Preparation and Formula Optimization of Harmine-loaded Ethosomes

MA Ting-yun; JIANG Ji-zong; ZHANG Liu-hong; CHENG Xue-mei; WANG Chang-hong

doi:10.13422/j.cnki.syfjx.20180805

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Preparation and Formula Optimization of Harmine-loaded Ethosomes

更新时间：2024-01-04

- Preparation and Formula Optimization of Harmine-loaded Ethosomes
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 24, Issue 8, Pages: 34-39(2018)
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- DOI：10.13422/j.cnki.syfjx.20180805
  CLC： R283.6
- Published：2018
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MA Ting-yun, JIANG Ji-zong, ZHANG Liu-hong, et al. Preparation and Formula Optimization of Harmine-loaded Ethosomes[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(8): 34-39.
DOI：

MA Ting-yun, JIANG Ji-zong, ZHANG Liu-hong, et al. Preparation and Formula Optimization of Harmine-loaded Ethosomes[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(8): 34-39. DOI： 10.13422/j.cnki.syfjx.20180805.

摘要

目的：制备去氢骆驼蓬碱醇质体并对其处方进行优化，为该药物的后续研究与开发提供参考。方法：采用乙醇注入法制备去氢骆驼蓬碱醇质体，以乙醇体积分数、卵磷脂用量、卵磷脂与胆固醇的用量比为考察因素，以粒径，Zeta电位和包封率为评价指标，应用三因素五水平星点设计-效应面法对去氢骆驼蓬碱醇质体的处方进行优化，并考察该制剂的初步稳定性。结果：最佳处方为去氢骆驼蓬碱0.03%，蛋黄卵磷脂1.13%，卵磷脂-胆固醇（41.55：1），乙醇体积分数28%。制得的醇质体大小均一、圆整、分散均匀，包封率、粒径及Zeta电位平均值分别为79.0%，124.8 nm，-57.1 mV。结论：去氢骆驼蓬碱醇质体制备工艺简单、处方设计合理、稳定性较高，为进一步探讨该制剂的皮肤给药奠定了基础。

Abstract

Objective: In order to provide a certain reference value for the follow-up research and development of harmine

harmine-loaded ethosomes were prepared and its formula was optimized. Method: Harmine-loaded ethosomes were prepared by ethanol injection method.With the volume fraction of ethanol

the amount of phospholipids and the ratio of phospholipids/cholesterol (P/C) as factors

the particle size

Zeta potential and encapsulation efficiency as evaluation indexes

central composite design-response surface methodology was used to optimize the prescription of harmine-loaded ethosomes.The preliminary stability of the ethosomes was also evaluated. Result: The best prescription for harmine-loaded ethosomes were 0.03% of harmine

1.13% of lecithin

P/C ratio of 41.55:1 and 28% of ethanol volume fraction.The prepared ethosomes were round with uniform size and well dispersed.The encapsulation efficiency

particle size and Zeta potential of harmine-loaded ethosomes were 79.0%

124.8 nm and -57.1 mV

respectively. Conclusion: The preparation process of harmine-loaded ethosomes is simple.The prescription design is reasonable with good stability

which lays the foundation for the further study on the transdermal delivery of harmine-loaded ethosomes.

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