10.1007/s40089-014-0103-x

Preparation and characterization of azithromycin nanodrug using solvent/antisolvent method

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  • Hamid Reza Pouretedal*1,
  1. Faculty of Applied Chemistry, Malek-ashtar University of Technology, Shahin-Shahr, IR
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Published in Issue 2014-03-15

How to Cite

Pouretedal, H. R. (2014). Preparation and characterization of azithromycin nanodrug using solvent/antisolvent method. International Nano Letters, 4(1 (March 2014). https://doi.org/10.1007/s40089-014-0103-x
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Abstract

Abstract Nanoparticles of azithromycin are prepared using solvent/antisolvent precipitation method. The solubility of drug in water and the oral bioavailability are increased with decreasing particle size. The effect of type and concentration of surfactant and feed drug concentration are evaluated on the precipitated particle size. The nano-azithromycin in range 200–400 nm is obtained by the addition of absolute ethanol as solvent, water as antisolvent in presence of Tween ® 80 as surfactant. The prepared nanoparticles are characterized by infra-red spectra, particle size distribution, scanning electron microscopy, X-ray diffraction and differential scanning calorimetry. The chemical structure of nanosized azithromycin does not show any change but the crystallinity reduces in comparison with raw drug. Dissolution of azithromycin nanoparticles in purified water and buffer phosphate (pH of 6.0) is 2.93 and 3.36, respectively, times of raw drug in 30 min.

Keywords

  • Azithromycin,
  • Nanoparticles,
  • Antisolvent,
  • Bioavailability,
  • Tween® 80
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References

  1. Mullin (1993) Butterworth-Heinemann
  2. Lipinski (2002) Poor aqueous solubility, an industry wide problem in drug discovery (pp. 82-85)
  3. Mersmann (1999) Crystallization and precipitation (pp. 345-353)
  4. Dalvi and Dave (2009) Controlling particle size of a poorly water-soluble drug using ultrasound and stabilizers in antisolvent precipitation (pp. 7581-7593) https://doi.org/10.1021/ie900248f
  5. Mosharrafand and Nystrom (1995) The effect of particle size and shape on the surface specific dissolution rate of microsized practically insoluble drugs (pp. 35-47) https://doi.org/10.1016/0378-5173(95)00033-F
  6. Muller et al. (2001) Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future (pp. 3-19) https://doi.org/10.1016/S0169-409X(00)00118-6
  7. Matteucci et al. (2006) Drug nanoparticles by antisolvent precipitation: mixing energy versus surfactant stabilization (pp. 8951-8959) https://doi.org/10.1021/la061122t
  8. Gradl et al. (2006) Precipitation of nanoparticles in a T-mixer: coupling the particle population with hydrodynamics through direct numerical simulation (pp. 908-916) https://doi.org/10.1016/j.cep.2005.11.012
  9. Johnson and Prud’homme (2003) Flash nanoprecipitation of organic actives and block copolymers using a confined impinging jets mixer (pp. 1021-1024) https://doi.org/10.1071/CH03115
  10. Ventosa et al. (2005) New technologies for the preparation of micro- and nanostructured materials with potential applications in drug delivery and clinical diagnostics (pp. 11-20)
  11. Kim et al. (2005) Control of the particle properties of a drug substance by crystallization engineering and the effect on drug product formulation (pp. 894-901) https://doi.org/10.1021/op050091q
  12. Liversidge and Cundy (1995) Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: absolute oral bioavailability of nanocrystalline Danzol in beagle dogs (pp. 91-97) https://doi.org/10.1016/0378-5173(95)00122-Y
  13. Noyes and Whitney (1997) The rate of solution of solid substances in their own solutions (pp. 930-934) https://doi.org/10.1021/ja02086a003
  14. Kesisoglou et al. (2007) Nanosizing- oral formulation development and biopharmaceutical evaluation (pp. 631-644) https://doi.org/10.1016/j.addr.2007.05.003
  15. Mullin and Nyvlt (1971) Programmed cooling of batch crystallizers (pp. 369-377) https://doi.org/10.1016/0009-2509(71)83012-9
  16. Gabas and Lague′rie (1992) Batch crystallization of D-xylose by programmed cooling or by programmed adding of ethanol (pp. 3145-3148) https://doi.org/10.1016/0009-2509(92)87017-K
  17. Reverchon (1999) Supercritical antisolvent precipitation of micro- and nano-particles (pp. 1-21) https://doi.org/10.1016/S0896-8446(98)00129-6
  18. Charoenchaitrakool et al. (2000) Micronization by rapid expansion of supercritical solutions to enhance the dissolution rates of poorly water-soluble pharmaceuticals (pp. 4794-4802) https://doi.org/10.1021/ie000151a
  19. Turk et al. (2002) Micronization of pharmaceutical substances by the rapid expansion of supercritical solutions (RESS): a promising method to improve bioavailability of poorly soluble pharmaceutical agents (pp. 75-84) https://doi.org/10.1016/S0896-8446(01)00109-7
  20. Sarkari et al. (2002) Enhanced drug dissolution using evaporative precipitation into aqueous solution (pp. 17-31) https://doi.org/10.1016/S0378-5173(02)00072-8
  21. Bilati et al. (2005) Development of a nanoprecipitation method intended for the entrapment of hydrophilic drugs into nanoparticles (pp. 67-75) https://doi.org/10.1016/j.ejps.2004.09.011
  22. Hua et al. (2003) Spray freezing into liquid (SFL) particle engineering technology to enhance dissolution of poorly water-soluble drugs: organic solvent versus organic/aqueous co-solvent systems (pp. 295-303) https://doi.org/10.1016/S0928-0987(03)00203-3
  23. Debuigne et al. (2001) Synthesis of nimesulide nanoparticles in the microemulsion epikuron—isopropyl myristate/water/n-butanol (or Isopropanol) (pp. 90-101) https://doi.org/10.1006/jcis.2001.7879
  24. Trotta et al. (2003) Preparation of griseofulvin nanoparticles from water-dilutable microemulsions (pp. 235-242) https://doi.org/10.1016/S0378-5173(03)00029-2
  25. Howard et al. (2009) Process analytical technology based investigation of the polymorphic transformations during the antisolvent crystallization of sodium benzoate from IPA/Water mixture (pp. 3964-3975) https://doi.org/10.1021/cg900108e
  26. O’Grady et al. (2007) The effect of mixing on the metastable zone width and nucleation kinetics in the anti-solvent crystallization of benzoic acid (pp. 945-952) https://doi.org/10.1205/cherd06207
  27. Nagy et al. (2008) Modelling and control of combined cooling and anti-solvent crystallization processes (pp. 856-864) https://doi.org/10.1016/j.jprocont.2008.06.002
  28. Overhoff1, K.A., Johnston, K.P., Robert, O., Williams, R.O.: Improvement of dissolution rate of poorly water soluble drugs using a new particle engineering process: spray freezing into liquid, In: Polymeric Drug Delivery II, Chapter 20, pp 305–319. (2006)
  29. Jie-Xin et al. (2010) Microfluidic synthesis of amorphous cefuroxime axetil nanoparticles with size-dependent and enhanced dissolution rate (pp. 844-851)
  30. USP-32th edition, NF-27nd edition. In: Azithromycin; United state pharmacopeial convention. 12601, Twinbrook Parkway, Rockville, MD 20852, Vol. 2, pp. 1613–1615. United book press, Maryland (2008)
  31. Yuancai et al. (2009) Preparation and characterization of spironolactone nanoparticles by antisolvent precipitation (pp. 84-88) https://doi.org/10.1016/j.ijpharm.2009.03.013
  32. Gandhi et al. (2002) Characterization of azithromycin hydrates (pp. 175-184) https://doi.org/10.1016/S0928-0987(02)00087-8
  33. Choemunng and Na-Bangchang (2010) An alternative liquid chromatography-mass spectrometric method for the determination of azithromycin in human plasma and its application to pharmacokinetic study of patients with malaria, Southeast Asian (pp. 1048-1058)
  34. Hattori et al. (2013) Dissolution process analysis using model-free Noyes–Whitney integral equation (pp. 227-231) https://doi.org/10.1016/j.colsurfb.2012.08.017