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目的研究丹皮酚(paeonol,PAE)脂质体凝胶制备及其体外透皮扩散。方法采用乙醇注入法制备PAE脂质体凝胶并对其物理特性进行研究;同时,采用Franz扩散池以大鼠皮肤进行体外经皮渗透实验,考察PAE脂质体凝胶的经皮渗透行为及皮内滞留药物量。结果制备的PAE脂质体凝胶包封率为78.62%,平均粒径为337 nm。体外经皮渗透实验表明,与PAE凝胶相比,其脂质体凝胶24 h内的累积渗透量为84.61μg/cm2,根据渗透动力学回归方程PAE脂质体凝胶累积渗透速度18.738μg/(cm2·h),透皮速率较慢;PAE脂质体凝胶、普通凝胶在凝胶内残留溶液浓度分别为2.550μg/ml、5.239μg/ml;PAE脂质体凝胶、普通凝胶在大鼠皮肤内残留溶液浓度分别为37.98μg/ml、17.99μg/ml,皮肤中药物滞留量明显增加。结论 PAE脂质体凝胶释放速率减慢,药物蓄积于皮肤内增多,对于治疗疾病有较多的释药量,达到长效持久抗炎效果,同时有利于避免丹皮酚因全身吸收而引起的副作用,可作为PAE临床应用的新剂型。
Objective To study the preparation and in vitro transdermal spread of paeonol (PAE) liposome gel. Methods PAE liposome gel was prepared by ethanol injection and the physical properties of PAE liposome gel were studied. At the same time, the percutaneous permeability of PAE liposome gel was investigated by Franz diffusion cell in vitro. Intradermal drug retention. Results The encapsulation efficiency of PAE liposome gel was 78.62% and the average particle size was 337 nm. In vitro transdermal permeation experiments showed that compared with PAE gel, the cumulative penetration of liposome gel in 24 h was 84.61μg / cm2. According to the equation of permeation kinetics, the cumulative penetration rate of PAE liposome gel was 18.738μg / (cm2 · h), the transdermal rate was slower; PAE liposome gel, gel in the gel residual concentration of 2.550μg / ml, 5.239μg / ml; PAE liposome gel, normal Gel residual concentration in rat skin were 37.98μg / ml, 17.99μg / ml, the skin drug retention was significantly increased. Conclusions The release rate of PAE liposome gel slows down, the accumulation of drug in the skin increases, and the release amount of PAE for the treatment of diseases is prolonged and long-lasting and anti-inflammatory effect is achieved. At the same time, it is beneficial to avoid the absorption of paeonol due to systemic absorption Side effects, can be used as PAE clinical application of new dosage forms.