包封视黄醇棕榈酸酯和肌肽的二元神经酰胺醇质体的制备和性能  

Preparation and properties of binary ceramide modified ethosomes for encapsulation of retinol palmitate and carnosine

作　　者：梁蓉 贾利萍 杨成 LIANG Rong;JIA Liping;YANG Cheng(School of Chemical&Material Engineering,Jiangnan University,Wuxi 214122,Jiangsu,China;Key Laboratory of Synthetic and Biological Colloids,Ministry of Education,Jiangnan University,Wuxi 214122,Jiangsu,China)

机构地区：[1]江南大学化学与材料工程学院,江苏无锡214122 [2]江南大学合成与生物胶体教育部重点实验室,江苏无锡214122

出　　处：《精细化工》2025年第1期159-165,232,共8页Fine Chemicals

基　　金：国家重点研发计划项目(2016YFD0400801)。

摘　　要：为了提高醇质体的稳定性和经皮输送效果,采用无水乙醇/丙二醇(PG)混合物对视黄醇棕榈酸酯(RP)和肌肽(Car)进行包封,构建了RP-Car二元神经酰胺醇质体(RC醇质体)。结合粒径测定、TEM和激光共聚焦显微镜(CLSM)表征,考察了RC醇质体储藏稳定性和透皮性能。结果表明,当V(无水乙醇)∶V(PG)=6∶4时,制备的RC醇质体为较规则的球状囊泡,平均粒径为70 nm左右;RC醇质体中RP的包封率为80.28%±0.10%,Car的包封率为47.20%±0.71%;RC醇质体在4、25和45℃下储藏120 d时,粒径无明显变化,且在25℃下储藏120 d时RP和Car的保留率也无明显变化;RP和Car经醇质体包封后,在透皮实验中12 h皮肤的累积量为(0.273±0.002)和(22.521±0.280)μg/cm^(2),Car在皮肤的渗透量为(20.559±0.120)μg/cm^(2)。In order to improve the stability and transdermal efficacy of ethosomes,RP-Car binary ceramide modified ethosomes(RC alcoholsome)was synthesized by encapsulation of retinol palmitate(RP)and carnosine(Car)with ethanol absolute/propylene glycol(PG)mixture.The storage stability and transdermal properties were evaluated through particle size,TEM and confocal laser scanning microscopy(CLSM).The results showed that when the volume ratio of ethanol absolute to PG was 6∶4,the RC ethosomes presented as relatively regular spherical vesicles with a particle size of about 70 nm.And the encapsulation efficiency of RP and Car in the RC ethosomes was 80.28%±0.10%and 47.20%±0.71%,respectively.The particle size of RC ethosomes exhibited no significant changes after 120 d of storage at 4,25 and 45℃,while the retention rate of RP and Car in RC ethosomes also showed no significant changes after 120 d of storage at 25℃.After encapsulation with ethosomes,the amount of RP and Car accumulated for 12 h in the skin were(0.273±0.002)and(22.521±0.280)μg/cm^(2),respectively,while the skin permeability of Car increased to(20.559±0.120)μg/cm^(2).

关 键 词：神经酰胺 二元醇质体 视黄醇棕榈酸酯 肌肽 乙醇注入法 医药原料 

分 类 号：TQ658[化学工程—精细化工]