Alshaya Hassa A, Alfahad Ahmed J, Alsulaihem Fatemah M, Aodah Alhassan H, Alshehri Abdullah A, Almughem Fahad A, Alfassam Haya A, Aldossary Ahmad M, Halwani Abdulrahman A, Bukhary Haitham A, Badr Moutaz Y, Massadeh Salam, Alaamery Manal, Tawfik Essam A
National Center of Biotechnology, Life Science and Environment Research Institute, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia.
KACST-BWH Centre of Excellence for Biomedicine, Joint Centers of Excellence Program, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia.
Pharmaceutics. 2022 Feb 4;14(2):358. doi: 10.3390/pharmaceutics14020358.
Geriatric patients are more likely to suffer from multiple chronic diseases that require using several drugs, which are commonly ingested. However, to enhance geriatric patients' convenience, the electrospun nanofiber system was previously proven to be a successful alternative for the existing oral dosage forms, i.e., tablets and capsules. These nanofibers prepared either as single- or multi-layered fibers could hold at least one active compound in each layer. They might also be fabricated as ultra-disintegrated fibrous films for oral cavity administration, i.e., buccal or sublingual, to improve the bioavailability and intake of the administered drugs. Therefore, in this work, a combination of nifedipine and atorvastatin calcium, which are frequently prescribed for hypertension and hyperlipidemia patients, respectively, was prepared in a coaxial electrospinning system for buccal administration. Scanning electron microscopy image showed the successful preparation of smooth, non-beaded, and non-porous surfaces of the drug-loaded nanofibers with an average fiber diameter of 968 ± 198 nm. In contrast, transmission electron microscopy distinguished the inner and outer layers of those nanofibers. The disintegration of the drug-loaded nanofibers was ≤12 s, allowing the rapid release of nifedipine and atorvastatin calcium to 61% and 47%, respectively, after 10 min, while a complete drug release was achieved after 120 min. In vitro, a drug permeation study using Franz diffusion showed that the permeation of both drugs from the core-shell nanofibers was enhanced significantly ( < 0.05) compared to the drugs in a solution form. In conclusion, the development of drug-loaded nanofibers containing nifedipine and atorvastatin calcium can be a potential buccal delivery system.
老年患者更有可能患有多种慢性病,需要服用多种常用药物。然而,为了提高老年患者用药的便利性,先前已证明电纺纳米纤维系统是现有口服剂型(即片剂和胶囊)的成功替代品。这些制备成单层或多层的纳米纤维每层可容纳至少一种活性化合物。它们也可以制成用于口腔给药(即颊部或舌下)的超崩解纤维膜,以提高所给药药物的生物利用度和摄入量。因此,在这项工作中,将分别常用于高血压和高脂血症患者的硝苯地平和阿托伐他汀钙组合,在同轴电纺系统中制备用于颊部给药。扫描电子显微镜图像显示成功制备了平均纤维直径为968±198nm的载药纳米纤维,其表面光滑、无珠粒且无孔隙。相比之下,透射电子显微镜区分了这些纳米纤维的内层和外层。载药纳米纤维的崩解时间≤12秒,10分钟后硝苯地平和阿托伐他汀钙的快速释放率分别达到61%和47%,120分钟后实现药物完全释放。体外使用Franz扩散池进行的药物渗透研究表明,与溶液形式的药物相比,两种药物从核壳纳米纤维中的渗透均显著增强(<0.05)。总之,含有硝苯地平和阿托伐他汀钙的载药纳米纤维的开发可能是一种潜在的颊部给药系统。