Tunçel Emre, Tort Serdar, Han Sevtap, Yücel Çiğdem, Tırnaksız Figen
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, Türkiye.
Department of Pharmacology, Faculty of Pharmacy, Gazi University, Ankara, Türkiye.
Drug Deliv Transl Res. 2025 Jun;15(6):2116-2145. doi: 10.1007/s13346-024-01728-1. Epub 2024 Oct 25.
With the developing manufacturing technologies, the use of 3D printers in microneedle production is becoming widespread. Hydrogel-forming microneedles (HFMs), a variant of microneedles, demonstrate distinctive features such as a high loading capacity and controlled drug release. In this study, the conical microneedle master molds with approximately 500 μm needle height and 250 μm base diameter were created using a Stereolithography (SLA) 3D printer and were utilized to fabricate composite HFMs containing diclofenac sodium. Using Box-Behnken Design, the effects of different polymers on swelling index and mechanical strength of the developed HFMs were evaluated. The optimum HFMs were selected according to experimental design results with the aim of the highest mechanical strength with varying swelling indexes, which was needed to use 20% Gantrez S97 and 0.1% (F22), 0.42% (F23), and 1% (F24) hyaluronic acid. The skin penetration and drug release properties of the optimum formulations were assessed. Ex vivo studies were conducted on formulations to determine drug penetration and accumulation. F24, which has the highest mechanical strength and optimized swelling index, achieved the highest drug accumulation in the skin tissue (17.70 ± 3.66%). All optimum HFMs were found to be non-cytotoxic by the MTT cell viability test (> 70% cell viability). In in vivo studies, the efficacy of the F24 was assessed for the treatment of xylene-induced ear edema by contrasting it to the conventional dosage form. It was revealed that HFMs might be an improved replacement for conventional dosage forms in terms of dermal diseases such as actinic keratosis.
随着制造技术的发展,3D打印机在微针生产中的应用越来越广泛。水凝胶形成微针(HFMs)作为微针的一种变体,具有高载药量和可控药物释放等独特特性。在本研究中,使用立体光刻(SLA)3D打印机制作了针高约500μm、基部直径250μm的锥形微针母模,并用于制造含双氯芬酸钠的复合HFMs。采用Box-Behnken设计,评估了不同聚合物对所制备HFMs溶胀指数和机械强度的影响。根据实验设计结果,选择了具有不同溶胀指数且机械强度最高的最佳HFMs,这需要使用20%的Gantrez S97和0.1%(F22)、0.42%(F23)和1%(F24)的透明质酸。评估了最佳配方的皮肤渗透和药物释放特性。对配方进行了体外研究以确定药物渗透和蓄积情况。机械强度最高且溶胀指数优化的F24在皮肤组织中实现了最高的药物蓄积(17.70±3.66%)。通过MTT细胞活力试验发现,所有最佳HFMs均无细胞毒性(细胞活力>70%)。在体内研究中,通过与传统剂型对比,评估了F24治疗二甲苯诱导的耳部水肿的疗效。结果表明,在治疗光化性角化病等皮肤病方面,HFMs可能是传统剂型的一种改进替代品。