Department of Biotechnology, Yonsei University, 262 Seongsanno, Seodaemun-gu, Seoul 120-749, Republic of Korea.
Biomaterials. 2011 Apr;32(11):3134-40. doi: 10.1016/j.biomaterials.2011.01.014. Epub 2011 Feb 2.
Dissolving microneedles, three-dimensional polymer structures with microscale cross-sectional dimensions, have been introduced as a means of safe transdermal drug delivery. Most dissolving microneedles have been fabricated using a traditional micro-casting method that cures biopolymers within three-dimensional mold, nevertheless, repeated molding process may cause damage to encapsulated drugs, a critical hurdle for clinical application. Here, we describe the stepwise controlled drawing technique that can directly fabricate dissolving microneedle from maltose by precise controlling the drawing time and the viscosity of the maltose. Controlled drawing shaped the particular sharp-conical microneedles of 1200 μm length with tip diameter of 60 μm, and dissolved within 20 min in-vivo after inserting to the skin. This technique surpasses the limitations of micro-casting for dissolving microneedle. Furthermore, transdermal delivery of impermeable hydrophilic molecules such as ascorbic acid-2-glucoside and niacinamide was confirmed as inhibition of cutaneous hypermelanosis. We anticipate that controlled drawing technique will be suitable to design dissolving microneedles for use in minimally invasive transcutaneous drug delivery to patients.
溶解微针是一种具有微尺度横截面尺寸的三维聚合物结构,已被引入作为安全经皮药物输送的一种手段。大多数溶解微针都是使用传统的微铸造方法制造的,该方法在三维模具中固化生物聚合物,然而,重复的成型过程可能会对封装药物造成损害,这是临床应用的一个关键障碍。在这里,我们描述了逐步控制拉伸技术,该技术可以通过精确控制拉伸时间和麦芽糖的粘度,直接从麦芽糖中制造出溶解微针。受控拉伸将麦芽糖成形为具有 1200μm 长度和 60μm 尖端直径的特殊尖锐锥形微针,在插入皮肤后 20 分钟内在体内溶解。该技术超越了微铸造对溶解微针的限制。此外,证实了不可渗透的亲水性分子(如抗坏血酸-2-葡萄糖苷和烟酰胺)的经皮传递可抑制皮肤过度色素沉着。我们预计,受控拉伸技术将适用于设计用于微创经皮药物输送给患者的溶解微针。