Mucoadhesive meloxicam-loaded nanoemulsions: Development, characterization and nasal applicability studies

黏膜黏附 鼻腔给药 生物利用度 药物输送 分散性 口腔给药 泊洛沙姆407 生物医学工程 材料科学 鼻粘膜 纳米技术 药理学 化学 色谱法 毒品携带者 泊洛沙姆 医学 高分子化学 复合材料 聚合物 共聚物 免疫学
作者
Bence Sipos,Ildikó Csóka,Nimród Szivacski,Mária Budai-Szűcs,Zsuzsanna Schelcz,István Zupkó,Piroska Szabó‐Révész,Balázs Volk,Gábor Katona
出处
期刊:European Journal of Pharmaceutical Sciences [Elsevier]
卷期号:175: 106229-106229 被引量:16
标识
DOI:10.1016/j.ejps.2022.106229
摘要

Intranasally administered non-steroidal anti-inflammatory drugs (NSAIDs) offer an innovative opportunity in the field of pain management. Combination of the nasal physiological advantages such as the rich vascularization and large absorption area along with novel nanomedical formulations can fulfill all the necessary criteria of an advanced drug delivery system. Nanoemulsions represent a versatile formulation approach suitable for nasal drug delivery by increasing the absorption and the bioavailability of many drugs for systemic and nose-to-brain delivery due to their stability, small droplet size and optimal solubilization properties. In this study we aimed to develop meloxicam (MX)-loaded mucoadhesive nanoemulsions and to investigate the nasal applicability of the optimized formulations. Our results indicated the optimized nanoemulsion formulation (MX-NE3) had a droplet size of 158.5 nm in monodisperse droplet size distribution (polydispersity index of 0.211). The surface charge was -11.2 mV, which helped with the colloidal stability upon dilution at simulated nasal conditions and storage. The high encapsulation efficiency (79.2%) mediated a 15-fold drug release and a 3-fold permeability increase at nasal conditions compared to the initial MX. Proper wetting properties associated with high mucoadhesion prosper the increased residence time on the surface of the nasal mucosa. No cytotoxic effect of the formulations was observed on NIH/3T3 mouse embryonic fibroblast cell lines, which supports the safe nasal applicability.
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