JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2013, 62(2):71-77

Optimization of diclofenac sodium profile from halloysite nanotubules

Kateřina Krejčová1, Patrick B. Deasy1, Miloslava Rabišková2,*
1 School of Pharmacy, Trinity College Dublin, Dublin, Ireland
2 Department of Pharmaceutical Technology, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic

Halloysite, aluminosilicate clay with the particle shape of multilayered hollow nanotubes, used in various non-medical applications, e.g. in ceramic industry, was discovered for pharmaceutical purposes in recent years. Several drugs of hydrophilic and lipophilic nature have been successfully encapsulated into halloysite tubules in order to modify their dissolution profile. The main goal of this experiment was to optimize the dissolution profile of diclofenac sodium - a drug with problematic solubility - from halloysite tubules using various polymers. Loading of the drug together with povidone or Eudragit® RS did not lead to drug burst effect reduction and its slower dissolution. In the case of povidone, drug improved wettability and solubilization rather than viscosity increasing expectations were observed. Eudragit® RS formed a solid dispersion with diclofenac sodium and thus the solvent/drug solution penetration through the polymer and not the drug solubility was the dissolution rate limiting factor. Reduction of the burst effect and further prolongation of drug release was achieved by coating the drug-loaded halloysite with chitosan. This formulation exhibited a diffusion-controlled prolonged release following Higuchi kinetic model.

Keywords: halloysite; diclofenac sodium; povidone; Eudragit® RS; chitosan; solid dispersion; prolonged release

Received: December 12, 2012; Accepted: January 14, 2013; Published: February 1, 2013  Show citation

ACS AIP APA ASA Harvard Chicago Chicago Notes IEEE ISO690 MLA NLM Turabian Vancouver
Krejčová K, Deasy PB, Rabišková M. Optimization of diclofenac sodium profile from halloysite nanotubules. Čes. slov. farm. 2013;62(2):71-77.
Share...
Download citation
  • BibTeX (.bib)
  • Bookends (.ris)
  • EasyBib (.ris)
  • EndNote (.enw)
  • EndNote 8 (.xml)
  • ISI WoS (.isi)
  • Medlars (.medlars)
  • Mendeley (.ris)
  • MODS (.xml)
  • Papers (.ris)
  • RefWorks (.txt)
  • RefManager (.ris)
  • RIS (.ris)
  • MS Word (.xml)
  • Zotero (.ris)
    • Open full article

    References

    1. Levis S. R., Deasy P. B. Use of coated microtubular halloysite for the sustained release of diltiazem hydrochloride and propranolol hydrochloride. Int. J. Pharm. 2003; 253, 145-157. Go to original source... Go to PubMed...
    2. Price R. R., Gaber B. P., Lvov Y. M. In-vitro release characteristics of tetracycline HCl, khellin and nicotinamide adenine dineculeotide from halloysite. J. Microencapsulation 2001; 18, 713-722. Go to original source... Go to PubMed...
    3. Forsgren J., Jamstorp E., Bredenberg S., Engqvist H., Strømme M. A ceramic drug delivery vehicle for oral administration of highly potent opioids. J. Pharm. Sci. 2010; 99, 219-226. Go to original source... Go to PubMed...
    4. Viseras M. T., Aguzzi C. Cerezo P., Viseras C., Valenzuela C. Equilibrium and kinetics of 5-aminosalicylic acid adsorption by halloysite. Micropor. Mesopor. Mater. 2008; 108, 112-116. Go to original source...
    5. Krejčová K., Deasy P. B., Rabišková M. Diclofenac sodium entrapment and release from halloysite nanotubules. Čes. slov. Farm. 2013; 62, 28-34.
    6. Frost R. L., Tran T. H., Kristof J. FT-Raman spectroscopy of the lattice region of kaolinite and its intercalates. Vibrational Spectroscopy 1997; 13, 175-186. Go to original source...
    7. Tari G., Bobos I., Gomes C. S. F., Ferreira J. M. F. Modification of surface charge properties during kaolinite to halloysite-7Å transformation. J. Colloid Interface Sci. 1999; 210, 360-366. Go to original source... Go to PubMed...
    8. Levis S. R., Deasy P. B. Characterization of halloysite for use as a microtubular drug delivery system. Int. J. Pharm. 2002; 243, 125-134. Go to original source... Go to PubMed...
    9. Lvov Y. M., Price R., Gaber B., Ichinose I. Thin film nanofabrication via layer-by-layer adsorption of tubule halloysite, spherical silica, proteins and polycations. Colloids and Surfaces A: Physicochem. Eng. Aspects 2002; 198-200, 375-382. Go to original source...
    10. Kumar M. N. V. R., Kumar N. Polymeric controlled drug-delivery systems: Perspective issues and opportunities. Drug Dev. Ind. Pharm. 2001; 27, 1-30. Go to original source... Go to PubMed...
    11. Kincl M., Vrečer F., Veber M. Characterization of factors affecting the release of low-solubility drug from prolonged release tablets. Anal. Chim. Acta 2004; 502, 107-113. Go to original source...
    12. Fini A., Fazio G., Gonzales-Rodriguez M., Cavallari C., Passerini N., Rodriguez L. Formation of ion-pairs in aqueous solutions of diclofenac sodium. Int. J. Pharm. 1999; 187, 163-173. Go to original source... Go to PubMed...
    13. Vadnere M. K. Coprecipitates and melts. In: Swarbrick J., Boylan J.C., editors. Encyclopedia of Pharmaceutical Technology. 2nd ed. New York - Basel: Marcel Dekker, Inc. 2002; 641-647.
    14. Bühler V. Kollidon: Polyvinylpyrrolidon for the pharmaceutical industry. 2nd ed. Ludwigshafen 1993. BASF 15-106.
    15. Pignatello R., Ferro M., De Guidi G., Salemi G., Vandelli M. A., Guccione S., Geppi M., Forte C., Puglisi G. Preparation, characterization and photosensitivity studies of solid dispersions of diflunisal and Eudragit® RS 100 and RL 100. Int. J. Pharm. 2001; 218, 27-42. Go to original source... Go to PubMed...
    16. Pignatello R., Consoli P., Puglisi G. In vitro release kinetics of tolmetin from tabletted Eudragit microparticles. J. Microencapsulation 2000; 17, 373-383. Go to original source... Go to PubMed...
    17. Khalil E., Sallam A. Interaction of two diclofenac acid salts with copolymers of ammoniomethacrylate: Effect of additives and release profiles. Drug Dev. Ind. Pharm. 1999; 25(4), 419-427. Go to original source... Go to PubMed...
    18. Pignatello R., Ferro M., Puglisi G. Preparation of solid dispersions of nonsteroidal anti-inflammatory drugs with acrylic polymers and studies on mechanisms of drug-polymer interactions. AAPS Pharm. Sci. Tech. 2002; 3, 1-11. Go to original source... Go to PubMed...
    19. Serajuddin A. T. M. Solid dispersions of poorly water-soluble drugs: Early promises, subsequent problems and recent breakthroughs. J. Pharm. Sci. 1999; 88, 1058-1066. Go to original source... Go to PubMed...
    20. Janquin M. R., McGinity J. W. Characterization of acrylic resin matrix films and mechanisms of drug-polymer interactions. Int. J. Pharm. 1994; 101, 23-34. Go to original source...
    21. Crea F., de Stefano C., Millero F. J. Dissociation constants for citric acid in NaCl and KCl solutions and their mixtures at 25 °C. J. Sol. Chem. 2004; 33, 1349-1366. Go to original source...

    Return to the content


    Czech and Slovak Pharmacy

    Madam, Sir,
    please be aware that the website on which you intend to enter, not the general public because it contains technical information about medicines, including advertisements relating to medicinal products. This information and communication professionals are solely under §2 of the Act n.40/1995 Coll. Is active persons authorized to prescribe or supply (hereinafter expert).
    Take note that if you are not an expert, you run the risk of danger to their health or the health of other persons, if you the obtained information improperly understood or interpreted, and especially advertising which may be part of this site, or whether you used it for self-diagnosis or medical treatment, whether in relation to each other in person or in relation to others.

    I declare:

    1. that I have met the above instruction
    2. I'm an expert within the meaning of the Act n.40/1995 Coll. the regulation of advertising, as amended, and I am aware of the risks that would be a person other than the expert input to these sites exhibited

    No
    Yes

    If your statement is not true, please be aware
    that brings the risk of danger to their health or the health of others.