Massella Daniele, Leone Federica, Peila Roberta, Barresi Antonello A, Ferri Ada
Department of Applied Science and Technology, Politecnico di Torino, Corso duca degli Abruzzi 24, 10129 Turin, Italy.
University Lille Nord de France, F-5900 Lille, France.
J Funct Biomater. 2017 Dec 24;9(1):1. doi: 10.3390/jfb9010001.
Drug delivery by means of transdermal patches raised great interest as a non-invasive and sustained therapy. The present research aimed to design a patch for transdermal delivery of melatonin, which was encapsulated in polycaprolactone (PCL) nanoparticles (NPs) by employing flash nanoprecipitation (FNP) technique. Melatonin-loaded PCL nanoparticles were successfully prepared with precise control of the particle size by effectively tuning process parameters. The effect of process parameters on the particle size was assessed by dynamic light scattering for producing particles with suitable size for transdermal applications. Quantification of encapsulated melatonin was performed by mean of UV spectrophotometry, obtaining the estimation of encapsulation efficiency (EE%) and loading capacity (LC%). An EE% higher than 80% was obtained. Differential scanning calorimetry (DSC) analysis of NPs was performed to confirm effective encapsulation in the solid phase. Cotton fabrics, functionalized by imbibition with the nano-suspension, were analyzed by scanning electron microscopy to check morphology, adhesion and distribution of the NPs on the surface; melatonin transdermal release from the functionalized fabric was performed via Franz's cells by using a synthetic membrane. NPs were uniformly distributed on cotton fibres, as confirmed by SEM observations; the release test showed a continuous and controlled release whose kinetics were satisfactorily described by Baker-Lonsdale model.
通过透皮贴剂进行药物递送作为一种非侵入性的持续治疗方法引起了极大的关注。本研究旨在设计一种用于褪黑素透皮递送的贴剂，该褪黑素通过采用快速纳米沉淀（FNP）技术封装在聚己内酯（PCL）纳米颗粒（NPs）中。通过有效调整工艺参数，成功制备了载褪黑素的PCL纳米颗粒，并精确控制了粒径。通过动态光散射评估工艺参数对粒径的影响，以制备出适合透皮应用的具有合适尺寸的颗粒。通过紫外分光光度法对包封的褪黑素进行定量，获得包封效率（EE%）和载药量（LC%）的估计值。获得了高于80%的EE%。对纳米颗粒进行差示扫描量热法（DSC）分析，以确认在固相中有效包封。通过用纳米悬浮液浸渍功能化的棉织物，通过扫描电子显微镜分析来检查纳米颗粒在表面的形态、附着力和分布；通过使用合成膜，经由弗兰兹扩散池对功能化织物上的褪黑素进行透皮释放。扫描电子显微镜观察证实，纳米颗粒均匀分布在棉纤维上；释放试验显示出持续且可控的释放，其动力学可用贝克-朗斯代尔模型令人满意地描述。
