Skip to main content
SpringerLink
Log in

Meloxicam Carrier Systems Having Enhanced Release and Aqueous Wettability Prepared Using Micro-suspensions in Different Liquid Media

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

Abstract

One of the conventional methods of alleviating the problem of poor drug solubility is the particle size reduction. The efficiency of this approach depends on successful formulation suppressing the drug agglomeration. The aim of this study was to circumvent the dissolution problems of model hydrophobic meloxicam drug (MLX) by using liquid media of different wetting capacity to comminute and formulate a rapidly dissolving carrier system without the use of surfactants. Micro-suspensions of MLX were prepared by ball milling, using water or n-Heptane as a liquid medium. The suspensions were used as granulation liquids to formulate granulate from microcrystalline cellulose and lactose mixture. The release kinetics from prepared granulates were studied using the USP-4 dissolution apparatus. Micro-suspensions prepared via wet milling in non-water liquid media exhibited a massive improvement of release rate compared with source meloxicam and they outperformed their water-milled counterparts. The release rates from those formulations, despite not comprising any surfactant, were comparable to those obtained by different authors using surfactant stabilized nanosuspension formulations. Thus, they can present an interesting formulation alternative for hydrophobic drugs that are dissolution limited.

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

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
Fig. 8
Fig. 9
Fig. 10

Similar content being viewed by others

References

  1. Chu KR, Lee E, Jeong SH, Park E-S. Effect of particle size on the dissolution behaviors of poorly water-soluble drugs. Arch Pharm Res. 2012;35(7):1187–95. https://doi.org/10.1007/s12272-012-0709-3.

    Article  CAS  PubMed  Google Scholar 

  2. Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN Pharmaceutics. 2012;2012:10–0. https://doi.org/10.5402/2012/195727.

  3. Al-Kassas R, Bansal M, Shaw J. Nanosizing techniques for improving bioavailability of drugs. J Control Release. 2017;260:202–12. https://doi.org/10.1016/j.jconrel.2017.06.003.

    Article  CAS  PubMed  Google Scholar 

  4. Patel VR, Agrawal YK. Nanosuspension: an approach to enhance solubility of drugs. J Adv Pharm Technol Res. 2011;2(2):81–7. https://doi.org/10.4103/2231-4040.82950.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  5. Malamatari M, Taylor KMG, Malamataris S, Douroumis D, Kachrimanis K. Pharmaceutical nanocrystals: production by wet milling and applications. Drug Discov Today. 2018;23(3):534–47. https://doi.org/10.1016/j.drudis.2018.01.016.

    Article  CAS  PubMed  Google Scholar 

  6. Bhakay A, Merwade M, Bilgili E, Dave RN. Novel aspects of wet milling for the production of microsuspensions and nanosuspensions of poorly water-soluble drugs. Drug Dev Ind Pharm. 2011;37(8):963–76. https://doi.org/10.3109/03639045.2010.551775.

    Article  CAS  PubMed  Google Scholar 

  7. Möschwitzer J. Particle size reduction technologies in the pharmaceutical development process. Am Pharm Rev. 2010;2010:54–9.

    Google Scholar 

  8. Rasenack N, Müller BW. Micron-size drug particles: common and novel micronization techniques. Pharm Dev Technol. 2004;9(1):1–13. https://doi.org/10.1081/PDT-120027417.

    Article  CAS  PubMed  Google Scholar 

  9. Wang Y, Zheng Y, Zhang L, Wang Q, Zhang D. Stability of nanosuspensions in drug delivery. J Control Release. 2013;172(3):1126–41. https://doi.org/10.1016/j.jconrel.2013.08.006.

    Article  CAS  PubMed  Google Scholar 

  10. Oliveira ÉFS, Azevedo RCP, Bonfilio R, Oliveira DB, Ribeiro GP, Araújo MB. Dissolution test optimization for Meloxicam in the tablet pharmaceutical form. Braz J Pharm Sci. 2009;45:67–73.

    Article  CAS  Google Scholar 

  11. Ambrus R, Kocbek P, Kristl J, Šibanc R, Rajkó R, Szabó-Révész P. Investigation of preparation parameters to improve the dissolution of poorly water-soluble meloxicam. Int J Pharm. 2009;381(2):153–9. https://doi.org/10.1016/j.ijpharm.2009.07.009.

    Article  CAS  PubMed  Google Scholar 

  12. Ochi M, Kawachi T, Toita E, Hashimoto I, Yuminoki K, Onoue S, et al. Development of nanocrystal formulation of meloxicam with improved dissolution and pharmacokinetic behaviors. Int J Pharm. 2014;474(1):151–6. https://doi.org/10.1016/j.ijpharm.2014.08.022.

    Article  CAS  PubMed  Google Scholar 

  13. Liu T, Yao G, Zhang X, Zuo X, Wang L, Yin H, et al. Systematical investigation of different drug nanocrystal technologies to produce fast dissolving meloxicam tablets. AAPS PharmSciTech. 2018;19(2):783–91. https://doi.org/10.1208/s12249-017-0889-8.

  14. Kassem MAA, ElMeshad AN, Fares AR. Enhanced solubility and dissolution rate of lacidipine nanosuspension: formulation via antisolvent sonoprecipitation technique and optimization using Box–Behnken design. AAPS PharmSciTech. 2017;18(4):983–96. https://doi.org/10.1208/s12249-016-0604-1.

    Article  CAS  PubMed  Google Scholar 

Download references

Acknowledgments

This work was realized within the Operational Programme Prague Competitiveness (CZ.2.16/3.1.00/24501) and “National Program of Sustainability” (NPU I LO1613 MSMT-43760/2015).

Author information

Authors and Affiliations

  1. Department of Organic Technology, University of Chemistry and Technology, Technická 5, 166 28, Prague 6, Czech Republic

    Nikita Marinko & Petr Zámostný

Authors
  1. Nikita Marinko
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Petr Zámostný
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Petr Zámostný.

Additional information

Publisher’s Note

Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Marinko, N., Zámostný, P. Meloxicam Carrier Systems Having Enhanced Release and Aqueous Wettability Prepared Using Micro-suspensions in Different Liquid Media. AAPS PharmSciTech 21, 155 (2020). https://doi.org/10.1208/s12249-020-01701-4

Download citation

  • Received:

  • Accepted:

  • Published:

  • DOI: https://doi.org/10.1208/s12249-020-01701-4

Key Words

Search

Navigation