Horvát Gabriella, Budai-Szűcs Mária, Berkó Szilvia, Szabó-Révész Piroska, Soós Judit, Facskó Andrea, Maroda Mónika, Mori Michela, Sandri Giuseppina, Bonferoni Maria Cristina, Caramella Carla, Csányi Erzsébet
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Department of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi fasor 10-11, H-6720 Szeged, Hungary.
Int J Pharm. 2015 Oct 15;494(1):321-8. doi: 10.1016/j.ijpharm.2015.08.024. Epub 2015 Aug 28.
Hyaluronic acid (HA) and its derivatives play important roles in many fields of therapy, such as arthritis treatment, plastic surgery, dermatology, otology, ophthalmology, etc. With a view to increase the beneficial properties of HA in ocular drug delivery, many types of chemical structural modifications have been performed. In the course of our research work, we characterized nanosized cross-linked - (CLNaHA), linear sodium hyaluronate (NaHA) and zinc-hyaluronate (ZnHA), as potential ocular drug delivery systems. The aim was to determine the influence of the structure on biocompatibility, mucoadhesion and drug release. The structure was characterized by means of rheology. The cytotoxicity of the samples was determined on rabbit corneal epithelial cells (RCE) by the MTT test. Mucoadhesion measurements were made by a rheological method in vitro and by tensile tests in vitro and ex vivo. The release of sodium diclofenac, a frequently used non-steroidal anti-inflammatory drug with low bioavailability, from the gels was determined with a vertical Franz diffusion cell. The results demonstrated that all three derivatives have adequate mucoadhesive properties and their rapid drug release profiles are beneficial in ocular therapy. Thanks to these properties, the bioavailability of the ophthalmic preparations can be increased, especially with the application of CLNaHA.
透明质酸（HA）及其衍生物在许多治疗领域发挥着重要作用，如关节炎治疗、整形手术、皮肤科、耳科、眼科等。为了增强HA在眼部药物递送中的有益特性，人们进行了多种类型的化学结构修饰。在我们的研究工作中，我们对纳米尺寸的交联透明质酸钠（CLNaHA）、线性透明质酸钠（NaHA）和锌透明质酸盐（ZnHA）进行了表征，将其作为潜在的眼部药物递送系统。目的是确定结构对生物相容性、粘膜粘附性和药物释放的影响。通过流变学方法对结构进行了表征。通过MTT试验在兔角膜上皮细胞（RCE）上测定了样品的细胞毒性。通过体外流变学方法以及体外和体内拉伸试验进行粘膜粘附性测量。使用垂直Franz扩散池测定了凝胶中双氯芬酸钠（一种常用的生物利用度低的非甾体抗炎药）的释放情况。结果表明，所有三种衍生物都具有足够的粘膜粘附特性，并且它们快速的药物释放曲线对眼部治疗有益。由于这些特性，可以提高眼科制剂的生物利用度，尤其是应用CLNaHA时。
