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灯盏花素新型给药系统的研究进展
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| 篇名： | 灯盏花素新型给药系统的研究进展 |
| TITLE： | Research progress in novel drug delivery systems of breviscapine |
| 摘要： | 灯盏花素（Bre）是灯盏细辛的黄酮类有效部位（其中灯盏乙素占90%以上），具有保护心血管和神经、抗肿瘤及调节免疫等药理作用。然而，Bre存在溶解度低、渗透率低、稳定性差与半衰期短等不足，严重制约了其临床应用。新型给药系统（NDDS）是可将增溶、促渗、缓/控释及靶向递送等多维技术复合实现药物高效递送的载体。本文系统总结了Bre-NDDS的研究进展，发现Bre-NDDS主要包括口服型（缓/控释给药系统、速释给药系统）、注射型（脂质体、固体脂质纳米粒、脂质乳剂、聚合物纳米粒、聚合物胶束）、黏膜递送型（鼻腔黏膜给药系统、口腔黏膜给药系统、肺部黏膜给药系统）以及透皮递送型，解析了不同Bre-NDDS的制备路径与体内外性能，提出了基于药代动力学/药效学的NDDS设计原则，可为高效、安全的Bre新制剂研发及产业化提供科学依据。 |
| ABSTRACT： | Breviscapine （Bre）， the effective flavonoid fraction extracted from Erigeron breviscapus ， contains more than 90% scutellarin. It exerts pharmacological effects including cardiovascular protection， neuroprotection， anti-tumor activity and immunomodulation. Nevertheless， Bre has several drawbacks such as low solubility， low permeability， poor stability and short half-life， which greatly restrict its clinical application. Novel drug delivery systems （NDDS） are carriers that integrate multi-dimensional technologies including solubilization， penetration enhancement， sustained/controlled release and targeted delivery to achieve efficient drug delivery. This paper systematically summarizes the research progress of Bre-NDDS， which mainly covers oral preparations （sustained/controlled-release drug delivery systems， immediate-release drug delivery systems）， injectable preparations （liposomes， solid lipid nanoparticles， lipid emulsions， polymeric nanoparticles， polymeric micelles）， mucosal delivery systems （nasal mucosal drug delivery systems， buccal mucosal drug delivery systems， pulmonary mucosal drug delivery systems） and transdermal delivery systems. The preparation routes as well as in vitro and in vivo performances of various Bre-NDDS are analyzed. The design principles for NDDS based on pharmacokinetics/pharmacodynamics are put forward， which can provide scientific evidence for the research， development and industrialization of high-efficiency and safe new Bre preparations. |
| 期刊： | 2026年第37卷第17期 |
| 作者： | 程玉钏；李伟泽；李宁；李媛媛；康瑞霞；吴丹 |
| AUTHORS： | CHENG Yuchuan，LI Weize，LI Ning，LI Yuanyuan，KANG Ruixia，WU Dan |
| 关键字： | 灯盏花素；溶解度；渗透性；生物利用度；新型给药系统 |
| KEYWORDS： | solubility;permeability;bioavailability;novel drug delivery systems |
| 阅读数： | 3 次 |
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