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载地塞米松的热敏原位凝胶和聚合物胶束用于眼部给药的比较研究。

Comparative Study of Dexamethasone-Loaded Thermoresponsive In Situ Gels and Polymeric Micelles for Ocular Drug Delivery.

作者信息

Szalai Boglárka, Jójárt-Laczkovich Orsolya, Kovács Anita, Berkó Szilvia, Sipos Bence, Katona Gábor, Budai-Szűcs Mária

机构信息

Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Street 6, H-6720 Szeged, Hungary.

出版信息

Int J Mol Sci. 2025 Aug 29;26(17):8414. doi: 10.3390/ijms26178414.

Abstract

Effective ocular drug delivery is still a challenge for pharmaceutical technologists due to the complex elimination mechanisms of the eye. In situ gels and polymeric micelles are among the pharmaceutical technologies that may enable us to overcome these challenges. Therefore, the objective of this study was to evaluate the ocular applicability of in situ gels and polymeric micelles, as well as their combinations, containing a steroidal anti-inflammatory drug, dexamethasone. The developed formulations were compared on the basis of their physicochemical characteristics, rheological behavior, mucoadhesion, in vitro drug release profile, and in vitro and ex vivo permeability. The developed formulations exhibited moderate stability according to the zeta potential measurements; however, they demonstrated appropriate mucoadhesion and sustained drug release. Furthermore, the results of the permeability studies suggest that combining thermoresponsive in situ gels and polymeric micelles represents a promising strategy for enhancing the therapeutic efficacy of ocular drug delivery.

摘要

由于眼睛复杂的清除机制,有效的眼部药物递送对药物技术专家来说仍然是一项挑战。原位凝胶和聚合物胶束属于可能使我们克服这些挑战的药物技术。因此,本研究的目的是评估含有甾体抗炎药地塞米松的原位凝胶和聚合物胶束及其组合的眼部适用性。根据其物理化学特性、流变行为、粘膜粘附性、体外药物释放曲线以及体外和离体渗透性对所开发的制剂进行比较。根据zeta电位测量,所开发的制剂表现出适度的稳定性;然而,它们表现出适当的粘膜粘附性和持续的药物释放。此外,渗透性研究结果表明,将热响应性原位凝胶和聚合物胶束相结合是提高眼部药物递送治疗效果的一种有前景的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0856/12428703/dc1ee16caf8d/ijms-26-08414-g001.jpg

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