雨生红球藻油柔性纳米脂质体冻干粉的制备与评价  

Preparation and Evaluation of Flexible Nano Liposome Lyophilized Powder of Haematococcus Pluvialis Oil

作　　者：张雨凝 郑茗冉 贾海强 吴振[2] 刘智阳 王立强[1] ZHANG Yuning;ZHENG Mingran;JIA Haiqiang;WU Zhen;LIU Zhiyang;WANG Liqiang(School of Medicine,Huaqiao University,Quanzhou 362021,China;College of Pharmacy,Xiamen University,Xiamen 361000,China;Guizhou Zhongming Biotechnology Limited Company,Guiyang 550001,China)

机构地区：[1]华侨大学医学院,福建泉州362021 [2]厦门大学药学院,福建厦门361100 [3]贵州中铭生物科技有限公司,贵州贵阳550001

出　　处：《华侨大学学报（自然科学版）》2022年第6期769-776,共8页Journal of Huaqiao University(Natural Science)

基　　金：国家重点研发计划项目(2016YFE0101700);福建省高校产学合作重大项目(2019Y4007)。

摘　　要：采用熔融乳化法与冷冻干燥法制备雨生红球藻油柔性纳米脂质体冻干粉(Hpo-FNL-LP),并研究其包封率、载药量、粒径、Zeta电位、微观形态及稳定性.采用桨法测定Hpo-FNL-LP体外累积溶出率,扩散池法测定皮肤累计渗透量,高效液相色谱法(HPLC)法测定虾青素血药质量浓度.结果表明:Hpo-FNL-LP的包封率为(89.16±1.21)%,载药量为(1.34±0.04)%,粒径为(165.75±0.11)nm,Zeta电位为(-18.45±0.48)mV,微观形态为双层膜的圆形结构,稳定性较好;与雨生红球藻油乙醇溶液相比,Hpo-FNL-LP具有一定的缓释效果;Hpo-FNL-LP中虾青素24 h的皮肤累计渗透量达到(12.84±0.36)μg·cm^(-2),显著高于雨生红球藻油普通脂质体;与虾青素油溶液相比,Hpo-FNL-LP的t_(1/2)延长,ρ_(max)与AUC_(0-t)增大,相对生物利用度高达(422.53±3.30)%.The flexible nano liposome lyophilized powder of haematococcus pluvialis oil(Hpo FNL LP)was prepared by melt emulsification method and lyophilization method,and the encapsulation rate,drug loading amount,particle size,Zeta potential,microscopic morphology and stability were investigated.The cumulative dissolution rate of Hpo FNL LP in vitro was determined by paddle method.The cumulative skin penetration amount was determined by diffusion chamber method.The blood mass concentration of astaxanthin was determined by high performance liquid chromatography(HPLC)method.The results show that,the encapsulation rate of Hpo FNL LP is(89.16±1.21)%,the drug loading amount is(1.34±0.04)%,the particle size is(165.75±0.11)nm,and the Zeta potential is(-18.45±0.48)mV.The microscopic morphology shows a double layer circular structure with good stability.Compared with haematococcus pluvialis oil ethanol solution,Hpo FNL LP has a certain sustained release effect.The cumulative penetration amount of astaxanthin in Hpo FNL LP at 24 h reaches(12.84±0.36)μg·cm-2,which is significantly higher than that of haematococcus pluvialis oil ordinary liposome.Compared with the astaxanthin oil solution,the t_(1/2)of Hpo FNL LP extends,ρ_(max)and AUC_(0-t)both increase,and the relative bioavailability rate is as high as(422.53±3.30)%.

关 键 词：雨生红球藻油 柔性纳米脂质体 冻干粉 体外评价 药动学 

分 类 号：Q949.212.05[生物学—植物学] R94[医药卫生—药剂学]