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 retinol palmitate and carnosine

摘要:

为了提高醇质体的稳定性和经皮输送效果,采用丙二醇和乙醇复配的方式构建了二元神经酰胺醇质体,并进一步选取脂溶性活性物——视黄醇棕榈酸酯(Retinol palmitate,RP)和水溶性活性物——肌肽(Carnosine,Car)制备了RP-Car二元神经酰胺醇质体,考察了其储藏稳定性和透皮性能。结果表明,当乙醇与丙二醇的体积比为6:4时,RP-Car二元神经酰胺醇质体的稳定性最好,其中RP的包封率为(80.28 ± 0.10)%,Car的包封率为(47.20 ± 0.71)%；TEM结果显示RP-Car神经酰胺二元醇质体是较为规则的球状囊泡,粒径为80 nm左右；该醇质体在4℃、25℃和45℃下储藏120天粒径无明显变化；体外透皮实验及激光共聚焦结果显示经包载后,RP和Car在皮肤中的累积量和渗透量均增加,其皮肤累积量分别为(0.273 ± 0.002)μg/cm2和(22.521 ± 0.280)μg/cm2,皮肤渗透量分别为0 μg/cm2和(20.559 ± 0.120)μg/cm2。

Abstract:

In order to improve the stability and transdermal efficacy of ethosomes, binary ceramide modified ethosomes was constructed by the combination of propylene glycol and ethanol. Furthermore, lipid soluble active substance, retinol palmitate (RP) and water-soluble active substance, carnosine (Car) were further selected to prepare RP-Car binary ceramide modified ethosomes (RP-Car binary cerethosomes), and the storage stability and transdermal properties were investigated. The results showed that when the volume ratio of ethanol to propylene glycol was 6:4, the encapsulation efficiency of RP in the RP-Car binary cerethosomes was (80.28 ± 0.10)%, and the encapsulation efficiency of Car was (47.20 ± 0.71)%; The TEM results showed that the RP-Car binary cerethosomes were relatively regular spherical vesicles with a particle size of about 70 nm; The RP-Car binary cerethosomes showed no significant changes after 120 days of storage at 4 ℃, 25 ℃ and 45 ℃; The results of in vitro transdermal experiment and laser confocal laser showed that the skin accumulation and permeability of RP and Car increased, and the skin accumulation was (0.273 ± 0.002) μg/cm2 and (22.521 ± 0.280) μg/cm2, respectively, the skin permeability was 0 μg/cm2 and (20.559 ± 0.120) μg/cm2, respectively.