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

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)%.