• 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
JIANG Meixia, XIONG Hui, LI Yue, ZHOU Jianping, YAO Jing. Preparation and evaluation of thermo-sensitive hyaluronic acid/thiolated chitosan ophthalmic complex nano-hydrogel[J]. Journal of China Pharmaceutical University, 2014, 45(4): 413-419. DOI: 10.11665/j.issn.1000-5048.20140406
Citation: JIANG Meixia, XIONG Hui, LI Yue, ZHOU Jianping, YAO Jing. Preparation and evaluation of thermo-sensitive hyaluronic acid/thiolated chitosan ophthalmic complex nano-hydrogel[J]. Journal of China Pharmaceutical University, 2014, 45(4): 413-419. DOI: 10.11665/j.issn.1000-5048.20140406
shu

Preparation and evaluation of thermo-sensitive hyaluronic acid/thiolated chitosan ophthalmic complex nano-hydrogel

More Information
    Graphical Abstract
    • Abstract
  • The aim of this research was to prepare and evaluate thermo-sensitive complex nano-hydrogel(HP/CN)comprising of hyaluronic acid derivative(HA-PN)and thiolated chitosan(CMCS-NAC)for the ocular delivery of cyclosporine A(CsA). The CsA complex nano-hydrogel(CsA HP/CN)was prepared by incubation, then the size, Zeta potential, low critical solution temperature(LCST)and drug-loading capacity were characterized. The rabbit eye irritation effect, tissue adhesiveness and pharmacokinetic studies were investigated to evaluate the ocular compatibility and bioavailability of CsA HP/CN formulation. CsA HP/CN was found to be spherical in shape with a mean diameter of(122. 7±17. 8)nm, the Zeta potential of -(27. 87±2. 16)mV and LCST of 28. 4 °C with a drug-loading capacity up to 15. 08%. The rabbit eye irritation experiment showed no irritation on rabbit eyes. The CsA HP/CN group displayed significantly higher adhesive effect(1. 97- fold)on eye tissue as compared to the control group(drug carrier alone)after 15 min of ocular administration. Rabbit eyes pharmacokinetic data confirmed significantly higher AUC(1. 67- fold)and MRT(5. 17- fold)compared to the control group. Therefore, CsA HP/CN with small particle size and high drug loading capacity could obviously extend the drug retention time and increase its bioavailability on eyes, thus with potential application prospect in ocular drug delivery system.
    • FullText(HTML)
    • References (20)
  • [1]
    El Tayar N,Mark AE,Vallat P,et al.Solvent-dependent conformation and hydrogen-bonding capacity of cyclosporin A:evidence from partition coefficients and molecular dynamics simulations[J].J Med Chem,1993,36(24):3 757-3 764.
    [2]
    Prasad V,Kumar N,Mishra PR.Amphiphilic gels as a potential carrier for topical drug delivery[J].Drug Deliv,2007,14(2):75-85.
    [3]
    Hornof MD,Kast CE,Bernkop-Schnürch A.In vitro evaluation of the viscoelastic properties of chitosan-thioglycolic acid conjugates[J].Eur J Pharm Biopharm,2003,55(2):185-190.
    [4]
    Kast CE,Bernkop-Schnürch A.Thiolated polymers—thiomers:development and in vitro evaluation of chitosan-thioglycolic acid conjugates[J].Biomaterials,2001,22(17):2 345-2 352.
    [5]
    Kast CE,Frick W,Losert U,et al.Chitosan-thioglycolic acid conjugate:a new scaffold material for tissue engineering[J].Int J Pharm,2003,256(1/2):183-189.
    [6]
    Schmitz T,Grabovac V,Palmberger TF,et al.Synthesis and characterization of a chitosan-N-acetyl cysteine conjugate[J].Int J Pharm,2008,347(1/2/3):79-85.
    [7]
    Kafedjiiski K,Hoffer M,Werle M,et al.Improved synthesis and in vitro characterization of chitosan-thioethylamidine conjugate[J].Biomaterials,2006,27(1):127-135.
    [8]
    Bernkop-Schnürch A,Hornof M,Zoidl T.Thiolated polymers—thiomers:synthesis and in vitro evaluation of chitosan-2-iminothiolane conjugates[J].Int J Pharm,2003,260(2):229-237.
    [9]
    Bernkop-Schnürch A, Kast C, Guggi D. Permeation enhancing polymers in oral delivery of hydrophilic macromolecules:thiomer/GSH systems[J].J Control Release,2003,93(2):95-103.
    [10]
    Kafedjiiski K,Föger F,Werle M,et al.Synthesis and in vitro evaluation of a novel chitosan-glutathione conjugate[J].Pharm Res,2005,22(9):1 480-1 488.
    [11]
    Leitner VM,Walker GF,Bernkop-Schnürch A.Thiolated polymers:evidence for the formation of disulphide bonds with mucus glycoproteins[J].Eur J Pharm Biopharm,2003,56(2):207-214.
    [12]
    Langoth N, Kalbe J, Bernkop-Schnürch A. Development of a mucoadhesive and permeation enhancing buccal delivery system for PACAP(pituitary adenylate cyclase-activating polypeptide)[J].Int J Pharm,2005,296(1/2):103-111.
    [13]
    Bernkop-Schnürch A,Pinter Y,Guggi D,et al.The use of thiolated polymers as carrier matrix in oral peptide delivery—proof of concept[J].J Control Release,2005,106(1/2):26-33.
    [14]
    Langoth N,Kahlbacher H,Schöffmann G,et al.Thiolated chitosans:design and in vivo evaluation of a mucoadhesive buccal peptide drug delivery system[J].Pharm Res,2006,23(3):573-579.
    [15]
    Clausen AE,Bernkop-Schnürch A.In vitro evaluation of the permeation-enhancing effect of thiolated polycarbophil[J].J Pharm Sci,2000,89(10):1 253-1 261.
    [16]
    Anitha A,Deepa N,Chennazhi K P,et al.Development of mucoadhesive thiolated chitosan nanoparticles for biomedical applications[J].Carbohydr Polym,2011,83(1):66-73.
    [17]
    Bernkop-Schnürch A,Hornof M,Guggi D.Thiolated chitosans[J].Eur J Pharm Biopharm,2004,57(1):9-17.
    [18]
    Wu Y,Yao J,Zhou J,et al.Enhanced and sustained topical ocular delivery of cyclosporine A in thermosensitive hyaluronic acid-based in situ forming microgels[J].Int J Nanomedicine,2013,8:3 587-3 601.
    [19]
    Zou Y,Brooks DE,Kizhakkedathu JN.A novel functional polymer with tunable LCST[J].Macromolecules,2008,41(14):5 393-5 405.
    [20]
    Langoth N, Kalbe J, Bernkop-Schnürch A. Development of a mucoadhesive and permeation enhancing buccal delivery system for PACAP(pituitary adenylate cyclase-activating polypeptide)[J].Int J Pharm,2005,296(1/2):103-111.
    • Related Articles

  • Related Articles

    [1]LI Juanjuan, HUANG Yue, WANG Yahe, ZHANG Lianxiang, QIANG Yuanyuan, GUO Le, LIU Kunmei. Antiepileptic and neuroprotective mechanism of ursolic acid based on full-length transcriptome analysis[J]. Journal of China Pharmaceutical University, 2024, 55(4): 512-521. DOI: 10.11665/j.issn.1000-5048.2023111303
    [2]PEI Ting, WANG Yuying. Synthesis and preliminary anti-tumor activity of novel ursolic acid derivative-chalcone conjugates[J]. Journal of China Pharmaceutical University, 2017, 48(1): 31-41. DOI: 10.11665/j.issn.1000-5048.20170105
    [3]CHEN Hong, YANG Jie, CUI Wei-xi, WANG Qiang. Effects and mechanism of ursolic acid on lipopolysaccharide-induced THP-1 cells[J]. Journal of China Pharmaceutical University, 2011, 42(5): 447-451.
    [4]WANG Jing-song, SHEN Jing, ZHANG Ting, TANG Cong, REN Tian-nian, XI Tao. Ursolic acid downregulates COX-2 expression by suppressing the activation of ERK in A549 cells[J]. Journal of China Pharmaceutical University, 2011, 42(1): 68-72.
    [5]Inhibitory effects and mechanism of ursolic acid on the proliferation of rataortic smooth muscle cells[J]. Journal of China Pharmaceutical University, 2010, 41(1): 66-69.
    [6]ZHENG Kai-bo, SUN Cheng-bin, MAO Hai-li, YANG Zai-bo. Progress in the research of chemical structural modification of ursolic acid and structure-activity relationship[J]. Journal of China Pharmaceutical University, 2009, 40(6): 580-584.
    [7]Release and Identification of Monocrotalic Acid from Dehydromonocrotaline[J]. Journal of China Pharmaceutical University, 2003, (6): 18-21.
    [8]Cloning of Spinach Glycolate Oxidase cDNA and Its Construction into Yeast Expression Vector[J]. Journal of China Pharmaceutical University, 2003, (1): 83-86.
    [9]Cloning of S-adenosyl-L-methionine Synthetase Gene from Saccharomyces ceverisiae and its Expression in E.coli[J]. Journal of China Pharmaceutical University, 2002, (3): 87-89.
    [10]Determination of Four Acids Components in Keyoulin Liquid Using Derivatization by GC[J]. Journal of China Pharmaceutical University, 1998, (6): 453-455.

  • Cited by

    Periodical cited type(1)

    1. 朱灵英，郭娟，张爱丽，王宝婕，曾礼芳，徐福荣，马晓惠. 参与植物三萜生物合成的细胞色素P450酶研究进展. 中草药. 2019(22): 5597-5610 .

    Other cited types(3)

Catalog

    Get Citation
    PDF
    XML
    Article views PDF downloads Cited by(4)
    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：318963

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return