Skip to main content
SpringerLink
Log in

The Studies of Phase Equilibria and Efficiency Assessment for Self-Emulsifying Lipid-Based Formulations

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

Abstract

The study was designed to build up a database for the evaluation of the self-emulsifying lipid formulations performance. A standard assessment method was constructed to evaluate the self-emulsifying efficiency of the formulations based on five parameters including excipients miscibility, spontaneity, dispersibility, homogeneity, and physical appearance. Equilibrium phase studies were conducted to investigate the phase changes of the anhydrous formulation in response to aqueous dilution. Droplet size studies were carried out to assess the influence of lipid and surfactant portions on the resulted droplet size upon aqueous dilution. Formulations containing mixed glycerides showed enhanced self-emulsification with both lipophilic and hydrophilic surfactants. Increasing the polarity of the lipid portion in the formulation leaded to progressive water solubilization capacity. In addition, formulations containing medium chain mixed glycerides and hydrophilic surfactants showed lower droplet size compared with their long chain and lipophilic counterparts. The inclusion of mixed glycerides in the lipid formulations enormously enhances the formulation efficiency.

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

Similar content being viewed by others

REFERENCES

  1. Rai A, Tiwari G, Tiwari R. Self-emulsifying drug delivery system: an approach to enhance solubility. Syst Rev Pharm. 2010;1:133–40.

    Article  Google Scholar 

  2. Porter CJH, Trevaskis NL, Charman WN. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discov. 2007;6:231–48.

    Article  PubMed  CAS  Google Scholar 

  3. Rahman MA, Harwansh R, Mirza MA, Hussain S, Hussain A. Oral lipid based drug delivery system (LBDDS): formulation, characterization and application: a review. Curr Drug Deliv. 2011;8:330–45.

    Article  PubMed  CAS  Google Scholar 

  4. Kohli K, Chopra S, Dhar D, Arora S, Khar RK. Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability. Drug Discov Today. 2010;15:958–65.

    Article  PubMed  CAS  Google Scholar 

  5. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother. 2004;58:173–82.

    Article  PubMed  Google Scholar 

  6. Gershanik T, Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur J Pharm Biopharm. 2000;50:179–88.

    Article  PubMed  CAS  Google Scholar 

  7. Pouton CW. Formulation of self-emulsifying drug delivery systems. Adv Drug Del Rev. 1997;25:47–58.

    Article  CAS  Google Scholar 

  8. Pouton CW. Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification. Int J Pharm. 1985;27:335–48.

    Article  CAS  Google Scholar 

  9. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and “self-microemulsifying” drug delivery systems. Eur J Pharm Sci. 2000;11:S93–8.

    Article  PubMed  CAS  Google Scholar 

  10. Pouton CW. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci. 2006;29:278–87.

    Article  PubMed  CAS  Google Scholar 

  11. Porter C, Pouton C, Cuine J, Charman W. Enhancing intestinal drug solubilisation using lipid-based delivery systems. Adv Drug Del Rev. 2008;60:673–91.

    Article  CAS  Google Scholar 

  12. Craig DQM, Barker SA, Banning D, Booth SW. An investigation into the mechanisms of self-emulsification using particle size analysis and low frequency dielectric spectroscopy. Int J Pharm. 1995;114:103–10.

    Article  CAS  Google Scholar 

  13. Kommuru TR, Gurley B, Khan MA, Reddy IK. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int J Pharm. 2001;212:233–46.

    Article  PubMed  CAS  Google Scholar 

  14. Nekkanti V, Karatgi P, Prabhu R, Pillai R. Solid self-microemulsifying formulation for candesartan cilexetil. AAPS PharmSciTech. 2010;11:9–17.

    Article  PubMed  CAS  Google Scholar 

  15. Thakkar H, Nangesh J, Parmar M, Patel D. Formulation and characterization of lipid-based drug delivery system of raloxifene-microemulsion and self-microemulsifying drug delivery system. J Pharm Bioallied Sci. 2011;3(3):442–8.

    Article  PubMed  CAS  Google Scholar 

  16. Date AA, Nagarsenker MS. Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm. 2007;329:166–72.

    Article  PubMed  CAS  Google Scholar 

  17. Kossena GA, Charman WN, Boyd BJ, Dunstan DE, Porter CJ. Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach. J Pharm Sci. 2004;93:332–48.

    Article  PubMed  CAS  Google Scholar 

  18. Mohsin K, Long MA, Pouton CW. Design of lipid-based formulations for oral administration of poorly water-soluble drugs: precipitation of drug after dispersion of formulations in aqueous solution. J Pharm Sci. 2009;98:3582–95.

    Article  PubMed  CAS  Google Scholar 

  19. Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm. 2004;274:65–73.

    Article  PubMed  CAS  Google Scholar 

  20. Atef E, Belmonte AA. Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur J Pharm Sci. 2008;35:257–63.

    Article  PubMed  CAS  Google Scholar 

  21. Wakerly MG, Pouton CW, Meakin BJ, Morton FS. Self-emulsification of vegetable oil-nonionic surfactant mixtures. In: Scamehorn JF, editor. Phenomena in mixed surfactant systems. Washington: American Chemical Society; 1986. p. 242–55.

    Chapter  Google Scholar 

  22. Charman SA, Charman WN, Rogge MC, Wilson TD, Dutko FJ, Pouton CW. Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm Res. 1992;9:87–93.

    Article  PubMed  CAS  Google Scholar 

  23. Shah NH, Carvajal MT, Patel CI, Infeld MH, Malick AW. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int J Pharm. 1994;106:15–23.

    Article  CAS  Google Scholar 

  24. Pouton CW, Porter CJ. Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies. Adv Drug Deliv Rev. 2008;60:625–37.

    Article  PubMed  CAS  Google Scholar 

Download references

ACKNOWLEDGMENTS

The authors would to like to acknowledge the SABIC graduate student fund (No: MED-30-44). The authors are grateful to the distinguished scientific support from Prof. Adel Sakr.

Author information

Authors and Affiliations

  1. Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Kingdom of Saudi Arabia

    Ahmad Abdul-Wahhab Shahba, Kazi Mohsin & Fars Kaed Alanazi

Authors
  1. Ahmad Abdul-Wahhab Shahba
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Kazi Mohsin
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Fars Kaed Alanazi
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Kazi Mohsin.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Shahba, A.AW., Mohsin, K. & Alanazi, F.K. The Studies of Phase Equilibria and Efficiency Assessment for Self-Emulsifying Lipid-Based Formulations. AAPS PharmSciTech 13, 522–533 (2012). https://doi.org/10.1208/s12249-012-9773-8

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-012-9773-8

KEY WORDS

Search

Navigation