Taherzade Seyed Dariush, Rojas Sara, Soleimannejad Janet, Horcajada Patricia
Advanced Porous Materials Unit (APMU), IMDEA Energy, Av. Ramón de la Sagra 3, 28935 Móstoles-Madrid, Spain.
School of Chemistry, College of Science, University of Tehran, P.O. Box 14155-6455, Tehran 1417614411, Iran.
Nanomaterials (Basel). 2020 Nov 25;10(12):2296. doi: 10.3390/nano10122296.
Combined therapies emerge as an interesting tool to overcome limitations of traditional pharmacological treatments (efficiency, side effects). Among other materials, metal-organic frameworks (MOFs) offer versatilities for the accommodation of multiple and complementary active pharmaceutical ingredients (APIs): accessible large porosity, availability of functionalization sites, and biocompatibility. Here, we propose topical patches based on water-stable and biosafe Fe carboxylate MOFs (MIL-100 and MIL-127), the biopolymer polyvinyl alcohol (PVA) and two co-encapsulated drugs used in skin disorders (azelaic acid (AzA) as antibiotic, and nicotinamide (Nic) as anti-inflammatory), in order to develop an advanced cutaneous combined therapy. Exceptional MOF drug contents were reached (total amount 77.4 and 48.1 wt.% for MIL-100 and MIL-127, respectively), while an almost complete release of both drugs was achieved after 24 h, adapted to cutaneous delivery. The prepared cutaneous PVA-MOF formulations are safe and maintain the high drug-loading capacity (total drug content of 38.8 and 24.2 wt.% for MIL-100 and MIL-127, respectively), while allowing a controlled delivery of their cargoes, permeating through the skin to the active target sites. The total amount of drug retained or diffused through the skin is within the range (Nic), or even better (AzA) than commercial formulations. The presented results make these drug combined formulations promising candidates for new cutaneous devices for skin treatment.
联合疗法成为克服传统药物治疗局限性(疗效、副作用)的一种有趣工具。在其他材料中,金属有机框架(MOF)为容纳多种互补的活性药物成分(API)提供了多种功能:具有可利用的大孔隙率、功能化位点以及生物相容性。在此,我们提出基于水稳定且生物安全的铁羧酸盐MOF(MIL - 100和MIL - 127)、生物聚合物聚乙烯醇(PVA)以及两种用于皮肤疾病的共包封药物(壬二酸(AzA)作为抗生素,烟酰胺(Nic)作为抗炎药)的局部贴剂,以开发一种先进的皮肤联合疗法。达到了优异的MOF药物含量(MIL - 100和MIL - 127的总量分别为77.4 wt.%和48.1 wt.%),同时两种药物在24小时后几乎完全释放,适合皮肤给药。所制备的皮肤PVA - MOF制剂是安全的,并保持了高载药量(MIL - 100和MIL - 127的总药物含量分别为38.8 wt.%和24.2 wt.%),同时允许其负载物的可控释放,透过皮肤渗透到活性靶位点。通过皮肤保留或扩散的药物总量在范围内(Nic),甚至比市售制剂更好(AzA)。所呈现的结果使这些药物联合制剂成为用于皮肤治疗的新型皮肤装置的有前景的候选物。