外药物释放曲线显示，UMNs显著提高了FITC - BSA的累积释放量。此外，UMNs对HaCaT和NIH3T3正常细胞具有良好的生物相容性。简而言之，本研究表明快速溶解的UMNs能够有效地将药物携带到皮肤中，因此可开发成为制药和化妆品领域潜在的经皮给药系统。
