Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Int J Nanomedicine. 2020 Nov 13;15:8933-8943. doi: 10.2147/IJN.S281158. eCollection 2020.
Gadodiamide (GDD) is a widely used magnetic resonance imaging (MRI) contrast agent. It is available only as intravenous injection. Unfortunately, it exhibits a high renal toxicity. In this respect, the author investigated the possibility of developing nanofibers (NFs, one-dimensional (1D) nanostructures) of GDD that would be promising for oral administration in intestinal imaging. NFs are prepared by electrospinning technique in which a strong electrostatic field is applied on a polymer solution.
NFs were prepared by coaxial electrospinning technique using Eudragit S100 (ES 100) as a shell layer and GDD loaded with polyvinylpyrrolidone K90 (PVP K90) and hydroxypropyl-beta-cyclodextrin (HP-β-CyD) as core fibers. Compatibility study of the NFs ingredients was attested through ATR and DSC investigations. Thermogravimetric analysis of NFs was done to insure its stability. In vitro release of GDD in the intestinal medium with different pH values was measured. In vitro cytotoxicity test was done to prove its safety. Additionally, stability of NFs to perform its function was examined by X-ray.
NFs experienced high entrapment efficiency of about 94.3% ± 3.1%. The ingredients of NFs were compatible through FT-IR and DSC study. The in vitro release data of GDD from coaxial NFs were slow (˂14%) in pH 1.2 till 2 h, while at pH 7.4 it showed burst release of about 12% in the first 2 min. Thermogravimetric analysis proved the NFs are stable. The in vitro cytotoxicity study proved the safety of NFs. Using mammography, the coaxial NFs behaved the same as GDD plain indicating its ability to be a contrasting agent.
Coaxial NFs of GDD as a core with PVP K90 and HP-β-CyD and ES 100 as a shell were stable and efficient as oral imaging dosage form for the intestine. It might be a prospective theranostic.
钆喷酸葡胺（GDD）是一种广泛应用于磁共振成像（MRI）的造影剂。它仅可通过静脉注射使用。不幸的是，它具有较高的肾毒性。在这方面，作者研究了开发 GDD 纳米纤维（NFs，一维（1D）纳米结构）的可能性，以便在肠道成像中进行口服给药。NFs 通过静电纺丝技术制备，其中在聚合物溶液上施加强静电场。
通过同轴静电纺丝技术制备 NFs，其中 Eudragit S100（ES 100）作为壳层，负载有聚维酮 K90（PVP K90）和羟丙基-β-环糊精（HP-β-CyD）的 GDD 作为芯纤维。通过 ATR 和 DSC 研究证明 NFs 成分的相容性。对 NFs 进行热重分析以确保其稳定性。在不同 pH 值的肠道介质中测量 GDD 的体外释放。进行体外细胞毒性试验以证明其安全性。此外，通过 X 射线检查 NFs 保持其功能的稳定性。
NFs 的包封效率约为 94.3%±3.1%。通过 FT-IR 和 DSC 研究证明 NFs 的成分具有相容性。在 pH 1.2 至 2 小时内，同轴 NFs 中 GDD 的体外释放数据较慢（˂14%），而在 pH 7.4 时，在前 2 分钟内显示约 12%的突释。热重分析证明 NFs 是稳定的。体外细胞毒性研究证明了 NFs 的安全性。通过乳房 X 光摄影，同轴 NFs 的行为与 GDD 素片相同，表明其有能力作为对比剂。
以 PVP K90 和 HP-β-CyD 为芯，以 ES 100 为壳的 GDD 同轴 NFs 是稳定且高效的肠道口服成像剂型。它可能是一种有前途的治疗诊断一体化药物。
