• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
PENG Yifan, WANG Zengming, WANG Rongrong, DU Yimeng, GAO Xiang, ZHENG Aiping, ZHANG Hui. Preparation and in vitro and in vivo evaluation of oral curcumin nanocrystalline capsules[J]. Journal of China Pharmaceutical University, 2021, 52(2): 211-218. DOI: 10.11665/j.issn.1000-5048.20210210
Citation: PENG Yifan, WANG Zengming, WANG Rongrong, DU Yimeng, GAO Xiang, ZHENG Aiping, ZHANG Hui. Preparation and in vitro and in vivo evaluation of oral curcumin nanocrystalline capsules[J]. Journal of China Pharmaceutical University, 2021, 52(2): 211-218. DOI: 10.11665/j.issn.1000-5048.20210210
shu

Preparation and in vitro and in vivo evaluation of oral curcumin nanocrystalline capsules

  • 1.

    China Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Academy of Military Sciences, Beijing 100850, China

  • 2.

    School of Pharmacy, North China University of Science and Technology, Tangshan 063210, China

Funds: This study was supported by the National Natural Science Foundation of China (No. 81573357, No. 82073793)
More Information
  • Received Date: December 28, 2020
  • Revised Date: April 08, 2021
    Graphical Abstract
    • Abstract
  • The poorly water-soluble drug curcumin was prepared into oral nanocrystalline solid preparation by nanocrystal technology to improve the solubility, dissolution rate, and bioavailability. Curcumin nanocrystals were prepared by media grinding technology, and two types of stable curcumin nanocrystal suspension formulations were developed. The stabilizers in the two formulations were polyvinylpyrrolidone (PVP K30)/sodium lauryl sulfate (SDS)(1∶1) and Tween 80, respectively. The prepared curcumin nanocrystal suspension was loaded onto microcrystalline cellulose pellets through fluidized bed coating technology, and the nanocrystalline capsules were obtained after filling. The results of nanocrystal redispersion stability and scanning electron microscope (SEM) showed that the morphology of drug-loaded pellets was uniform when PVP K30 and SDS were used as stabilizers, and the diameter of nanocrystals before and after redispersion was about 200 nm, which was determined as the optimal formulation. In vitro dissolution study showed that curcumin nanocrystals at the size of 200 nm exhibited significantly promoted dissolution. The results of X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) showed that the curcumin crystalline partly turned amorphous during the preparation of nanocrystals.Pharmacokinetic studies in rats showed that the bioavailability of curcumin nanocrystals was 9.3 times higher than that of the bulk drug. The curcumin nanocrystalline capsules developed in this research can significantly improve the dissolution rate and bioavailability, which is of great significance in improving the poor solubility of drugs, and is expected to become a new dosage form for clinical treatment.
    • FullText(HTML)
    • References (22)
  • [1]
    .Clin Cancer Res，2008，14（14）：4491-4499.
    [2]
    Wo XD，Hong XQ，Gao CX，et al.Long-period virulent test of curcumin［J］.J Zhejiang Tradit Chin Med Coll （浙江中医学院学报），2000，24（1）：61-65.
    [3]
    Wo XD，Hong XQ，Gao CX.Maximum toleration test of curcumin［J］.J Zhejiang Tradit Chin Med Coll （浙江中医学院学报），2000，24（2）：55-55.
    [4]
    Sharma RA，McLelland HR，Hill KA，et al.Pharmacodynamic and pharmacokinetic study of oral Curcuma extract in patients with colorectal cancer［J］.Clin Cancer Res，2001，7（7）：1894-1900.
    [5]
    Lao CD，Ruffin MT，Normolle D，et al.Dose escalation of a curcuminoid formulation［J］.BMC Complement Altern Med，2006，6：10.
    [6]
    Cheng AL，Hsu CH，Lin JK，et al.Phase I clinical trial of curcumin，a chemopreventive agent，in patients with high-risk or pre-malignant lesions［J］.Anticancer Res，2001，21（4b）：2895-2900.
    [7]
    T?nnesen HH，Másson M，Loftsson T.Studies of curcumin and curcuminoids.XXVII.Cyclodextrin complexation：solubility，chemical and photochemical stability［J］.Int J Pharm，2002，244（1/2）：127-135.
    [8]
    Khan MA.Enhancement of solubility of poorly water soluble drugs diclofenac Sodium by mixed solvency approach［J］.Res J Pharm Dosage Form Technol，2013，5（1）：39-41.
    [9]
    Millard J，Alvarez-Nú?ez F，Yalkowsky S.Solubilization by cosolvents.Establishing useful constants for the log-linear model［J］.Int J Pharm，2002，245（1/2）：153-166.
    [10]
    Gupta NK，Dixit VK.Bioavailability enhancement of curcumin by complexation with phosphatidyl choline［J］.J Pharm Sci，2011，100（5）：1987-1995.
    [11]
    Shulman M，Cohen M，Soto-Gutierrez A，et al.Enhancement of naringenin bioavailability by complexation with hydroxypropyl-β-cyclodextrin.［corrected］［J］.PLoS One，2011，6（4）：e18033.
    [12]
    Ko?bia? M，Gierycz P.Comparison of aqueous and 1-octanol solubility as well as liquid-liquid distribution of acyclovir derivatives and their complexes with hydroxypropyl-β-cyclodextrin［J］.J Solution Chem，2013，42（4）：866-881.
    [13]
    Serajuddin AT.Salt formation to improve drug solubility［J］.Adv Drug Deliv Rev，2007，59（7）：603-616.
    [14]
    Liversidge GG，Cundy KC.Particle size reduction for improvement of oral bioavailability of hydrophobic drugs：I.Absolute oral bioavailability of nanocrystalline danazol in beagle dogs［J］.Int J Pharm，1995，125（1）：91-97.
    [15]
    Rao S，Song Y，Peddie F，et al.Particle size reduction to the nanometer range：a promising approach to improve buccal absorption of poorly water-soluble drugs［J］.Int J Nanomedicine，2011，6：1245-1251.
    [16]
    Sigfridsson K，Lundqvist AJ，Strimfors M.Particle size reduction for improvement of oral absorption of the poorly soluble drug UG558 in rats during early development［J］.Drug Dev Ind Pharm，2009，35（12）：1479-1486.
    [17]
    Liversidge GG，Conzentino P.Drug particle size reduction for decreasing gastric irritancy and enhancing absorption of naproxen in rats［J］.Int J Pharm，1995，125（2）：309-313.
    [18]
    Zhou XY，Lin HQ，Lei W.Research progress of insoluble drug nanocrystals［J］.Cent South Pharm （中南药学），2013，11（5）：353-358.
    [19]
    Yue PF，Liu Y，Xie J，et al.Review and prospect on preparation technology of drug nanocrystals in the past thirty years［J］.Acta Pharm Sin （药学学报），2018，53（4）：529-537.
    [20]
    Peltonen L，Hirvonen J.Pharmaceutical nanocrystals by nanomilling：critical process parameters，particle fracturing and stabilization methods［J］.J Pharm Pharmacol，2010，62（11）：1569-1579.
    [21]
    Chang TL，Zhan HL，Liang DN，et al.Nanocrystal technology for drug formulation and delivery［J］.Front Chem Sci Eng，2015，9（1）：1-14.
    [22]
    Yu WB，Jin ZM，Jian YF，et al.The pharmacokinetics of curcumin extract and turmeric monomer after administration in rats［J］.Pharmacol Clin Chin Mater Med （中药药理与临床），2018，34（5）：30-33.
    • Related Articles

  • Related Articles

    [1]ZHONG Shuisheng, LUO Zhu, SUN Luning, JANVIER Engelbert Agbokponto, LIANG Maozhi, DING Li. Pharmacokinetic interaction between bencycloquidium bromide nasal spray and budesonide nasal spray in healthy volunteers[J]. Journal of China Pharmaceutical University, 2013, 44(5): 447-450. DOI: 10.11665/j.issn.1000-5048.20130512
    [2]YANG Zhi-xin, WANG Jing, CHEN Zhong-xin, WANG Rui, XIE Li, CHANG Shuang. Comparative study of three pore-forming agents for colon coating solution of 5-aminosalicylic acid[J]. Journal of China Pharmaceutical University, 2012, 43(4): 325-328.
    [3]SONG Yi-ting, ZHOU Hong, SUN Wan-jin, GAO Yuan, LI Chao. Preparation and physicochemical characterization of a spray-dried lornoxicam self-microemulsifying system[J]. Journal of China Pharmaceutical University, 2012, 43(2): 137-141.
    [4]ZHAO Yan-rong, DING Li, RAO Ya-kun, TANG Xiao-wen, DING Jun-hong. Stability and degradation products of otilonium bromide in different media[J]. Journal of China Pharmaceutical University, 2010, 41(6): 548-554.
    [5]CHEN Liang, TONG Xin-yong, SHI Yuan, TAN Yan. Preparation of fluticasone propionate nasal spray and its spray characteristics[J]. Journal of China Pharmaceutical University, 2010, 41(6): 524-528.
    [6]YANG Yan, ZHU Jia-bi, ZHENG Chun-li, CHEN Sheng-jun. Preparation and characterization of aqueous polymer dispersions with high flexibility for coating[J]. Journal of China Pharmaceutical University, 2009, 40(4): 310-315.
    [7]Preparation of Compound Lonicera japonica Effervescent Spray[J]. Journal of China Pharmaceutical University, 2002, (4): 39-41.
    [8]Study onDrug Release Characteristics from Aqueous Ethylcellulose Dispersion Coated Pellets[J]. Journal of China Pharmaceutical University, 2000, (1): 27-30.
    [9]Preparation and Evaluation of Enteric Tablet Erythromycin Coated by Acrylic Resin No.2 Pseudolatex[J]. Journal of China Pharmaceutical University, 1994, (5): 267-270.
    [10]Studies on Aqueous Coating Technique for Acetylsalicylic Acid Enteric Tablets[J]. Journal of China Pharmaceutical University, 1991, (3): 154-157.

  • Cited by

    Periodical cited type(5)

    1. 阿文丽，张衡頔，胡吉蕾，肖春秀，凡蝶，康超，时皎皎，林宁. 姜黄素在低压低氧环境下对机体保护作用机制的研究进展. 中国医药导报. 2024(06): 50-53 .
    2. 郑光艳，吴文丽，刘泽梅，车鑫，王立红. 微流控技术制备槲皮素纳米晶及其大鼠体内药动学研究. 中国医药工业杂志. 2024(04): 519-526 .
    3. 陈榕，颜烨，何梓炫，黄小红，林昭妍. 提升姜黄素疗效的策略及技术研究进展. 中草药. 2024(15): 5315-5330 .
    4. 李双霞，薛晶晶. 浅谈浸出制剂的技术难点与研发策略. 基层中医药. 2023(02): 70-74 .
    5. 王培，牛丽丽，李静宇，耿红梅. 医用多孔支架材料的制备及缓释性能分析. 中国塑料. 2022(11): 73-78 .

    Other cited types(3)

Catalog

    Get Citation
    PDF
    XML
    Article views (316) PDF downloads (698) Cited by(8)
    Turn off MathJax
    Article Contents
    Abstract
    References
    Related Articles

    Copyright © Journal of China Pharmaceutical University苏ICP备12050101号-2

    Address：24 Tongjia Lane, Nanjing City, Jiangsu Province （210009）Tel: 025-83271566E-mail: xuebao@cpu.edu.cn

    Supported by: Beijing Renhe Information Technology Co., Ltd.  Baidu Analytics

    Total visits：311885

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return