Skip to main content

Advertisement

SpringerLink
Log in

Polydimethylsiloxane–Indomethacin Blends and Nanoparticles

  • Research Article
  • Published:
AAPS PharmSciTech Aims and scope Submit manuscript

Abstract

A series of blends of polydimethylsiloxane (PDMS) and indomethacin (IMC), containing 20–80 wt.% IMC were obtained and characterized by differential scanning calorimetry, Fourier transform–infrared spectroscopy, and powder X-ray diffraction in order to observe the mutual influence of the two components. The main thermal transitions of PDMS remained un-changed. Both the solvent (tetrahydrofuran, THF) and the PDMS influenced the crystalline form of IMC. The blends were subsequently re-dissolved in THF, with or without cross-linking reagents added and precipitated into diluted aqueous solutions of siloxane-based surfactants. The resulted nanoparticles were analyzed by dynamic light scattering and scanning electron microscopy. Most of the particles had diameters between 200 and 300 nm. The surfactants, the IMC content and the cross-linking influenced the particles size and polydispersity, as well as the nanoparticle yield. The maximum drug release from selected aqueous formulations was 30%.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

Scheme 1
Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7

Similar content being viewed by others

REFERENCES

  1. Habal MB. The biologic basis for the clinical application of the silicones. A correlate to their biocompatibility. Arch Surg. 1984;119(7):843–8.

    Article  PubMed  CAS  Google Scholar 

  2. Thomas X. Silicone adhesives in healthcare applications. http://www.dowcorning.com/content/publishedlit/52-1057-01.pdf. Accessed 10 Jan 2013.

  3. Andriot M, Chao SH, Colas A, Cray S, de Buyl F, DeGroot JV, Dupont A, Easton T, Garaud JL, Gerlach E, Gubbels F, Jungk M, Leadley S, Lecomte JP, Lenoble B, Meeks R, Mountney A, Shearer G, Stassen S, Stevens C, Thomas X, Wolf AT. Silicones in industrial applications. In: De Jaeger R, Gleria M, editors. Inorganic Polymers. Nova; 2007. p. 61–161.

  4. European Centre for Ecotoxicology and Toxicology of Chemicals. Joint Assessment of Commodity Chemicals JACC 055: Linear Polydimethylsiloxanes CAS No. 63148-62-9 (Second Edition). Brussels. 2011.

  5. Noll W. Chemistry and technology of silicone. New York: Academic; 1968.

    Google Scholar 

  6. Colas A. Silicones in pharmaceutical applications. http://www.dowcorning.com/content/publishedlit/51-993a-01.pdf. Accessed 13 Dec 2012.

  7. Di Colo G. Controlled drug release from implantable matrices based on hydrophobic polymers. Biomaterials. 1992;13:850–6.

    Article  PubMed  Google Scholar 

  8. Racles C, Hamaide T, Ioanid A. Siloxane surfactants in polymer nanoparticles formulation. Appl Organomet Chem. 2006;20:235–45.

    Article  CAS  Google Scholar 

  9. Racles C, Cazacu M, Hitruc G, Hamaide T. On the feasibility of chemical reactions in the presence of siloxane-based surfactants. Colloid Polym Sci. 2009;287:461–70.

    Article  CAS  Google Scholar 

  10. Racles C, Alexandru M, Cazacu M, Ioanid A, Hamaide T. Obtention des elastomeres silicones en nanoreacteurs siloxane-organiques. Rev Roum Chim. 2009;54:583–8.

    CAS  Google Scholar 

  11. Hadgraft J, Plessis J, Goosen C. The selection of NSAIDs for dermal delivery. Int J Pharm. 2000;207:31–7.

    Article  PubMed  CAS  Google Scholar 

  12. Cordero J, Camacho M, Obach R, Domenench J, Vila L. In vitro based index of topical anti-inflammatory activity to compare a series of NSAIDs. Eur J Pharm Biopharm. 2001;51:135–42.

    Article  PubMed  CAS  Google Scholar 

  13. Rhee Y, Choi J, Park E, Chi S. Transdermal delivery of ketoprofen using microemulsions. Int J Pharm. 2001;228:161–70.

    Article  PubMed  CAS  Google Scholar 

  14. Kawashima Y. Nanoparticulate systems for improved drug delivery. Adv Drug Del Rev. 2001;47:1–2.

    Article  CAS  Google Scholar 

  15. Panyam J, Labhasetwar V. Biodegradable nanoparticle from drug and gene delivery to cells and tissue. Adv Drug Del Rev. 2003;55:329–47.

    Article  CAS  Google Scholar 

  16. Petros RA, DeSimone JM. Strategies in the design of nanoparticles for therapeutic applications. Nature Reviews: Drug Discovery. 2010;9:615–27.

    Article  PubMed  CAS  Google Scholar 

  17. Racles C. Siloxane-based surfactants containing tromethamol units. Soft Materials. 2010;8:1–11.

    Article  Google Scholar 

  18. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52:1145–9.

    Article  PubMed  CAS  Google Scholar 

  19. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15:25–35.

    Article  CAS  Google Scholar 

  20. Ritger PL, Peppas NA. A simple equation for description of solute release I. Fickian and non-Fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs. J Control Release. 1987;5:23–6.

    Article  CAS  Google Scholar 

  21. Martena V, Censi R, Hoti E, Malaj L, Di Martino P. Indomethacin nanocrystals prepared by different laboratory scale methods: effect on crystalline form and dissolution behavior. J Nanopart Res. 2012;14:1275. doi:10.1007/s11051-012-1275-9.

    Article  Google Scholar 

  22. Taylor LS, Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm Res. 1997;14:1691–8.

    Article  PubMed  CAS  Google Scholar 

  23. Yilgor I, McGrath JE. Polysiloxane containing copolymers: a survey of recent developments. Adv Polym Sci. 1988;86:1–87.

    Article  CAS  Google Scholar 

  24. Pan X, Julian T, Augsburger L. Quantitative measurement of indomethacin crystallinity in indomethacin-silica gel binary system using differential scanning calorimetry and X-ray powder diffractometry. AAPS PharmSciTech. 2006;7(1):11.

    Article  Google Scholar 

  25. Crowley KJ, Zografi G. Cryogenic grinding of indomethacin polymorphs and solvates: assessment of amorphous phase formation and amorphous phase physical stability. J Pharm Sci. 2002;91:492–507.

    Article  PubMed  CAS  Google Scholar 

  26. Greco K, Bogner R. Crystallization of amorphous indomethacin during dissolution: effect of processing and annealing. Mol Pharm. 2010;7:1406–18. doi:10.1021/mp1000197.

    Article  PubMed  CAS  Google Scholar 

  27. Qi C, Xia X, Zhang W, Xie C, Cai S. Indomethacin/Cu/LDPE porous composite for medicated copper intrauterine devices with controlled release performances. Compos Sci Technol. 2012;72:428–34. doi:10.1016/j.compscitech.2011.12.004.

    Article  CAS  Google Scholar 

  28. Bodmeier R, Chen H. Indomethacin polymeric nanosuspensions prepared by microfluidization. J Contr Release. 1990;12:223–33.

    Article  CAS  Google Scholar 

  29. Raval A, Parikha J, Engineer C. Dexamethasone eluting biodegradable polymeric matrix coated stent for intravascular drug delivery. Chem Eng Res Des. 2010;88:1479–84. doi:10.1016/j.cherd.2010.03.007.

    Article  CAS  Google Scholar 

  30. Dash AK, Suryanarayanan R. An implantable dosage form for the treatment of bone infections. Pharm Res. 1992;9:993–1002.

    Article  PubMed  CAS  Google Scholar 

  31. Yohe ST, Colson YL, Grinstaff MW. Superhydrophobic materials for tunable drug release: using displacement of air to control delivery rates. J Am Chem Soc. 2012;134:2016–9. doi:10.1021/ja211148a.

    Article  PubMed  CAS  Google Scholar 

Download references

ACKNOWLEDGMENTS

This work was partly supported by a grant of the Romanian National Authority for Scientific Research, CNCS–UEFISCDI, project number PN-II-ID-PCCE-2011-2-0028. The author thanks Dr. V. Cozan and Prof. S. Shova for helpful discussions.

Author information

Authors and Affiliations

  1. “Petru Poni” Institute of Macromolecular Chemistry, Aleea Gr. Ghica Voda 41A, 700487, Iasi, Romania

    Carmen Racles

  2. Department of Natural and Synthetic Polymers, “Gh. Asachi” Technical University, 700050, Iasi, Romania

    Carmen Racles

Authors
  1. Carmen Racles
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Carmen Racles.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Racles, C. Polydimethylsiloxane–Indomethacin Blends and Nanoparticles. AAPS PharmSciTech 14, 968–976 (2013). https://doi.org/10.1208/s12249-013-9989-2

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-013-9989-2

Key words

Search

Navigation