Skip to main content
Log in

Nanoparticles containing ketoprofen and acrylic polymers prepared by an aerosol flow reactor method

  • Published:
AAPS PharmSciTech Aims and scope Submit manuscript

Abstract

The purpose of this study was to outline the effects of interactions between a model drug and various acrylic polymers on the physical properties of nanoparticles prepared by an aerosol flow reactor method. The amount of model drug, ketoprofen, in the nanoparticles was varied, and the nanoparticles were analyzed for particle size distribution, particle morphology, thermal properties, IR spectroscopy, and drug release. The nanoparticles produced were spherical, amorphous, and had a matrix-type structure. Ketoprofen crystallization was observed when the amount of drug in Eudragit L nanoparticles was more than 33% (wt/wt). For Eudragit E and Eudragit RS nanoparticles, the drug acted as an effective plasticizer resulting in lowering of the glass transition of the polymer. Two factors affected the preparation of nanoparticles by the aerosol flow reactor method, namely, the solubility of the drug in the polymer matrix and the thermal properties of the resulting drug-polymer matrix.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Kreuter J. Nanoparticles. In: Swarbrick J, Boylan J C, eds.Encyclopedia of Pharmaceutical Technology. Vol. 10. New York, NY: Marcel Dekker, 1994:165–190.

    Google Scholar 

  2. Couvreur P, Dubernet C, Puisieux F. Controlled drug delivery with nanoparticles: current possibilities and future trends.Eur J Pharm Biopharm. 1995;41:2–13.

    CAS  Google Scholar 

  3. Brigger I, Dubernet C, Couvreur P. Nanoparticles in cancer therapy and diagnosis.Adv Drug Deliv Rev. 2002;54:631–651.

    Article  CAS  Google Scholar 

  4. Peltonen L, Koistinen P, Karjalainen M, Häkkinen A, Hirvonen J. The effect of cosolvents on the formulation of nanoparticles from low-molecular-weight poly(1)lactide.AAPS PharmSciTech. 2002;3:E32.

    Article  Google Scholar 

  5. Damgé C, Michel C, Aprahamian M, Couvreur P, Devissaguet, JP. Nanocapsules as carriers for oral peptide delivery.J Control Release. 1990;13:233–239.

    Article  Google Scholar 

  6. Damgé C, Vranckx H, Balschmidt P, Couvreur P. Poly(alkyl cyanoacrylate) nanospheres for oral administration of insulin.J Pharm Sci. 1997;86:1403–1409.

    Article  Google Scholar 

  7. Chen X, Young TJ, Sarkari M, Williams RO III, Johnston KP. Preparation of cyclosporine A nanoparticles by evaporative precipitation into aqueous solution.Int J Pharm. 2002;242:3–14.

    Article  CAS  Google Scholar 

  8. Eerikäinen H, Kauppinen EI. Preparation of polymeric nanoparticles containing corticosteroid by a novel aerosol flow reactor method.Int J Pharm. 2003;263:69–83.

    Article  Google Scholar 

  9. Eerikäinen H, Kauppinen EI, Kansikas J. Polymeric drug nanoparticles prepared by an aerosol flow reactor method.Pharm Res. 2004;21:136–143.

    Article  Google Scholar 

  10. Shukla AJ. Polymethacrylates. In: Wade A, Weller P J, eds.Handbook of Pharmaceutical Excipients. 2nd ed. Washington, DC: American Pharmaceutical Association, Pharmaceutical Press, 1994.

    Google Scholar 

  11. Dittgen M, Durani M, Lehmann K. Acrylic polymers: a review of pharmaceutical applications.STP Pharma Sci. 1997;7:403–437.

    CAS  Google Scholar 

  12. US Pharmacopeia XXVII. <724> Drug Release. Rockville, MD: United States Pharmacopeial Convention; 2003.

  13. US Pharmacopeia XXVII. <711> Dissolution. Rockville, MD: United States Pharmacopeial Convention; 2003.

  14. TSI Incorporated.Model 3075/3076 Constant Output Atomizer Instruction Manual. St Paul, MN: TSI Incorporated; 2000.

  15. Lefebvre AH. Atomization and sprays. In: Chigier N, ed.Combustion: An International Series New York, NY: Hemisphere Publishing Corporation; 1989.

    Google Scholar 

  16. Bodmeier R, Chen H. Preparation and characterization of microspheres containing the anti-inflammatory agents, indomethacin, ibuprofen, and ketoprofen.J Control Release. 1989;10:167–175.

    Article  CAS  Google Scholar 

  17. Habib MJ, Mesue R. Development of controlled release formulations of ketoprofen for oral use.Drug Dev Ind Pharm. 1995;21:1463–1472.

    Article  CAS  Google Scholar 

  18. Dubernet C, Rouland JC, Benoit JP. Ibuprofen-loaded ethylcellulose microspheres: analysis of the matrix structure by thermal analysis.J Pharm Sci. 1991;80:1029–1033.

    Article  CAS  Google Scholar 

  19. Palmieri GF, Bonacucina G, Di Martino P, Martelli S. Gastro-resistant microspheres containing ketoprofen.J Microencapsul. 2002;19:111–119.

    Article  CAS  Google Scholar 

  20. 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 PharmSciTech. 2002;3:E10.

    Article  Google Scholar 

  21. Wunderlich B.Thermal Analysis. San Diego, CA: Academic Press, Inc; 1990.

    Google Scholar 

  22. Dubernet C. Thermoanalysis of microspheres.Thermochim Acta. 1995;248:259–269.

    Article  Google Scholar 

  23. Wu C, McGinity JW. Non-traditional plasticization of polymeric films.Int J Pharm. 1999;177:15–27.

    Article  CAS  Google Scholar 

  24. Wu C, McGinity JW. Influence of ibuprofen as a solid-state plasticizer in Eudragit RS 30 D on the physicochemical properties of coated beads.AAPS PharmSciTech. 2001;2:E24.

    Article  Google Scholar 

  25. Sancin P, Caputo O, Cavallari C, et al. Effects of ultrasound-assisted compaction on Ketoprofen/Eudragit S100 mixtures.Eur J Pharm Sci. 1999;7:207–213.

    Article  CAS  Google Scholar 

  26. Mura P, Faucci MT, Parrini PL, Furlanetto S, Pinzauti S. Influence of the preparation method on the physicochemical properties of ketoprofen-cyclodextrin binary systems.Int J Pharm. 1999;179:117–128.

    Article  CAS  Google Scholar 

  27. Lin S-Y, Liao C-M, Hsiue G-H, Liang R-C. Study of a theophylline-Eudragit L mixture using a combined system of microscopic Fourier-transform infrared spectroscopy and differential scanning calorimetry.Thermochim Acta. 1995;254:153–166.

    Article  CAS  Google Scholar 

  28. Lin SY, Peng RI. Solid-state interaction studies of drugs/polymers: I. Indomethacin/Eudragit E, RL or S resins.STP Pharm Sci. 1993;3:465–471.

    CAS  Google Scholar 

  29. Lin S-Y, Yu H-L, Li M-J. Formation of six-membere cyclic anhydrides by thermally induced intramolecular ester condensation in Eudragit E film.Polym. 1999;40:3589–3593.

    Article  CAS  Google Scholar 

  30. Krause H-J, Schwarz A, Rohdewald P. Polyactic acid nanoparticles, a colloidal delivery system for lipophilic drugs.Int J Pharm. 1985;27:145–155.

    Article  CAS  Google Scholar 

  31. Higuchi T. Mechanism of sustained-action medication.J Pharm Sci. 1963;52:1145–1149.

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Esko I. Kauppinen.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Eerikäinen, H., Peltonen, L., Raula, J. et al. Nanoparticles containing ketoprofen and acrylic polymers prepared by an aerosol flow reactor method. AAPS PharmSciTech 5, 68 (2004). https://doi.org/10.1208/pt050468

Download citation

  • Received:

  • Accepted:

  • DOI: https://doi.org/10.1208/pt050468

Keywords

Navigation