Preparation of Oxymatrine Phospholipid Complex Solid Lipid Nanoparticles Lyophilized Powder and Evaluation of Its Quality

Jun-li YAN; Wan-rong LI; Jia-jia YANG; Yi WANG; Zhi-yong HE; Feng JIANG; Xue ZHOU; Lin-jing WU; Shi-quan GAN; Heng WANG; Xiang-chun SHEN; Ling TAO

doi:10.13422/j.cnki.syfjx.20190306

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Preparation of Oxymatrine Phospholipid Complex Solid Lipid Nanoparticles Lyophilized Powder and Evaluation of Its Quality

Pharmacy and Processing | 更新时间：2021-02-09

- Preparation of Oxymatrine Phospholipid Complex Solid Lipid Nanoparticles Lyophilized Powder and Evaluation of Its Quality
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 25, Issue 7, Pages: 146-152(2019)
- 作者机构：
  
  1.贵州医科大学　省部共建药用植物功效与利用国家重点实验室，贵州省天然药物资源高效利用工程中心，贵州省高等学校天然药物药理与成药性评价特色重点实验室，天然药物资源优效利用重点实验室，贵阳　 550025；
  2.黔南民族医学高等专科学校，贵州　都匀　 558003
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20190306
  CLC： R22;R94;R28;C37
- Received：17 June 2018，
  
  Published Online：16 November 2018，
  
  Published：05 April 2019
- 稿件说明：
移动端阅览
Jun-li YAN, Wan-rong LI, Jia-jia YANG, et al. Preparation of Oxymatrine Phospholipid Complex Solid Lipid Nanoparticles Lyophilized Powder and Evaluation of Its Quality[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(7): 146-152.
DOI：

Jun-li YAN, Wan-rong LI, Jia-jia YANG, et al. Preparation of Oxymatrine Phospholipid Complex Solid Lipid Nanoparticles Lyophilized Powder and Evaluation of Its Quality[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(7): 146-152. DOI： 10.13422/j.cnki.syfjx.20190306.

摘要

目的：

制备氧化苦参碱磷脂复合物固体脂质纳米粒(OMT-PC-SLN)冻干粉，并对其进行药剂学性质评价。

方法：

采用伪三元相图优选微乳处方；以包封率为指标，采用单因素试验优选OMT-PC-SLN冻干粉的处方工艺；利用透射电子显微镜(TEM)观察该制剂的外观形态，激光粒度仪测定粒径，并考察OMT-PC-SLN冻干粉的体外释药性能。

结果：

最佳处方工艺为大豆磷脂和15-羟基硬脂酸聚乙二醇酯（Kolliphor HS 15）为乳化剂，乙醇为助乳化剂，乳化剂与助乳化剂的比例（

）＝3∶2，油相∶（乳化剂＋助乳化剂）＝1∶9，氧化苦参碱磷脂复合物-硬脂酸-大豆磷脂-Kolliphor HS 15-乙醇（30∶100∶180∶360∶360）；含4%甘露醇的水50 mL为外水相，1 000 r·min

－1

冰浴搅拌固化1 h，于－20 ℃预冻24 h，取出，干燥24 h。OMT-PC-SLN冻干粉外观呈类球形，包封率（38.09±1.24）%，平均粒径785.5 nm，多分散系数（PDI）0.456，Zeta电位－24.82 mV；体外释放结果表明OMT-PC-SLN冻干粉2 h时累积释放率72.63%，12 h累积释放率98.42%，原料药在2 h的累积释放率98.60%。

结论：

优选的OMT-PC-SLN冻干粉处方工艺稳定、重复性好；与原料药相比，OMT-PC-SLN冻干粉体外释放较慢，具有一定的缓释效果。

Abstract

Objective:

To prepare oxymatrine phospholipid complex solid lipid nanoparticles(OMT-PC-SLN) lyophilized powder and evaluate its pharmaceutical properties.

Method:

Pseudo-ternary phase diagram was employed to optimize the formula of microemulsion; single factor experiments were adopted to optimize the formulation process of OMT-PC-SLN lyophilized powder with encapsulation efficiency as index; the morphology of this preparation was observed by transmission electron microscope(TEM). The particle size was measured by particle size analyzer and the

in vitro

release performance of OMT-PC-SLN lyophilized powder was examined.

Result:

Optimal formulation process was as following: taking soybean phospholipid and polyethylene glycol 15-hydroxystearate(Kolliphor HS 15) as the emulsifier

ethanol as co-emulsifier

ratio of emulsifier to co-emulsifier(

)=3∶2

oil phase∶(emulsifier+ co-emulsifier)=1∶9

oxymatrine phospholipid complex-stearic acid-soybean phospholipid-Kolliphor HS 15-ethanol(30∶100∶180∶360∶360); taking 50 mL of 4%mannitol solution as the external aqueous phase

ice bath stirring at 1 000 r·min

-1

and solidifying for 1 h

precooled at -20 ℃ for 24 h

took out and dried for 24 h. OMT-PC-SLN lyophilized powder was spherical in appearance with encapsulation efficiency of (38.09±1.24)%

average particle size of 785.5 nm

polydispersity coefficient(PDI) of 0.456 and the Zeta potential of -24.82 mV.The cumulative release rates of OMT-PC-SLN lyophilized powder were 72.63%at 2 h and 98.42%at 12 h; the cumulative release rate of oxymatrine(crude drug) was 98.60%at 2 h.

Conclusion:

This optimized formulation process of OMT-PC-SLN lyophilized powder is stable with good repeatability; compared with oxymatrine

OMT-PC-SLN lyophilized powder has a certain sustained-release effect.

关键词

Keywords

references

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