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李艳辉, 刘卫平, 李涛, 周颖倩, 陈园, 邹龙.冰片负载黄芪、三七总皂苷共载脂质体的制备及评价[J].湖南中医药大学学报英文版,2026,46(8):1559-1569.[Click to copy
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| 冰片负载黄芪、三七总皂苷共载脂质体的制备及评价 |
| 李艳辉,刘卫平,李涛,周颖倩,陈园,邹龙 |
| (长沙医学院, 湖南 长沙 410200;湖南中医药大学药学院, 湖南 长沙 410208) |
| 摘要: |
| 目的 构建冰片（Bor）负载黄芪总皂苷与三七总皂苷共载脂质体（Bor-TAS/PNS-Lip），建立其含量的测定方法，优化制备工艺并评价其理化性质及体外安全性。方法 采用高效液相色谱-蒸发光散射检测法（HPLC-ELSD）同时测定黄芪总皂苷（TAS）与三七总皂苷（PNS）含量，并进行专属性、线性关系、精密度、重复性、稳定性及加样回收率考察；薄膜分散-超声法制备Bor-TAS/PNS-Lip，以TAS和PNS包封率为评价指标，通过单因素试验结合Box-Behnken响应面法优化处方工艺；动态光散射法测定脂质体粒径、多分散性指数（PDI）及Zeta电位，并通过透射电子显微镜观察其形貌；评价脂质体的体外释放行为、溶血性能及细胞安全性。结果 HPLC-ELSD方法专属性良好，TAS和PNS在考察范围内线性关系良好（r＞0.999），精密度、重复性、稳定性及回收率均符合方法学要求。响应面分析结果表明，药脂比、磷脂胆固醇比及水化温度对脂质体包封率具有显著影响（P<0.05）。经Box-Behnken响应面法优化，确定最佳处方工艺条件为药脂比1∶23、磷脂胆固醇质量比7.6∶1、水化温度48 ℃。在此条件下制备的Bor-TAS/PNS-Lip中TAS和PNS包封率分别为75.37%±2.31%和63.37%±1.86%，平均粒径为（131.8±2.8） nm，PDI为（0.17±0.05），Zeta电位为（-22.93±0.81） mV。脂质体形态完整，具有良好的体外缓释性能。溶血率低于5%，空白脂质体在0.1～1.2 mg/mL浓度范围内对HT22细胞活性及乳酸脱氢酶释放均无明显影响，提示其具有良好的体外生物相容性。结论 建立的HPLC-ELSD含量测定方法准确可靠，优化所得Bor-TAS/PNS-Lip具有较高包封率、良好的理化稳定性、生物相容性及缓释性能，为Bor-TAS/PNS-Lip的制备及评价提供了实验依据。 |
| 关键词: 冰片|黄芪总皂苷|三七总皂苷|脂质体|响应面法 |
| DOI：10.3969/j.issn.1674-070X.2026.08.003 |
| Received:June 30, 2026 |
| 基金项目:湖南省自然科学基金项目（2026JJ81251）；湖南中医药大学研究生科研创新项目（2025CX092）。 |
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| Preparation and evaluation of borneol-loaded liposomes co-loaded with total Astragalus saponins and panax notoginseng saponins |
| LI Yanhui, LIU Weiping, LI Tao, ZHOU Yingqian, CHEN Yuan, ZOU Long |
| (Changsha Medical University, Changsha, Hunan 410200, China;School of Pharmacy, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China) |
| Abstract: |
| Objective To construct borneol-loaded liposomes co-loaded with total Astragalus saponins and Panax notoginseng saponins (Bor-TAS/PNS-Lip), establish a quantitative assay method, optimize the preparation procedure, and evaluate its physicochemical properties and in-vitro safety. Methods High-performance liquid chromatography coupled with evaporative light-scattering detection (HPLC-ELSD) was adopted for simultaneous determination of total Astragalus saponins (TAS) and panax notoginseng saponins (PNS). Methodological validations including specificity, linearity, precision, repeatability, stability, and sample-spiked recovery were performed. Bor-TAS/PNS-Lip was prepared by the film-hydration-sonication method. With the encapsulation efficiencies of TAS and PNS as evaluation indices, formulation and processing parameters were optimized by single-factor experiments combined with Box-Behnken response-surface methodology. The particle size, polydispersity index (PDI), and Zeta potential of liposomes were measured by dynamic light scattering, and the morphology was observed by transmission electron microscopy. In vitro release behavior, hemolytic property and cellular safety of liposomes were further evaluated. Results The established HPLC-ELSD method exhibited favorable specificity. TAS and PNS showed good linear relationships within the investigated concentration ranges (r>0.999). Precision, repeatability, stability, and recovery all met methodological requirements. Response surface analysis demonstrated that drug-to-lipid ratio, phospholipid-to-cholesterol ratio and hydration temperature exerted significant influences on encapsulation efficiency (P<0.05). The optimal formulation and technological conditions determined via Box-Behnken design were as follows: drug-to-lipid ratio of 1:23, phospholipid-to-cholesterol mass ratio of 7.6:1, and hydration temperature of 48 ℃. Under these conditions, the encapsulation efficiencies of TAS and PNS in Bor-TAS/PNS-Lip were 75.37%±2.31% and 63.37%±1.86%, respectively. The average particle size was (131.8±2.8) nm, PDI was (0.17±0.05), and Zeta potential was (22.93±0.81) mV. The liposomes possessed intact morphology and desirable in-vitro sustained-release performance. The hemolysis rate was lower than 5%. Blank liposomes showed no obvious effects on HT22 cell viability and lactate dehydrogenase release at concentrations ranging from 0.1 to 1.2 mg/mL, indicating favorable in-vitro biocompatibility. Conclusion The developed HPLC-ELSD assay is accurate and reliable. The optimized Bor-TAS/PNS-Lip possesses high encapsulation efficiency, satisfactory physicochemical stability, biocompatibility, and sustained-release property. It provides experimental evidence for the preparation and evaluation of borneol-loaded Bor-TAS/PNS-Lip. |
| Key words: borneol|total Astragalus saponins|Panax notoginseng saponins|liposomes|response surface methodology |
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