Ginkgolide B-cyclodextrin inclusion complexes: an encapsulation strategy for improved solubility and aerosol inhalation therapy in bronchial asthma.

IF 6.9 3区 医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL
Drug Delivery and Translational Research Pub Date : 2026-10-01 Epub Date: 2026-03-13 DOI:10.1007/s13346-026-02075-z
Yuying Wang, MingLi Wei, Yan Zhang, Yuxin Liu, Xiaoshuang Bi, Xingting Fan, Jingxin Gou, Haibing He, Xing Tang, Yu Zhang, Tian Yin
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Abstract

Bronchial asthma represents a long-term inflammatory reaction in the airways, marked by the accumulation of eosinophils. Ginkgolide B (GB), derived from ginkgo biloba, serves as a potent natural antagonist of platelet activating factor (PAF). It can greatly reduce the production and release of eosinophils while minimizing the infiltration of other inflammatory cells in the airways, thus contributing to the management of bronchial asthma. However, due to its low bioavailability caused by poor water solubility and inherent bitter taste, it's hard for Ginkgolide B to meet the standards required for effective treatment of asthma. In this study, we developed two cyclodextrin derivatives of Ginkgolide B, namely GB-SBE-β-CD and GB-HP-γ-CD, for the therapy of bronchial asthma through aerosol inhalation. Both SBE-β-CD and HP-γ-CD effectively capsulated the Ginkgolide B. Molecular docking analysis revealed the spatial structure of GB-SBE-β-CD and GB-HP-γ-CD, highlighting hydrogen bonding as the primary driving force behind their formation. In vitro cell assays demonstrated that both Ginkgolide B and Ginkgolide B-cyclodextrin inclusion compounds exhibited good safety and potent anti-inflammatory activity. In addition, inhalation of aerosolized GB-SBE-β-CD and GB-HP-γ-CD markedly alleviated the symptoms of OVA-induced asthma in BALB/c mice, lowering infiltration of inflammatory cells, and significantly contributing to asthma treatment. The current findings suggest that the inhalation of Ginkgolide B-cyclodextrin represents a safe and promising option for managing bronchial asthma.

银杏内酯b -环糊精包合物:改善溶解度和雾化吸入治疗支气管哮喘的包封策略。
支气管哮喘是气道中的一种长期炎症反应,其特征是嗜酸性粒细胞的积累。银杏内酯B (Ginkgolide B, GB)来源于银杏叶,是一种有效的血小板活化因子(PAF)的天然拮抗剂。它可以大大减少嗜酸性粒细胞的产生和释放,同时最大限度地减少气道中其他炎症细胞的浸润,从而有助于支气管哮喘的治疗。然而,银杏内酯B由于水溶性差导致生物利用度低,且其固有的苦味,使得银杏内酯B很难达到有效治疗哮喘的标准。本研究开发了银杏内酯B的两种环糊精衍生物GB-SBE-β-CD和GB-HP-γ-CD,用于雾化吸入治疗支气管哮喘。SBE-β-CD和HP-γ-CD都能有效地封装银杏内酯b。分子对接分析揭示了GB-SBE-β-CD和GB-HP-γ-CD的空间结构,强调氢键是它们形成的主要驱动力。体外细胞实验表明,银杏内酯B和银杏内酯B-环糊精包合物均具有良好的安全性和抗炎活性。此外,吸入雾化的GB-SBE-β-CD和GB-HP-γ-CD可显著缓解ova诱导的BALB/c小鼠哮喘症状,降低炎症细胞的浸润,对哮喘治疗有显著作用。目前的研究结果表明,吸入银杏内酯b -环糊精是治疗支气管哮喘的一种安全且有前途的选择。
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来源期刊
Drug Delivery and Translational Research
Drug Delivery and Translational Research MEDICINE, RESEARCH & EXPERIMENTALPHARMACOL-PHARMACOLOGY & PHARMACY
CiteScore
11.70
自引率
1.90%
发文量
160
期刊介绍: The journal provides a unique forum for scientific publication of high-quality research that is exclusively focused on translational aspects of drug delivery. Rationally developed, effective delivery systems can potentially affect clinical outcome in different disease conditions. Research focused on the following areas of translational drug delivery research will be considered for publication in the journal. Designing and developing novel drug delivery systems, with a focus on their application to disease conditions; Preclinical and clinical data related to drug delivery systems; Drug distribution, pharmacokinetics, clearance, with drug delivery systems as compared to traditional dosing to demonstrate beneficial outcomes Short-term and long-term biocompatibility of drug delivery systems, host response; Biomaterials with growth factors for stem-cell differentiation in regenerative medicine and tissue engineering; Image-guided drug therapy, Nanomedicine; Devices for drug delivery and drug/device combination products. In addition to original full-length papers, communications, and reviews, the journal includes editorials, reports of future meetings, research highlights, and announcements pertaining to the activities of the Controlled Release Society.
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