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基于结冷胶的原位水凝胶用于载有利培酮的聚合物胶束的鼻腔给药

Gellan Gum-Based In Situ Hydrogels for Nasal Delivery of Polymeric Micelles Loaded with Risperidone.

作者信息

Sipos Bence, Budai-Szűcs Mária, Katona Gábor, Csóka Ildikó

机构信息

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

出版信息

Gels. 2025 May 28;11(6):404. doi: 10.3390/gels11060404.

Abstract

Nasal drug delivery faces numerous challenges related to the ineffectiveness of most nasal formulations without a mucoadhesive nature, prolonging residence time on the nasal mucosa. Another challenge is the low administrable dosage strength, which can be solved via nano-encapsulation techniques, including the utilization of polymeric micelles. In this study, gellan gum-cellulose derivative complex in situ gelling matrices were formulated to test their effect on the colloidal characteristics of polymeric micelles, their respective rheological behavior, and nasal applicability. It has been proven that these complex matrices can form gels upon contact with nasal fluid without disrupting the micellar structure. Changes in the drug release and permeation profile have been shown in a concentration-dependent manner to hinder the burst-like drug release profile of polymeric micelles. Formulations show concentration- and composition-dependent mucoadhesive features under nasal conditions. Most of the hydrogels possess a soft gel characteristic, making them suitable for nasal administration. In conclusion, this descriptive study provides useful insights for conscious, nasal dosage form design.

摘要

鼻腔给药面临诸多挑战,大多数无粘膜粘附性的鼻腔制剂效果不佳,难以延长在鼻粘膜上的停留时间。另一个挑战是可给药剂量强度低,这可通过纳米包封技术解决,包括利用聚合物胶束。在本研究中,制备了结冷胶 - 纤维素衍生物原位凝胶基质,以测试其对聚合物胶束胶体特性、各自流变行为和鼻腔适用性的影响。已证明这些复合基质在与鼻液接触时可形成凝胶,而不会破坏胶束结构。药物释放和渗透曲线的变化呈浓度依赖性,可阻碍聚合物胶束的突释型药物释放曲线。制剂在鼻腔条件下表现出浓度和组成依赖性的粘膜粘附特性。大多数水凝胶具有软凝胶特性,使其适合鼻腔给药。总之,这项描述性研究为有意识地设计鼻腔剂型提供了有用的见解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c518/12191529/f9901d160c9e/gels-11-00404-g001.jpg

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