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Thermal characterization and compatibility studies of itraconazole and excipients for development of solid lipid nanoparticles

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Abstract

The current study was performed to investigate possible interactions between triazole antifungal drug itraconazole (ITR) with selected excipients commonly used for development of solid lipid nanoparticles. The excipients included common lipids (glyceryl behenate (Compritol 888 ATO™), glyceryl monostearate, stearic acid, and cetyl palmitate), charge inducers (dicetyl phosphate and stearlyamine), and surfactants (sodium cholate and sodium deoxycholate). Differential scanning calorimetry, isothermal stress testing, Fourier transform infrared spectral analysis, optical microcopy, and X-ray powder diffraction analysis were performed for assessing the compatibility between the drug and the excipients. Results of the study suggest that the stearic acid exhibited drug–excipient interactions, whereas all other excipients used in the study were found to be compatible with ITR.

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References

  1. Verma RK, Garg S. Selection of excipients for extended release formulations of glipizide through drug–excipient compatibility testing. J Pharm Biomed Anal. 2005;38:633–44.

    Article  CAS  Google Scholar 

  2. Verma RK, Garg S. Compatibility studies between isosorbide mononitrate and selected excipients used in the development of extended release formulations. J Pharm Biomed Anal. 2004;35:449–58.

    Article  CAS  Google Scholar 

  3. Pani NR, Nath LK, Acharya S. Compatibility studies of nateglinide with excipients in immediate release tablets. Acta Pharm. 2011;61:237–47.

    Article  CAS  Google Scholar 

  4. Abbas D, Kaloustian J, Orneto C, Piccerelle P, Portugal H, Nicolay A. DSC and physico-chemical properties of a substituted pyridoquinoline and its interaction study with excipients. J Therm Anal Calorim. 2008;93(2):353–60. doi:10.1007/s10973-008-9062-7.

    Article  CAS  Google Scholar 

  5. Drebushchak VA, Shakhtshneider TP, Apenina SA, Medvedeva AS, Safronova LP, Boldyrev VV. Thermoanalytical investigation of drug–excipient interaction. J Therm Anal Calorim. 2006;86(2):303–9. doi:10.1007/s10973-005-7440-y.

    Article  CAS  Google Scholar 

  6. Pani N, Nath L, Acharya S, Bhuniya B. Application of DSC, IST, and FTIR study in the compatibility testing of nateglinide with different pharmaceutical excipients. J Therm Anal Calorim. 2012;108(1):219–26. doi:10.1007/s10973-011-1299-x.

    Article  CAS  Google Scholar 

  7. Bruni G, Berbenni V, Milanese C, Girella A, Marini A. Drug–excipient compatibility studies in binary and ternary mixtures by physico-chemical techniques. J Therm Anal Calorim. 2010;102(1):193–201. doi:10.1007/s10973-009-0382-z.

    Article  CAS  Google Scholar 

  8. Marini A, Berbenni V, Pegoretti M, Bruni G, Cofrancesco P, Sinistri C, et al. Drug–excipient compatibility studies by physico-chemical techniques: the case of atenolol. J Therm Anal Calorim. 2003;73(2):547–61. doi:10.1023/a:1025478129417.

    Article  CAS  Google Scholar 

  9. Tita D, Jurca T, Fulias A, Marian E, Tita B. Compatibility study of the acetylsalicylic acid with different solid dosage forms excipients. J Therm Anal Calorim. 2013;112(1):407–19. doi:10.1007/s10973-013-2937-2.

    Article  CAS  Google Scholar 

  10. De Beule K, Van Gestel J. Pharmacology of itraconazole. Drugs. 2001;61(S1):27–37.

    Article  Google Scholar 

  11. Dobaria N, Badhan A, Mashru R. A novel itraconazole bioadhesive film for vaginal delivery: design, optimization, and physicodynamic characterization. AAPS PharmSciTech. 2009;10(3):951–9. doi:10.1208/s12249-009-9288-0.

    Article  CAS  Google Scholar 

  12. Heykants J, Van Peer A, Van de Velde V, Van Rooy P, Meuldermans W, Lavrijsen K, et al. The clinical pharmacokinetics of itraconazole: an overview. Mycoses. 1989;32:67–87. doi:10.1111/j.1439-0507.1989.tb02296.x.

    Article  Google Scholar 

  13. Buchanan CM, Buchanan NL, Edgar KJ, Klein S, Little JL, Ramsey MG, et al. Pharmacokinetics of itraconazole after intravenous and oral dosing of itraconazole-cyclodextrin formulations. J Pharm Sci. 2007;96(11):3100–16. doi:10.1002/jps.20878.

    Article  CAS  Google Scholar 

  14. Barone JA, Moskovitz BL, Guarnieri J, Hassell AE, Colaizzi JL, Bierman RH, et al. Food interaction and steady-state pharmacokinetics of itraconazole oral solution in healthy volunteers. Pharmacotherapy. 1998;18(2):295–301.

    CAS  Google Scholar 

  15. Singh AK, Nath LK. Evaluation of compatibility of tablet excipients and novel synthesized polymer with lamivudine. J Therm Anal Calorim. 2012;108:263–7.

    Article  CAS  Google Scholar 

  16. Kumar N, Shishu, Bansal G, Kumar S, Jana AK. Preparation and cyclodextrin assisted dissolution rate enhancement of itraconazolium dinitrate salt. Drug Dev Ind Pharm. 2012;. doi:10.3109/03639045.2012.681382.

    Google Scholar 

  17. Kumar N, Shishu, Bansal G, Kumar S, Jana AK. Ditosylate salt of itraconazole and dissolution enhancement using cyclodextrins. AAPS PharmSciTechnol. 2012;. doi:10.1208/s12249-012-9804-5.

    Google Scholar 

  18. Kumar N, Shishu, Kapoor VR. Facile syntheses of novel salts of a triazole antifungal agent with enhanced solubility. J Heterocycl Chem. 2012;. doi:10.1002/jhet.1120.

    Google Scholar 

  19. DiNunzio JC, Brough C, Miller DA, Williams RO, McGinity JW. Fusion processing of itraconazole solid dispersions by kinetisol® dispersing: a comparative study to hot melt extrusion. J Pharm Sci. 2010;99(3):1239–53. doi:10.1002/jps.21893.

    Article  CAS  Google Scholar 

  20. Six K, Daems T, de Hoon J, Van Hecken A, Depre M, Bouche M-P, et al. Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion. Eur J Pharm Sci. 2005;24(2–3):179–86.

    Article  CAS  Google Scholar 

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Correspondence to Shishu Goindi.

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Kumar, N., Goindi, S., Saini, B. et al. Thermal characterization and compatibility studies of itraconazole and excipients for development of solid lipid nanoparticles. J Therm Anal Calorim 115, 2375–2383 (2014). https://doi.org/10.1007/s10973-013-3237-6

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