中国中药杂志2025，Vol.50Issue(23)：6550-6559,10.DOI:10.19540/j.cnki.cjcmm.20250916.304
小分子干凝胶多尺度结构提升冰片稳定性与生物利用度
Multiscale structure of small-molecule dry gels enhances stability and bioavailability of Borneolum Syntheticum
摘要
Abstract
The chemical instability of the core active components of Borneolum Syntheticum(borneol and isoborneol)is a key factor limiting its quality improvement.In this study,a series of small-molecule gelators based on a cholesterol skeleton were designed and synthesized,and the optimal gelator was selected through gelation-capacity-guided screening to construct a"Borneolum Syntheticum-gelator"dry gel self-assembly system.The preparation process of the dry gel was determined based on Borneolum Syntheticum loss rate,encapsulation efficiency,drug loading capacity,physicochemical characterization,and stability assessment.Results showed that dry gels were successfully formed at mass ratios of 1∶1 and 3∶1(Borneolum Syntheticum to gelator 2),with minimal Borneolum Syntheticum loss(0.7%and 0.8%).Corresponding encapsulation efficiencies and drug loading capacities reached 98.86%,98.96%and 49.76%,74.88%,respectively.IR and SEM analyses indicated that hydrogen bonding and other intermolecular forces drove the formation of multi-level fibrous network structures,with the 3∶1 ratio producing a more compact three-dimensional architecture.XRD and DSC confirmed the masking of Borneolum Syntheticum's crystalline structure and the formation of new phases in the dry gel system,suggesting that synergistic stabilization was achieved through crystalline transformation and effective encapsulation.Both formulations exhibited excellent stability under high temperature,high humidity,and intense light.The 3∶1 dry gel was selected for pharmacokinetic studies,revealing that the active components,borneol and isoborneol,in the dry gel exhibited prolonged retention time and more stable release profiles in vivo.This study provides new insights for improving the quality of easily degradable TCM components.关键词
多尺度结构/小分子胶凝剂/冰片挥发性/药效组分/药代动力学Key words
multi-scale structure/small-molecule gelator/Borneolum Syntheticum volatility/pharmacodynamic components/pharmacokinetics引用本文复制引用
ZHANG Kai-xuan,SHI Ya-jun,LIANG Yu-jie,JIANG Yi,LUAN Fei,SUN Lu,ZOU Jun-bo,FENG Liang..小分子干凝胶多尺度结构提升冰片稳定性与生物利用度[J].中国中药杂志,2025,50(23):6550-6559,10.基金项目
国家自然科学基金面上项目(82274105) （82274105）
陕西中医药大学科技创新人才体系建设计划项目(2024-CXTD-03) （2024-CXTD-03）
芳香中药产业化关键技术青年创新团队项目(2022-95) （2022-95）
陕西省重点研发计划项目-秦创原产业创新聚集区"四链"融合项目(2024CY-JJQ-36,2024CY-JJQ-78) （2024CY-JJQ-36,2024CY-JJQ-78）
西安市创新联盟技术攻关集群项目(23CXLHTJSGG0004-2023) （23CXLHTJSGG0004-2023）
