Mohamed Abdelrahman, Korzhikov-Vlakh Viktor, Zhang Nan, Said André, Pilipenko Iuliia, Schäfer-Korting Monika, Zoschke Christian, Tennikova Tatiana
Institute of Chemistry, St. Petersburg State University, Universitetskii Pr. 26, Peterhoff, 198504 St. Petersburg, Russia.
Chemistry Department, Faculty of Science, Beni-Suef University, Salah Salem Street, Beni Suef 62511, Egypt.
Pharmaceutics. 2021 May 27;13(6):801. doi: 10.3390/pharmaceutics13060801.
A plethora of micro- and nanoparticle types are currently investigated for advanced ocular treatment due to improved drug retention times, higher bioavailability and better biocompatibility. Yet, comparative studies of both physicochemical and toxicological performance of these novel drug delivery systems are still rare. Herein, poly(L-lactic acid)- and poly(ε-caprolactone)-based micro- and nanoparticles were loaded with prednisolone as a model drug. The physicochemical properties of the particles were varied with respect to their hydrophilicity and size as well as their charge and the effect on prednisolone release was evaluated. The particle biocompatibility was assessed by a two-tier testing strategy, combining the EpiOcular eye irritation test and bovine corneal opacity and permeability assay. The biodegradable polyelectrolyte corona on the particles' surface determined the surface charge and the release rate, enabling prednisolone release for at least 30 days. Thereby, the prednisolone release process was mainly governed by molecular diffusion. Finally, the developed particle formulations were found to be nontoxic in the tested range of concentrations.
由于药物保留时间延长、生物利用度提高和生物相容性更好，目前正在研究大量的微米和纳米颗粒类型用于先进的眼部治疗。然而，对这些新型药物递送系统的物理化学和毒理学性能进行比较研究仍然很少。在此，以聚（L-乳酸）和聚（ε-己内酯）为基础的微米和纳米颗粒负载了泼尼松龙作为模型药物。颗粒的物理化学性质在亲水性、大小、电荷方面有所不同，并评估了其对泼尼松龙释放的影响。通过结合EpiOcular眼刺激试验和牛角膜混浊和通透性测定的两级测试策略评估颗粒的生物相容性。颗粒表面的可生物降解聚电解质冠层决定了表面电荷和释放速率，使泼尼松龙能够释放至少30天。因此，泼尼松龙的释放过程主要受分子扩散控制。最后，在所测试的浓度范围内，所开发的颗粒制剂被发现是无毒
