论文部分内容阅读
目的:优化盐酸倍他洛尔-蒙脱石脂质体(Mt-BH-LP)的处方及制备工艺,考察其体外释放性能和渗透性能。方法:采用乙醇注入法-硫酸铵梯度法制备Mt-BH-LP;以包封率和载药量为评价指标,采用正交试验优化Mt-BH-LP的处方;通过透析法考察Mt-BH-LP的体外释放性能;以家兔离体角膜为模型,采用体外改良的Franz扩散池法研究Mt-BH-LP的渗透性,以人永生化角膜上皮细胞(i HCEC)为模型,研究Mt-BH-LP的渗透性。结果:Mt-BH-LP处方工艺条件为卵磷脂-BH(5∶1),卵磷脂-胆固醇(9∶1),硫酸铵浓度0.15 mol·L~(-1),卵磷脂质量225 mg。Mt-BH-LP包封率(75.85±2.15)%,载药量(11.41±0.29)%,平均粒径(218±22.32)nm,Zeta电位(17.03±0.25)m V;体外释放试验表明Mt-BH-LP在10 h累计释放度达到60.2%,离体角膜透过试验结果表明Mt-BH-LP的角膜水化值[(76.72±2.68)%]在正常范围内。结论:采用乙醇注入法-硫酸铵梯度法制备的Mt-BH-LP包封率和载药量较高,缓释性能良好,具有良好的开发与应用前景。
OBJECTIVE: To optimize the formulation and preparation of the beta-tollol montmorillonite hydrochloride (Mt-BH-LP) liposome and study its in vitro release and permeation performance. Methods: Mt-BH-LP was prepared by ethanol injection-ammonium sulfate gradient method. Orthogonal test was used to optimize the formula of Mt-BH-LP with the encapsulation efficiency and drug loading as evaluation index. -LP in vitro; using rabbit cornea as a model, the permeability of Mt-BH-LP was studied by Franz diffusion cell method modified in vitro. The model of human immortalized corneal epithelial cells (i HCEC) -BH-LP permeability. Results: The technological conditions of Mt-BH-LP prescription were lecithin-BH (5:1), lecithin-cholesterol (9:1), ammonium sulfate concentration 0.15 mol·L -1 and lecithin 225 mg. The encapsulation efficiency of Mt-BH-LP was 75.85 ± 2.15%, the drug loading was 11.41 ± 0.29%, the average particle diameter was 218 ± 22.32 nm and the Zeta potential was 17.03 ± 0.25 mV. The corneal hydration value of Mt-BH-LP [(76.72 ± 2.68)%] was within the normal range when the cumulative release of BH-LP reached 60.2% at 10 h. CONCLUSION: Mt-BH-LP prepared by ethanol injection-ammonium sulfate gradient has high entrapment efficiency and drug loading, good sustained release performance and good prospect of development and application.