雷公藤红素醇质体的制备及体外透皮性能研究(3)

　　本研究通过考察磷脂含量、乙醇体积分数、胆

　　试验号p包封率/%

　　1 80.0

　　2 80.5

　　3 81.2

　　d 粒径/nm

　　394.9

　　404.0

　　404.7

　　VZeta /mV

　　-2.55

　　-3.15

　　-2.55

　　IPDI

　　0.186

　　0.229

　　0.215

　　表4 Cel 醇质体粒径、PDI、电位和包封率

　　Table 4 The particle size， PDI， zeta potential andencapsulation efficiency of celastrol ethosomest ／min

　　组别

　　Cel 溶液

　　空白醇质体/Cel 溶液

　　Cel 醇质体

　　累积渗透方程

　　Q=0.439 9 t-2.229

　　Q=1.090 1 t-7.068

　　Q=1.640 9 t-9.154 5

　　J ／ （μg·cm-2·h-1）

　　0.439 9

　　1.090 1

　　1.640 9

　　r

　　0.990 3

　　0.956 1

　　0.965 1

　　表5 Cel 醇质体、空白醇质体/Cel 溶液及Cel 溶液的体外渗透比较

　　Table 5 Comparison of transdermal permeation property invitro between celastrol ethosomes, blank ethosomes /celestrol solution and celestrol solution广州中医药大学学报2015 年第32 卷

　　Cumulative amount permeated（μg/cm2）

　　932

　　Study on Preparation of Celastrol Ethosome and Its Skin PenetrationProperties in Vitro

　　WU Jun， WU Ming， LIU Di， MA Zhuo

　　（Hubei University of Technology， Wuhan 430068 Hubei， China）Abstract： Objective To prepare celastrol ethosomes and to observe the permeability characteristics of theethosomes which act as the transdermal delivery carriers of celastrol in vitro. Methods Celastrol ethosomes wereprepared by ethanol injection method， and then the encapsulation efficiency， particle size， polydispersity index(PDI) and zeta potential of the ethosomes were analyzed. TP2A intelligent percutaneous penetration instrumentwas used to compare the skin penetration properties of celastrol ethosomes， celastrol solution and the mixture ofblank ethosomes with celastrol solution. Results The prepared celastrol ethosomes were spherical， and theaverage particle size was (401.3 ± 5.5) nm， PDI was 0.21± 0.02， steady zeta potential was (-2.75 ± 0.1) mV，and average encapsulation efficiency was (80.6 ± 0.7) %. The amount of accumulative penetration of celastrolethosomes at 48 h was 76.86 μg·cm -2 and the permeation rate was 1.640 9 μg·cm -2·h -1， which weresignificantly higher than the celastrol solution and the mixture of blank ethosomes with celastrol solution.

　　Conclusion The prepared ethosomes have high encapsulation efficiency， uniform particle size and stablequality， and are beneficial to the transdermal absorption of celastrol.

　　Key words： Celastrol/production & preparation； Ethosomes/ultrastructure；Encapsulation efficiency； Percutaneous penetration in vitro；Disease models， animal； Mice

　　固醇含量及Cel 含量对醇质体稳定性及包封率的影响， 以“正交设计” 筛选出了最优处方； 并通过比较Cel 醇质体、空白醇质体/Cel 溶液及Cel 溶液体外累积渗透量的差异， 表明醇质体有利于Cel 的渗透， 为Cel 的临床用药新剂型提供了相关依据及参考。

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