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目的:优选白桦脂酸醇质体的处方工艺参数,考察醇质体作为白桦脂酸经皮给药载体的可行性。方法:采用乙醇注入法制备白桦脂酸醇质体,以包封率为评价指标,通过正交试验考察白桦脂酸和磷脂的质量比、磷酸盐缓冲液pH和乙醇体积分数对白桦脂酸醇质体处方工艺的影响。利用透射电镜和激光粒径分析仪考察白桦脂酸醇质体的形态及粒径分布,采用Franz扩散池考察其体外经皮给药特性,并与脂质体和10%异丙醇溶液比较。运用HPLC测定白桦脂酸含量,检测波长207nm,流动相乙腈-0.1%冰乙酸(70∶30)。结果:最佳处方工艺为磷脂与白桦脂酸的质量比19∶1,磷酸盐缓冲液pH 7.4,乙醇体积分数30%;醇质体粒径94.3 nm,包封率86.3%;白桦脂酸醇质体12 h的累积经皮渗透量(108.33±10.26)μg·cm-2,分别是脂质体和10%异丙醇饱和溶液2.12倍和5.98倍。结论:醇质体作为经皮给药载体,能明显促进白桦脂酸的经皮渗透,效果优于脂质体,为五环三萜类化合物的抗肿瘤及抗获得性免疫缺陷综合症治疗提供新思路。
OBJECTIVE: To optimize the prescription parameters of betulinic acid ethosomes and investigate the feasibility of using ethosome as transdermal carrier of betulinic acid. Methods: Betulinic alcoplanes were prepared by ethanol injection. The entrapment efficiency was used as the evaluation index. The orthogonal test was conducted to evaluate the effect of the ratio of betulinic acid to phospholipid, the pH value of phosphate buffer and the volume fraction of ethanol on betulinic acid Impact of Plastid Prescription Technology. The morphology and particle size distribution of betulinic alcoplast were investigated by transmission electron microscopy and laser particle size analyzer. The in vitro transdermal administration characteristics of betulinic acid were compared with that of liposome and 10% isopropanol solution by Franz diffusion cell. The content of betulinic acid was determined by HPLC with the detection wavelength at 207nm and the mobile phase of acetonitrile-0.1% glacial acetic acid (70:30). Results: The optimal prescription was the mass ratio of phospholipid to betulinic acid 19:1, phosphate buffer pH 7.4, the volume fraction of ethanol 30%; the size of ethosomes 94.3 nm, encapsulation efficiency 86.3%; betulinic acid alcohol The transdermal permeation volume of plastids at 12 h was (108.33 ± 10.26) μg · cm-2, which was 2.12 and 5.98 times higher than that of the liposome and 10% isopropanol-saturated solutions respectively. CONCLUSION: As a transdermal delivery carrier, ethosomes can significantly promote the transdermal penetration of betulinic acid, which is superior to liposomes and provide antitumor and anti-ADHD treatment for pentacyclic triterpenoids New ideas.