Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
권호 표지
DOI QR코드

DOI QR Code

The Functional Behaviors of Cosurfactant in Design of Self-nanoemulsifying Drug Delivery Systems

  • Received : 2010.07.21
  • Accepted : 2010.08.13
  • Published : 2010.10.20
Download PDF
⟨ Previous Next ⟩

Abstract

Nanoemulsions have been widely investigated for many years because of their attractive and unique characteristics. Nanoemulsions are composed of oil, surfactant, co-surfactant and water. Especially, cosurfactant plays a critical role in formation of nanoemulsions. In pharmaceutical area, a pre-concentrate form of nanoemulsions which is known as self-nanoemulsifying drug delivery systems (SNEDDS) was available for some water-insoluble drugs. In this study, we investigated the functional behaviors of cosurfactant in design of SNEDDS and nanoemulsions. Cremophor RH 40$^{(R)}$, Propylene carbonate and medium chain triglyceride were selected for surfactant, cosurfactant and oil, respectively. Cyclosporine was employed as a drug. Phase diagrams showed the area of isotropic o/w region which forms o/w nanoemulsions was not significantly affected by the compositional ratio of cosurfactant. But, drug solubilization capacity, droplet size of nanoemulsions and drug release rate were greatly affected by the cosurfactant.

Keywords

References

  1. Alany, R.G., Rades, T., Agatonovic-Kustrin, S., Davies, N.M., Tucker, I.G., 2000. Effects of alcohols and diols on the phase behaviour of quaternary systems. Int. J. Pharm. 196, 141- 145. https://doi.org/10.1016/S0378-5173(99)00408-1
  2. Attwood, D., 1994. Microemulsions. In: Colloidal Drug Delivery Systems. Marcel Dekker, New York.
  3. Bumajdad, A., Eastoe, J., Zaki, M.I., Heenan, R.K., Pasupulety, L., 2007. Generation of metal oxide nanoparticles in optimised microemulsions. J. Colloid Interface Sci. 312, 68-75. https://doi.org/10.1016/j.jcis.2006.09.007
  4. Charman, S.A., Charman, W.N., Rogge, M.C., Wilson, T.D., Dutko, F.J., Pouton, C.W., 1992. Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm. Res. 9, 87-93. https://doi.org/10.1023/A:1018987928936
  5. Constantinides, P. P., 1995. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm. Res. 12, 1561-1572. https://doi.org/10.1023/A:1016268311867
  6. Eastoe, J., Hollamby, M.J., Hudson, L., 2006. Recent advances in nanoparticle synthesis with reversed micelles. Adv. Colloid Interface Sci. 128-130, 5-15. https://doi.org/10.1016/j.cis.2006.11.009
  7. Farago, B., Richter, D., Huang, J.S., Safran, S.A., Milner, S.T., 1990. Shape and size fluctuations of microemulsion droplets: The role of cosurfactant. Phys. Rev. Lett. 65, 3348-3351. https://doi.org/10.1103/PhysRevLett.65.3348
  8. Gershanik, T., Benita, S., 2000. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur. J. Pharm. Biopharm. 50, 179-188. https://doi.org/10.1016/S0939-6411(00)00089-8
  9. Hansen, S.H., 2003. Recent applications of microemulsion electrokinetic chromatography. Electrophoresis 24, 3900-3907. https://doi.org/10.1002/elps.200305637
  10. Hauer, B., Meinzer, A., Posanski, U., Richter, F., 1994. Pharmaceutical compositions comprising cyclosporins. United States Patent 5342625.
  11. Kawakami, K., Yoshikawa, T., Moroto, Y., Kanaoka, E., Takahashi, K., Nishihara, Y., Masuda, K., 2002. Microemulsion formulation for enhanced absorption of poorly soluble drugs. I. Prescription design. J. Control. Release 81, 65-74. https://doi.org/10.1016/S0168-3659(02)00049-4
  12. Kim, C.K., Cho, Y.J., Gao, Z.G., 2001. Preparation and evaluation of biphenyl dimethyl dicarboxylate microemulsions for oral delivery. J. Control. Release 70, 149-155. https://doi.org/10.1016/S0168-3659(00)00343-6
  13. Lawrence, M.J., Rees, G.D., 2000. Microemulsion-based media as novel drug delivery systems. Adv. Drug Deliv. Rev. 45, 89- 121. https://doi.org/10.1016/S0169-409X(00)00103-4
  14. Porter, C.J., Trevaskis, N.L., Charman, W.N., 2007. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat. Rev. Drug Discov. 6, 231-248. https://doi.org/10.1038/nrd2197
  15. Sarker, D.K., 2005. Engineering of nanoemulsions for drug delivery. Curr. Drug Deliv. 2, 297-310. https://doi.org/10.2174/156720105774370267
  16. Charinpanitkul, T., Chanagul, A., Dutta, J., Rungsardthong, U., Tanthapanichakoon, W., 2005. Effects of cosurfactant on ZnS nanoparticle synthesis in microemulsion. Sci. Tech. Adv. Mat. 6, 266-271. https://doi.org/10.1016/j.stam.2005.02.005
  17. Tarr, B.D., Yalkowsky, S.H., 1989. Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size. Pharm. Res. 6, 40-43. https://doi.org/10.1023/A:1015843517762

Cited by

  1. Efavirenz Self-Nano-Emulsifying Drug Delivery System: In Vitro and In Vivo Evaluation vol.17, pp.5, 2016, https://doi.org/10.1208/s12249-015-0446-2