Preparation and evaluation of curcumin/berberine co-loaded self-microemulsion drug delivery system

HAN Hua; LIANG Lüyuan; JI Ke; WEI Bingqi; REN Lingjia; SU Jiexin; GUAN Yanbin

doi:10.6039/j.issn.1001-0408.2022.20.11

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Preparation and evaluation of curcumin/berberine co-loaded self-microemulsion drug delivery system

更新时间：2025-12-05

- Preparation and evaluation of curcumin/berberine co-loaded self-microemulsion drug delivery system
- ZHONGGUO YAOFANG Vol. 33, Issue 20, Pages: 2487-2492(2022)
- 作者机构：
  
  1.河南中医药大学药学院，郑州　450040
  2.河南中医药大学儿科医学院，郑州　450040
  3.河南中医药大学仲景学院，郑州　450040
- 作者简介：
- 基金信息：
- DOI：10.6039/j.issn.1001-0408.2022.20.11
  CLC： R943;R965
- Received：19 April 2022，
  
  Revised：2022-08-21，
  
  Published：30 October 2022
- 稿件说明：
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韩华,梁绿圆,季珂,等.共载姜黄素/小檗碱自微乳给药系统的制备及评价[J].中国药房,2022,33(20):2487-2492.

HAN Hua,LIANG Lüyuan,JI Ke,et al.Preparation and evaluation of curcumin/berberine co-loaded self-microemulsion drug delivery system[J].ZHONGGUO YAOFANG,2022,33(20):2487-2492.
韩华,梁绿圆,季珂,等.共载姜黄素/小檗碱自微乳给药系统的制备及评价[J].中国药房,2022,33(20):2487-2492. DOI： 10.6039/j.issn.1001-0408.2022.20.11.

HAN Hua,LIANG Lüyuan,JI Ke,et al.Preparation and evaluation of curcumin/berberine co-loaded self-microemulsion drug delivery system[J].ZHONGGUO YAOFANG,2022,33(20):2487-2492. DOI： 10.6039/j.issn.1001-0408.2022.20.11.

摘要

目的

制备共载姜黄素/小檗碱的自微乳给药系统（CUR/BER-SMEDDS），并对其理化性质和体外抗肿瘤作用进行评价。

方法

以CUR、BER为模型药物，在筛选油相种类，乳化剂、助乳化剂及二者质量比优化范围的基础上，以粒径和载药量为评价指标，以油相的质量百分比、乳化剂与助乳化剂的质量比为因素，采用星点设计-效应面法优化其处方并验证；对优化所得CUR/BER-SMEDDS的理化性质、体外溶出度、体外抗肿瘤作用进行评价。

结果

CUR/BER-SMEDDS最优处方的油相为中链甘油三酯（30.97%），乳化剂为聚氧乙烯40氢化蓖麻油（46.77%），助乳化剂为聚乙二醇400（22.26%），乳化剂与助乳化剂质量比为2.10∶1。验证实验表明，CUR/BER-SMEDDS的平均粒径为（58.90±5.41）nm，平均载药量为（94.94±3.87）mg/g，与预测值的相对偏差分别为－2.90%、－0.14%。按最优处方所制CUR/BER-SMEDDS加水乳化后为淡黄色澄清透明液体，其微粒呈圆球形。体外溶出实验结果显示，制成SMEDDS后，CUR在人工肠液、人工胃液，BER在人工肠液中的累积溶出度均明显高于对应原料药。体外抗肿瘤实验结果显示，CUR/BER-SMEDDS对PC-3、DU-145细胞的IC

分别为（17.38±2.84）、（20.89±1.26）μmol/L，均显著低于CUR、EBR单药（

＜0.05）。

结论

优化所得CUR/BER-SMEDDS制备工艺稳定、可行；所制CUR/BER-SMEDDS改善了药物的溶出速度，且具有更强的体外抗前列腺癌作用。

Abstract

OBJECTIVE

To prepare curcumin/berberine co-loaded self-microemulsion drug delivery system（CUR/BER-SMEDDS） and evaluate its physicochemical properties and

in vitro

anti-tumor effects.

METHODS

Using CUR and BER as model drug， based on the screening of the type of oil phase， emulsifier， co emulsifier and their mass ratio， the formulation of CUR/BER-SMEDDS were optimized by central composite design-response surface methodology， taking particle size and drug loading as evaluation parameters， with the mass percentage of oil phase and the mass ratio of emulsifier to co emulsifier as factors， and verification test was conducted. CUR/BER-SMEDDS prepared by optimized formulation were evaluated in terms of　physicochemical properties，

in vitro　

dissolution and

in vitro

anti-tumor effects.

RESULTS

The optimized formulation of CUR/BER-SMEDDS included that the oil phase was medium chain triglyceride （30.97%）， the emulsifier was polyoxyl 40 hydrogenated castor oil （46.77%）， the co emulsifier was polyethylene glycol 400 （22.26%）， and the mass ratio of emulsifier to co emulsifier was 2.10∶1. The validation experiments showed that mean particle size of CUR/BER-SMEDDS　was （58.90±5.41） nm， the average drug loading was （94.94±3.87） mg/g， and the relative deviations from the predicted values were －2.90% and －0.14%， respectively. The CUR/BER-SMEDDS prepared by optimal formulation was light yellow， clear and transparent liquid after emulsified with water， and its particles were spherical. The results of dissolution test

in vitro

showed that after SMEDDS was made， the cumulative dissolution of CUR in artificial intestinal fluid and artificial gastric fluid and that of BER in artificial intestinal fluid were significantly higher than those of its raw material. Results of

in vitro

anti-tumor experiment showed that IC

values of CUR/BER-SMEDDS for PC-3 cells and DU-145 cells were（17.38±2.84） and （20.89±1.26） μmol/L， which were all lower than those of CUR and EBR significantly （

＜0.05）.

CONCLUSIONS

The optimized preparation process of CUR/BER-SMEDDS is stable and feasible. The drug release of CUR/BER-SMEDDS is more complete than that of single drug， and has stronger anti-prostate cancer effect

in vitro

关键词

Keywords

references

NIEDZWIECKI A ， ROOMI M W ， KALINOVSKY T ， et al . Anticancer efficacy of polyphenols and their combinations [J ] . Nutrients ， 2016 ， 8 （ 9 ）： 552 .

陈美霓，郭巍，郝琴，等 . 姜黄素的药理作用、临床应用及机制研究进展 [J ] . 延安大学学报（医学科学版）， 2021 ， 19 （ 3 ）： 96 - 99 .

WANG Y ， LIU Y F ， DU X Y ， et al . The anti-cancer mechanisms of berberine：a review [J ] . Cancer Manag Res ， 2020 ， 12 ： 695 - 702 .

LIU Y X ， HUA W W ， LI Y ， et al . Berberine suppresses colon cancer cell proliferation by inhibiting the SCAP/SREBP-1 signaling pathway-mediated lipogenesis [J ] . Biochem Pharmacol ， 2020 ， 174 ： 113776 .

ZIASARABI P ， SAHEBKAR A ， GHASEMI F . Evalu-ation of the effects of nanomicellar curcumin，berberine，and their combination with 5-fluorouracil on breast cancer cells [J ] . Adv Exp Med Biol ， 2021 ， 1328 ： 21 - 35 .

MAITI P ， PLEMMONS A ， DUNBAR G L . Combination treatment of berberine and solid lipid curcumin particles increased cell death and inhibited PI3K/Akt/mTOR pathway of human cultured glioblastoma cells more effectively than did individual treatments [J ] . PLoS One ， 2019 ， 14 （ 12 ）： e0225660 .

BALAKRISHNA A ， KUMAR M H . Evaluation of synergetic anticancer activity of berberine and curcumin on different models of A549，hep-G2，MCF-7，jurkat，and K562 cell lines [J ] . Biomed Res Int ， 2015 ， 2015 ： 354614 .

杨建苗，许东航，李范珠 . 克服肿瘤多药耐药的药物共递送纳米载体的设计及研究新方向 [J ] . 中国现代应用药学， 2020 ， 37 （ 6 ）： 750 - 754 .

石金凤，李杰，杨晓琴，等 . 中药活性成分协同化疗药物的纳米共载体系联合抗肿瘤现状分析 [J ] . 药学学报， 2019 ， 54 （ 2 ）： 258 - 268 .

马巧芳，曾佳，沙康，等 . 口服自微乳给药系统的研究进展 [J ] . 药学进展， 2020 ， 44 （ 6 ）： 466 - 475 .

韩冰，关延彬，田雨冬，等 . 盐酸小檗碱自微乳释药系统的制备与体外评价 [J ] . 中药材， 2018 ， 41 （ 10 ）： 2398 - 2402 .

国家药典委员会 . 中华人民共和国药典：四部 [S ] . 2020年版. 北京：中国医药科技出版社，2020：132，480- 483 .

张婷，王镜，申宝德，等 . 共载细叶远志皂苷和β-细辛醚自微乳的制备及体外质量评价 [J ] . 中国中药杂志， 2020 ， 45 （ 24 ）： 5988 - 5995 .

赵艺宁，韩叶枫，梁建坤，等 . 香叶木素自微乳的制备 [J ] . 中成药， 2022 ， 44 （ 5 ）： 1588 - 1593 .

陈旺，帅丽霞，袁袁，等 . 单纯形网格法优选马甲子总三萜自微乳处方 [J ] . 中药新药与临床药理， 2022 ， 33 （ 6 ）： 836 - 841 .

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