Skip to main content
Log in

Preparation and evaluation of flutamide mucoadhesive microparticles loaded poloxamer suppositories

  • Research Article
  • Published:
Journal of Pharmaceutical Investigation Aims and scope Submit manuscript

Abstract

Flutamide (FLT) is a potent non-steroidal anti-androgen drug primarily used in palliative treatment of prostate cancer that inhibits androgen uptake and/or nuclear binding of androgen in target tissues. The objective of the present study was to prepare FLT mucoadhesive microparticles. FLT mucoadhesive microparticles were developed by ionic gelation technique using hydrophilic polymers such as sodium alginate and Carbopol 971P and optimised by one factorial design of response surface methodology. The optimised microparticles were characterised by zeta potential study, in vitro release study, scanning electron microscopy and X-ray diffraction study. The stability studies performed on the optimized batch at 40 °C/75 % RH for 90 days indicated no significant change in the physicochemical properties. Optimised batch of microparticles was further developed as suppository system using different proportions of Poloxamer 407:Poloxamer 188 as suppository base by fusion method.

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.

Fig. 1
Fig. 2
Fig. 3
Fig. 4

Similar content being viewed by others

References

  • Barichello JM, Morishita M, Takayama K, Nagai T (1999) Absorption of insulin from pluronic F-127 gels following subcutaneous administration in rats. Int J Pharm 184(2):189–198

    Article  CAS  PubMed  Google Scholar 

  • Belgamwar V, Shah V, Surana SJ (2009) Formulation and evaluation of oral mucoadhesive multiparticulate system containing metoprolol tartarate: an in vitro-ex vivo characterization. Curr Drug Deliv. 6:113–121

    Article  CAS  PubMed  Google Scholar 

  • Boer AG, Breimer DD (1997) Hepatic first-pass effect and controlled drug delivery following rectal administration. Adv Drug Deliv Rev 28(2):229–237

    Article  Google Scholar 

  • Chen PC, Kohane DS, Park YJ, Bartlett RH, Langer R, Yang VC (2004) Injectable microparticle-gel system for prolonged and localized lidocaine release II. In vivo aesthetic effects. J Biomed Mater Res 70(3):459–466

    Article  Google Scholar 

  • Choi H, Oh Y, Kim Y, Kim JO, Yoo B, Rhee J, Kang Lee KC, Kim D, Park Y, Kim C, Yong CS (2005) Physicochemical characterization and in vivo evaluation of poloxamer-based solid suppository containing diclofenac sodium in rats Int. J Pharm 301:54–61

    Google Scholar 

  • Chowdhary KPR, Rao Y (2004) Mucoadhesive microspheres for controlled drug delivery. Biol Pharm Bull 27(11):1717–1724

    Article  Google Scholar 

  • Dumortier G, Grossiord JL, Agnely F, Chaumeil JC (2006) A review of poloxamer 407 pharmaceutical and pharmacological characteristics. Pharm Res 23(12):2709–2728

    Article  CAS  PubMed  Google Scholar 

  • Elgindy N, Elkhodairy K, Molokhia A, Elzoghby A (2010) Lyophilization monophase solution technique for improvement of the physicochemical properties of an anticancer drug, flutamide. Eur J Pharm Biopharm 74:397–405

    Article  CAS  PubMed  Google Scholar 

  • Elgindy N, Elkhodairy K, Molokhia A, Elzoghby A (2011a) Lyophilization monophase solution technique for preparation of amorphous flutamide dispersions. Drug Dev Ind Pharm 1–11:539232. doi:10.3109/03639045.2010

    Google Scholar 

  • Elgindy N, Elkhodairy K, Molokhia A, Elzoghby A (2011b) Lyophilized flutamide dispersions with polyols and amino acids: preparation and in vitro evaluation. Drug Dev Ind Pharm 37:446–455

    Article  CAS  PubMed  Google Scholar 

  • Gao W (2010) Androgen receptor as a therapeutic target. Adv Drug Deliv Rev 62:1277–1284

    Article  CAS  PubMed  Google Scholar 

  • Madhusudhan B, Rambhau D, Apte S, Gopinath D (2007) Oral bioavailability of flutamide from 1-O-alkylglycerol stabilized o/w nanoemulsions. J Dispers Sci Technol 28(8):1254–1261

    Article  CAS  Google Scholar 

  • Nesalin A, Gowthamarajan K, Somashekhara C (2009) Formulation and evaluation of nanoparticles containing flutamide. Int J Chem Tech Res 1:1331–1334

    CAS  Google Scholar 

  • Peppas NA, Buri PA (1985) Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues. J Control Release 2:257–275

    Article  CAS  Google Scholar 

  • Ryu JM, Chung SJ, Lee MH, Kim CK, Shim CK (1999) Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum. J Control Release 59(2):163–172

    Article  CAS  PubMed  Google Scholar 

  • Sweetman SC (2005) Martindale the complete drug reference, 34th edn. Pharmaceutical Press, London

    Google Scholar 

  • Vasir J, Tambwekar K, Garg S (2003) Bioadhesive microspheres as a controlled drug delivery system. Int J Pharm 255:13–32

    Article  CAS  PubMed  Google Scholar 

  • Vyas SP, Khar RK (2008) Targeted and controlled drug delivery novel carrier systems, 1st edn. CBS Publishers & Distributers, New Delhi, p 417

    Google Scholar 

  • Wiebe L, Zuo Z, Tam Y, Diakur J (2002) Hydroxypropyl β-cyclodextrin flutamide inclusion complex. II. Oral and intravenous pharmacokinetics of flutamide in the rat. J Pharm Pharm Sci. 5(3):292–298

    PubMed  Google Scholar 

Download references

Acknowledgments

The authors are thankful to Cipla Ltd., Mumbai, India for providing gift sample of flutamide.

Conflicts of the Interest and State of human and Animal Rights

B.S. Patil, H.S. Mahajan, and S.J. Surana declare that they have no conflict of interest. This article does not contain any studies with human and animal subjects performed by any of the authors.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to B. S. Patil.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Patil, B.S., Mahajan, H.S. & Surana, S.J. Preparation and evaluation of flutamide mucoadhesive microparticles loaded poloxamer suppositories. Journal of Pharmaceutical Investigation 46, 139–146 (2016). https://doi.org/10.1007/s40005-015-0217-9

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40005-015-0217-9

Keywords

Navigation