SEDDS-loaded mucoadhesive fiber patches for advanced oromucosal delivery of poorly soluble drugs

黏膜黏附 口腔给药 药物输送 静电纺丝 生物相容性 聚丙烯酸 渗透(战争) 生物医学工程 乳状液 姜黄素 化学 纳米技术 材料科学 药理学 毒品携带者 聚合物 生物化学 有机化学 医学 工程类 运筹学
作者
Julian David Friedl,Marcel Walther,Pia Katharina Vestweber,Jana Wächter,Patrick Knoll,Arne Matteo Jörgensen,Andreas Bernkop‐Schnürch,Maike Windbergs
出处
期刊:Journal of Controlled Release [Elsevier]
卷期号:348: 692-705 被引量:12
标识
DOI:10.1016/j.jconrel.2022.06.023
摘要

To date, buccal administration of lipophilic drugs is still a major challenge due to their poor solubility in saliva and limited penetration into mucosal tissues. To overcome these limitations, we developed electrospun patches combining the benefits of mucoadhesive fibers and self-emulsifying drug delivery systems (SEDDS). The fiber system comprises a combination of mucoadhesive thiolated polyacrylic acid fibers and SEDDS-loaded fibers fabricated by parallel electrospinning. The resulting mucoadhesive electrospun SEDDS patches were systemically investigated for fiber characteristics, self-emulsification, mucoadhesion, drug penetration into porcine buccal tissue and biocompatibility. The patches showed high encapsulation efficiency for SEDDS without causing fiber defects or leakage. SEDDS incorporation enhanced the spinning process and reduced the fiber diameter and fiber size distribution. Hydration-dependent self-emulsification provided a controlled release of curcumin being encapsulated in nano-scaled o/w emulsion for over 3 h. Due to the thiolated polyacrylic acid fibers, the buccal residence time of patches was 200-fold prolonged. Further, they promoted a significantly increased drug penetration into buccal tissue compared to fiber patches without SEDDS. Finally, biocompatibility and improved therapeutic effects of curcumin-loaded patches on human keratinocytes and fibroblasts were confirmed. Mucoadhesive electrospun SEDDS patches represent a promising approach to overcome current challenges in the oromucosal delivery of lipophilic drugs to unlock their full therapeutic potential.
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