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| 穿心莲内酯纳米结构脂质载体滴眼液的制备及体内外评价 |
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陈亚男1,2,3, 林芸1,2,3, 赵梦菲1,2,3, 刘晏玲1,2,3, 谢昊楠1,2,3, 邓秀平2,3, 李佳玮1,2,3, 刘志东1,2,3
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1.天津中医药大学中药学院, 天津 301617;2.现代中药发现与制剂技术教育部工程研究中心, 天津 301617;3.组分中药国家重点实验室, 天津 301617
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| 摘要: |
| [目的] 制备穿心莲内酯纳米结构脂质载体滴眼液（AG-NLCs），并对其进行体内外评价。[方法] 研究采用溶剂注入法制备AG-NLCs，测定其包封率、载药量、粒径、电位等，用透射电镜观察形态，并以穿心莲内酯眼用凝胶（AG-Gel）及穿心莲内酯原料药混悬液（AG）为参比制剂，进行体外释放、离体角膜渗透研究，体内兔眼微渗析动力学及组织分布研究。[结果] AG-NLCs包封率为（79.98±0.75）%，载药量为（0.36±0.03）%，粒径为（15.64±0.97） nm，多分散指数（PDI）为（0.193±0.013），电位为（1.05±0.00） mV，电镜下为均匀圆形颗粒。AG-NLCs、AG-Gel的体外释放速率明显优于AG，AG-NLCs、AG-Gel的3 h药物累积渗透量分别是AG的6.18倍（P<0.01）和4.69倍（P<0.05）；AG-NLCs的表观渗透系数（Papp）分别是AG-Gel的7.27倍（P<0.01）和AG的13.55倍（P<0.01）；AG-NLCs给药，其AUC0-8 h分别是AG-Gel的2.49（P<0.05）和AG的5.21倍（P<0.01），且有更强的组织停留能力。[结论] 与参比制剂相比，纳米结构脂质载体滴眼液的应用可以改善穿心莲内酯眼部生物利用度。 |
| 关键词: 穿心莲内酯 纳米结构脂质载体 微渗析药动学 组织分布 |
| DOI：10.11656/j.issn.1673-9043.2026.09.06 |
| 分类号:R285.5 |
| 基金项目: |
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| Preparation and in vitro/in vivo evaluation of andrographolide nano-structured lipid carrier eye drops |
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CHEN Yanan1,2,3, LIN Yun1,2,3, ZHAO Mengfei1,2,3, LIU Yanling1,2,3, XIE Haonan1,2,3, DENG Xiuping2,3, LI Jiawei1,2,3, LIU Zhidong1,2,3
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1.School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China;2.Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China;3.State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China
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| Abstract: |
| [Objective] To prepare Andrographolide-loaded nanostructured lipid carrier（AG-NLC） eye drops and evaluate them in vitro and in vivo. [Methods] In this study，AG-NLCs were prepared using the solvent injection method. Their encapsulation efficiency，drug loading，particle size，and zeta potential were determined. Morphology was observed using transmission electron microscopy. In vitro release and ex vivo corneal permeation studies were conducted using Andrographolide ophthalmic gel（AG-Gel） and an andrographolide API suspension（AG） as reference formulations，in vivo microdialysis kinetics and tissue distribution studies in rabbit eyes. [Results] The encapsulation efficiency of AG-NLCs was（79.98±0.75）%，drug loading was（0.36±0.03）%，particle size was（15.64±0.97） nm，the polydispersity index（PDI） was（0.193±0.013），the zeta potential was（1.05±0.00） mV，and the particles appeared as uniform spherical particles under electron microscopy. The in vitro release rates of AG-NLCs and AG-Gel were significantly superior to those of AG；the cumulative drug permeation at 3 h for AG-NLCs and AG-Gel was 6.18 times（P<0.01） and 4.69 times（P<0.05） that of AG，respectively；The apparent permeability coefficients（Papp） of AG-NLCs were 7.27 times that of AG-Gel（P<0.01） and 13.55 times that of AG（P<0.01）；Following administration of AG-NLCs，the AUC0-8 values were 2.49 times（P<0.05） that of AG-Gel and 5.21 times（P<0.01） that of AG，and AG-NLCs demonstrated greater tissue retention capacity. [Conclusion] Compared with the reference formulation，the use of nanostructured lipid carrier eye drops can improve the ocular bioavailability of andrographolide. |
| Key words: andrographolide nanostructured lipid carrier microdialysis pharmacokinetics tissue distribution |
