Massaro Marina, Buscemi Gabriella, Arista Luca, Biddeci Giuseppa, Cavallaro Giuseppe, D'Anna Francesca, Di Blasi Francesco, Ferrante Angelo, Lazzara Giuseppe, Rizzo Carla, Spinelli Gaetano, Ullrich Thomas, Riela Serena
Dipartimento STEBICEF, Sez. Chimica, Università degli Studi di Palermo, Viale delle Scienze, Ed. 17, 90128 Palermo, Italy.
Global Discovery Chemistry, Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
ACS Med Chem Lett. 2018 Oct 22;10(4):419-424. doi: 10.1021/acsmedchemlett.8b00465. eCollection 2019 Apr 11.
A novel carrier system based on halloysite nanotubes (HNT), for the potential intraarticular delivery of kartogenin (KGN) by means laponite (Lap) hydrogel (HNT/KGN/Lap), is developed. The drug was first loaded into HNT, and the hybrid composite obtained was used as filler for laponite hydrogel. Both the filler and the hydrogel were thoroughly investigated by several techniques and the hydrogel morphology was imaged by transmission electron microscopy. Furthermore, the gelating ability of laponite in the presence of the filler and the rheological properties of the hybrid hydrogel were also investigated. The kinetic release of kartogenin from HNT and HNT/Lap hybrid hydrogel was studied both in physiological conditions and in synovial fluid. In the last case, the kinetic results highlighted that HNT carrier can effectively release KGN in a sustained manner for at least 38 days. Finally, a preliminary biological assays showed that the HNT/KGN/Lap hybrid hydrogel did not exhibit any cytotoxic effect.
开发了一种基于埃洛石纳米管（HNT）的新型载体系统，用于通过锂皂石（Lap）水凝胶（HNT/KGN/Lap）将软骨生成素（KGN）潜在地关节内递送。首先将药物加载到HNT中，所得的混合复合材料用作锂皂石水凝胶的填料。通过几种技术对填料和水凝胶进行了全面研究，并通过透射电子显微镜对水凝胶形态进行了成像。此外，还研究了锂皂石在填料存在下的凝胶化能力以及混合水凝胶的流变学性质。在生理条件和滑液中研究了软骨生成素从HNT和HNT/Lap混合水凝胶中的动力学释放。在后一种情况下，动力学结果突出表明，HNT载体可以持续有效地释放KGN至少38天。最后，初步生物学试验表明，HNT/KGN/Lap混合水凝胶没有表现出任何细胞毒性作用。
