盐酸倍他洛尔-蒙脱石脂质体的制备与性能考察

李娟; 侯冬枝; 胡晟; 黄燚; 田双艳; 陈燕忠; 吕竹芬; 段豪云; 周庆军

doi:10.13422/j.cnki.syfjx.2017230007

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盐酸倍他洛尔-蒙脱石脂质体的制备与性能考察

药剂与炮制 | 更新时间：2024-01-04

- 盐酸倍他洛尔-蒙脱石脂质体的制备与性能考察
- Preparation and Properties of Montmorillonite-betaxolol Hydrochloride Liposomes
- 中国实验方剂学杂志 2017年23卷第23期页码：7-12
- 作者机构：
- 作者简介：
- 基金信息：
  
  国家自然科学基金项目（51102052）;广东省医学科学技术研究项目（A2016275）
- DOI：10.13422/j.cnki.syfjx.2017230007
  中图分类号： R943
- 纸质出版日期：2017
- 稿件说明：
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李娟, 侯冬枝, 胡晟, 等. 盐酸倍他洛尔-蒙脱石脂质体的制备与性能考察[J]. 中国实验方剂学杂志, 2017,23(23):7-12.

LI Juan, HOU Dong-zhi, HU Sheng, et al. Preparation and Properties of Montmorillonite-betaxolol Hydrochloride Liposomes[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(23): 7-12.
李娟, 侯冬枝, 胡晟, 等. 盐酸倍他洛尔-蒙脱石脂质体的制备与性能考察[J]. 中国实验方剂学杂志, 2017,23(23):7-12. DOI： 10.13422/j.cnki.syfjx.2017230007.

LI Juan, HOU Dong-zhi, HU Sheng, et al. Preparation and Properties of Montmorillonite-betaxolol Hydrochloride Liposomes[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(23): 7-12. DOI： 10.13422/j.cnki.syfjx.2017230007.

摘要

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（iHCEC）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） mV；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。

Abstract

Objective: To optimize formulation and preparation technology of montmorillonite-betaxolol hydrochloride liposomes (Mt-BH-LP)

and evaluate its in vitro release performance and permeability. Method: Mt-BH-LP was prepared by ethanol injection combined with ammonium sulfate gradient method.With composite score of encapsulation efficiency and drug loading as index

Orthogonal test was used to optimize the formulation.The in vitro release of Mt-BH-LP was detected by dialysis method.With isolated corneas of rabbit as a model

the in vitro modified Franz diffusion cell method was used to measure the permeability of Mt-BH-LP.The permeability of Mt-BH-LP was further studied by taking human immortalized corneal epithelial cells (iHCEC) as model. Result: Optimum prescription was as following:ammonium sulfate concentration of 0.15 moL·L-1

lecithin quality of 225 mg

lecithin-BH (5:1)

lecithin-cholesterol (9:1).Encapsulation efficiency of Mt-BH-LP was (75.85±2.15)%

its drug loading

average particle size and Zeta potential were (11.41±0.29)%

(218±22.32) nm and (17.03±0.25) mV

respectively.The cumulative release of Mt-BH-LP was 60.2% in 10 h

the corneal hydration value of Mt-BH-LP was (76.72±2.68)% within the normal range. Conclusion: Mt-BH-LP prepared by optimized formulation has high encapsulation efficiency and drug loading

which displays good sustained-release performance

and it has a good development of application prospect.

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