Skip to main content

Advertisement

SpringerLink
Log in

Influence of Processing Parameters and Formulation Factors on the Bioadhesive, Temperature Stability and Drug Release Properties of Hot-Melt Extruded Films Containing Miconazole

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

Abstract

This study investigated the processing parameters and formulation factors on the bioadhesive properties, temperature stability properties, and drug release properties of miconazole in PolyOx® and Klucel® matrix systems produced by Hot-melt Extrusion (HME) technology. Miconazole incorporated into these matrix systems were found to be stable for 8 months by X-ray diffraction (XRD). The addition of miconazole increased area under the curve (AUC) at contact time intervals of 30 and 60 sec, while the bioadhesion decreased with an increase in processing temperatures. The release profiles suggest that a sustained release of miconazole was observed from all of the tested HME film formulations for approximately 10 h. The release from the optimal HME film extruded at 205°C was found to be significantly different than that extruded at 190°C. Therefore, this matrix system may address the present shortcomings of currently available therapy for oral and pharyngeal candidiasis.

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
Fig. 11

Similar content being viewed by others

References

  1. Sawyer PR, Brogden RN, Pinder RM, Speight TM, Avery GS. Miconazole: a review of its antifungal activity and therapeutic efficacy. Drugs. 1975;9(6):406–23.

    Article  CAS  PubMed  Google Scholar 

  2. Chang HT, Chen WC, Chen JS, Lu YC, Hsu SS, Wang JL, et al. Effect of miconazole on intracellular Ca2+ levels and proliferation in human osteosarcoma cells. Life Sci. 2005;76(18):2091–101.

    Article  CAS  PubMed  Google Scholar 

  3. Devaraj A, O’Beirne JP, Veasey R, Dunk AA. Interaction between warfarin and topical miconazole cream. Bmj. 2002;325(7355):77.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  4. Mohammed FA, Khedr H. Preparation and in vitro/in vivo evaluation of the buccal bioadhesive properties of slow-release tablets containing miconazole nitrate. Drug Dev Ind Pharm. 2003;29(3):321–37.

    Article  CAS  PubMed  Google Scholar 

  5. Hynninen VV, Olkkola KT, Neuvonen PJ, Laine K. Oral voriconazole and miconazole oral gel produce comparable effects on the pharmacokinetics and pharmacodynamics of etoricoxib. Eur J Clin Pharmacol. 2009;65(1):89–95.

    Article  CAS  PubMed  Google Scholar 

  6. Mandal TK. Swelling-controlled release system for the vaginal delivery of miconazole. Eur J Pharm Biopharm. 2000;50:7.

    Article  Google Scholar 

  7. Bioadhesion of Carbopol polymers, BF Goodrich Specialty Chemicals, Cleveland, Ohio. 1994: 7.

  8. Repka MA, McGinity JW. Bioadhesive properties of hydroxypropylcellulose topical films produced by hot-melt extrusion. J Control Release. 2001;70(3):341–51.

    Article  CAS  PubMed  Google Scholar 

  9. Repka MA, ElSohly MA, Munjal M, Ross SA. Temperature stability and bioadhesive properties of delta9-tetrahydrocannabinol incorporated hydroxypropylcellulose polymer matrix systems. Drug Dev Ind Pharm. 2006;32(1):21–32.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  10. Thumma S, Majumdar S, ElSohly MA, Gul W, Repka MA. Chemical stability and bioadhesive properties of an ester prodrug of 9-tetrahydrocannabinol in poly(ethylene oxide) matrices: Effect of formulation additives. Int J Pharm. 2008;362:7.

    Article  Google Scholar 

  11. Repka MA, McGinity JW. Physical-mechanical, moisture absorption and bioadhesive properties of hydroxypropylcellulose hot-melt extruded films. Biomaterials. 2000;21(14):1509–17.

    Article  CAS  PubMed  Google Scholar 

  12. Prodduturi, S., K.L. Urman, J.U. Otaigbe and M.A. Repka, Stabilization of hot-melt extrusion formulations containing solid solutions using polymer blends. AAPS PharmSciTech, 2007. 8(2): Article 50.

    Google Scholar 

Download references

Acknowledgments

This work was supported by the project of Research Center of Drug-Delivery Systems in Universities of Guangdong Province (No.: GCZX-A0802). In addition, this research was supported by Grant Number P20GM104931 from the National Institute of General Medical Sciences (NIGMS), a component of the National Institutes of Health (NIH). Its contents are solely the responsibility of the authors and do not necessarily represent the official view of NIGMS or NIH.

Author information

Authors and Affiliations

  1. GuangDong Research Center for Drug Delivery Systems, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, Guangdong, 510006, China

    Meiwan Chen & Chuanbin Wu

  2. Department of Pharmaceutics, School of Pharmacy, University of Mississippi, University, Mississippi, 38677, USA

    Meiwan Chen, Jiannan Lu, Weibin Deng, Abhilasha Singh, Noorullah Naqvi Mohammed & Michael A. Repka

  3. State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical Sciences, University of Macau, Macau, 999078, China

    Meiwan Chen

Authors
  1. Meiwan Chen
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Jiannan Lu
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Weibin Deng
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Abhilasha Singh
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Noorullah Naqvi Mohammed
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. Michael A. Repka
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. Chuanbin Wu
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Chuanbin Wu.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Chen, M., Lu, J., Deng, W. et al. Influence of Processing Parameters and Formulation Factors on the Bioadhesive, Temperature Stability and Drug Release Properties of Hot-Melt Extruded Films Containing Miconazole. AAPS PharmSciTech 15, 522–529 (2014). https://doi.org/10.1208/s12249-013-0029-z

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-013-0029-z

KEY WORDS

Search

Navigation