Enhancement of transdermal delivery of ibuprofen using microemulsion vehicle

Hu, Liandong; Hu, Qiaofeng; Yang, Jianxue

doi:10.22038/ijbms.2014.3450

Enhancement of transdermal delivery of ibuprofen using microemulsion vehicle

Document Type : Original Article

Authors

¹ 1 College of Pharmaceutical Sciences, Hebei University, Baoding, China 2 Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding, China

² College of Pharmaceutical Sciences, Hebei University, Baoding, China. NBP Pharmaceutical Company Limited, CSPC Pharmaceutical Group Limited, Shijiazhuang 052165, People’s Republic of China

³ 1 College of Pharmaceutical Sciences, Hebei University, Baoding, China.3 NBP Pharmaceutical Company Limited, CSPC Pharmaceutical Group Limited, Shijiazhuang 052165, People’s Republic of China

10.22038/ijbms.2014.3450

Abstract

Objective(s):The objective of this study was to find a stable microemulsion vehicle for transdermal delivery of ibuprofen to improve the skin permeability.
Materials and Methods: Microemulsion was prepared using different sorts of oils, surfactants and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The effects of oleic acid and surfactant mixture on skin permeation of ibuprofen were evaluated with excised skins.
Results: The optimum formulation F3 consisting of 6% oleic acid, 30% Cremophor RH40/Transcutol P (2:1, w/w) and 59% water phase, showed a high permeation rate of 42.98 μg/cm²/hr. The mean droplet size of microemulsion was about 43 nm and no skin irritation signs were observed on the skin of rabbits.
Conclusion: These results indicated that this novel microemulsion is a useful formulation for the transdermal delivery of ibuprofen.

Keywords

References

1. Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev 2000; 45:89-121.

2. Rhee YS, Choi JG, Park ES, Chi SC. Transdermal delivery of ketoprofen using microemulsions. Int J Pharm 2001; 228:161-170.

3. Chen H, Chang X, Weng T, Zhao X, Gao Z, Yang Y, et al. A study of microemulsion systems for transdermal delivery of triptolide. J Control Release 2004; 98:427-436.

4. Peira E, Scolari P, Gasco MR. Transdermal per-meation of apomorphine through hairless mouse skin from microemulsions. Int J Pharm 2001; 226:47-51.

5. Kreilgaard M, Pedersen EJ, Jaroszewski JW. NMR characterisation and transdermal drug delivery potential of microemulsion systems. J Control Release 2000; 69:421-433.

6. Peltola S, Saarinen-Savolainen P, Kiesvaara J, Suhonen TM, Urtti A. Microemulsions for topical delivery of estradiol. Int J Pharm 2003; 254: 99-107.

7. Salimi A, Sharif Makhmal Zadeh B, Moghimipour E. Preparation and characterization of cyanocobalamin (vit B12) microemulsion properties and structure for topical and transdermal application. Iran J Basic Med Sci 2013; 16:865-872.

8. Yong CS, Oh YK, Jung SH, Rhee JD, Kim HD, Kim CK, et al. Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol. Eur J Pharm Sci 2004; 23:347-353.

9. Newa M, Bhandari KH, Li DX, Kwon TH, Kim JA, Yoo BK, et al. Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188. Int J Pharm 2007; 343:228-237.

10. Glowka FK. Stereoselective pharmacokinetics of ibuprofen and its lysinate from suppositories in rabbits. Int J Pharm 2000; 199:159-166.

11. Ghorab MK, Adeyeye MC. Enhancement of ibuprofen dissolution via wet granulation with beta-cyclodextrin. Pharm Dev Technol 2001; 6:305-314.

12. Maghsoodi M, Kiafar F. Co-precipitation with PVP and Agar to Improve Physicomechanical Properties of Ibuprofen. Iran J Basic Med Sci 2013; 16:635-642.

13. Ji HY, Lee HW, Kim YH, Jeong DW, Lee HS. Simultaneous determination of piroxicam, Meloxicam and tenoxicam in human plasma by liquid chromatography with tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2005; 826: 214-219.

14. Gupta SK, Bansal P, Bhardwaj RK, Jaiswal J, Velpandian T. Comparison of analgesic and anti-inflammatory activity of meloxicam gel with diclofenac and piroxicam gels in animal models: pharmacokinetic parameters after topical application. Skin Pharmacol Appl Skin Physiol 2002; 15:105-111.

15. Zhu W, Yu A, Wang W, Dong R, Wu J, Zhai GX. Formulation design of microemulsion for dermal delivery of penciclovir. Int J Pharm 2008; 360:184-190.

16. Draize J, Woodard G, Calvery H. Methods for the study of irritation and toxicity of substances applied topically to the skin and mucous membranes. J Pharmacol Exp Ther 1944; 82:377–390.

17. Joshi M, Pathak S, Sharma S, Patravale V. Design and in vivo pharmacodynamic evaluation of nanostructured lipid carriers for parenteral delivery of artemether: Nanoject. Int J Pharm 2008; 364:119–126.

18. Sintov AC, Shapiro L. New microemulsion vehicle facilitates percutaneous penetration in vitro and cutaneous drug bioavailability in vivo. J Control Release 2004; 95:173-183.

19. Kanikkannan N, Kandimalla K, Lamba SS, Singh M. Structure-activity relationship of chemical penetration enhancers in transdermal drug delivery. Curr Med Chem 2000; 7:593-608.

20. Chen H, Chang X, Du D, Li J, Xu H, Yang X. Microemulsion-based hydrogel formulation of ibuprofen for topical delivery. Int J Pharm 2006; 315:52-58.

21. Hadgraft J, Whitefield M, Rosher PH. Skin penetration of topical formulations of ibuprofen 5%: an in vitro comparative study. Skin Pharmacol Appl Skin Physiol 2003; 16:137-142.

22. Park ES, Chang SY, Hahn M, Chi SC. Enhancing effect of polyoxyethylene alkyl ethers on the skin permeation of ibuprofen. Int J Pharm 2000; 209:109-119.

23. Al-Saidan SM. Transdermal self-permeation enhancement of ibuprofen. J Control Release 2004; 100:199-209.