中国兽医杂志2025，Vol.61Issue(3)：1-11,11.DOI:10.20157/j.cnki.zgsyzz.2025.03.001
转铁蛋白修饰辣蓼黄酮脂质体的制备和体外释放研究
Preparation and In Vitro Release Study of Transferrin-Modified Flavonoid of Polygonum hydropiper L.Liposomes
摘要
Abstract
In order to optimize the preparation process of transferrin(Tf)-modified flavonoid of Polygonum hydropiper L.(FPHL)liposomes(Tf-FPHL-Lip),and to clarify their characterization and in vitro release properties,this study first prepared FPHL liposomes(FPHL-Lip)using ethanol injection,thin-film dispersion,and reverse evaporation methods,and selected the method with the highest encapsulation efficiency.The preparation process of FPHL-Lip was optimized by evaluating the encapsulation efficiency as the key indicator through single-factor experiments and Box-Behnken response surface methodology.The Tf was connected to the liposomes using the active terminal carboxyl group of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[(polyethylene glycol)-2000]-carboxylic acid(DSPE-PEG2000-COOH)under a catalytic condition.The preparation process of Tf-FPHL-Lip was further optimized by single-factor experiments,and the morphology,particle size,polydispersity index(PDI),Zeta potential,and in vitro release were evaluated.The results showed that the optimal conditions for preparing Tf-FPHL-Lip using the thin-film dispersion method were a lipid-to-cholesterol ratio of 6.28∶1,a drug-to-lipid ratio of 1∶6.48,a preparation temperature of 58.48℃,a hydration volume of 15 mL,a surfactant concentration of 7.5 mg/mL,an sonication time of 6 minutes,a N-(carbonyl-methoxypolyethylene glycol 2000)-1,2-distearoyl-sn-glycerol-3-phosphoethanolamine,sodium salt(DSPE-MPEG2000)-to-phospholipid molar ratio of 6%,a DSPE-PEG2000-COOH-to-DSPE-MPEG2000 molar ratio of 5%,an 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride(EDC)-N-Hydroxysuccinimide(NHS)-DSPE-PEG2000-COOH molar ratio of 10∶10∶1,and a Tf-to-DSPE-PEG2000-COOH molar ratio of 1∶40.Under these optimized conditions,the prepared Tf-FPHL-Lip showed an average encapsulation efficiency of(63.35±3.41)%,an average particle size of(96.46±1.32)nm,an average PDI of 0.312±0.029,an average Zeta potential of(-2.02±0.22)mV,and an average conjugation rate of(68.64±0.07)%.The appearance was a pale yellow,clear,and transparent liquid,and the electron microscope showed a unilamellar liposome with a spherical shape,intact surface,and a particle size of approximately 100 nm.Compared to FPHL,the Tf-FPHL-Lip exhibited significant sustained-release behavior in vitro.The results suggest that the optimized preparation conditions are stable and feasible,and the prepared Tf-FPHL-Lip has a high encapsulation rate,small and uniform particle size,providing a theoretical foundation for further development and utilization of Tf-FPHL-Lip.关键词
辣蓼黄酮/转铁蛋白/脂质体/响应面法/表征/体外释放Key words
flavonoid of Polygonum hydropiper L./transferrin/liposome/response surface methodology/characterization/in vitro release分类
农业科技引用本文复制引用
吴昌旭,何家康,胡庭俊,于美玲,张金武,彭春子,吕茂杰,梁静,蒋凯屹,赖鹏羽,韦英益,陈海兰..转铁蛋白修饰辣蓼黄酮脂质体的制备和体外释放研究[J].中国兽医杂志,2025,61(3):1-11,11.基金项目
国家自然科学基金项目(32202850,32360894) （32202850,32360894）
广西自然科学基金面上基金项目(2021GXNSFAA196004) （2021GXNSFAA196004）
广西大学自然科学与技术创新发展倍增计划项目(2024BZRC013) （2024BZRC013）
