• Heba A. Aboutaleb Department of Pharmaceutics, Faculty of Pharmacy, Nahda University, Bani-sueif, Egypt
  • Rasha M. Kharshoum Beni Sueif University
  • Hatem R. Ismail Al-Azhar University


Objective: The present study aims to utilize the nanotechnology technique to formulate the Cinnarizine (CNZ) in the form of solid self-nano emulsifying system to enhance the dissolution and hence the bioavailability.

Methods: Screening study for solubility of CNZ in different vehicles was carried out. The selected system was optimized for saturated solubility, globule size, zeta potential, polydispersity index (PDI) and self-emulsification time. The solidified nanoemulsion was prepared using; Aeroperl 300, Aerosil 200, hydrophilic nanosilica and Neusilin US2 as porous carrier materials. The compressed CNZ tablets were evaluated regarding their physicochemical characteristics, in-vitro release, and bioavailability study.

Results: Self nano-emulsifying system composed of Labrafil (oil), tween 80 (surfactant), and transcutol (cosurfactant) was successfully developed with a droplet size range of 11.37-92.58 nm. The in-vitro release results revealed that the developed formulation improved the release of CNZ and enhanced the bioavailability in the rabbits (190%) more than the commercial product (Stugeron® tablets).

Conclusion: Solid self-nano-emulsifying system of CNZ was successfully developed by different ratios of Labrafil (oil), tween 80 (surfactant), transcutol (cosurfactant) and solidified by the adsorption on hydrophilic nano silica and the optimized formula could be expected to increase and improve the bioavailability of CNZ.


Keywords: Pseudo-ternary phase diagram, Self-nanoemulsion, Porous carriers, Bioavailability study


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1. Sarpal K, Pawar YB, Bansal AK. Self-emulsifying drug delivery system: a strategy to improve oral bioavailability. Curr Res Pharm Sci 2010;11:342-9.
2. Tang J, Sun J, He ZG. Self-emulsifying drug delivery systems: a strategy for improving oral delivery of poorly soluble drugs. Curr Drug Ther 2007;2:85–93.
3. Sevda RR, Ravetkar AS, Shirote PJ. UV spectrophotometric estimation of Rosuvastatin calcium and fenofibrate in bulk drug and dosage form using simultaneous equation method. Int J Chem Tech Res 2011;3:629–35.
4. Liu Y, Feng N, Xu J. Preparation and evaluation of self micro-emulsifiying drug delivery system of oridonin. Int J Pharm 2008;355:269–76.
5. Goddeeris C, Cuppo F, Reynaers H, Bouwman WG, Van den Mooter G. Light scattering measurements on microemulsions: estimation of droplet sizes. Int J Pharm 2006;312:187–95.
6. Pouton CW. Formulation of self-emulsifying drug delivery systems. Adv Drug Delivery Rev 1997;25:47–58.
7. Porter CJH, Pouton CW, Cuine JF, Charman WN. Enhancing intestinal drug solubilization using lipid-based delivery systems. Adv Drug Delivery Rev 2008;60:673–91.
8. Charman SA, Charman WN, Rogge MC, Wilson TD, Dutko FJ, Pouton CW. Self-emulsifying drug delivery systems: formulation and bio-pharmaceutic evaluation of an investigational lipophilic compound. Pharm Res 1992;9:87–93.
9. Craig DQM, Lievens HSR, Pitt KG, Storey DE. An investigation into the physicochemical properties of self-emulsifying systems using low-frequency dielectric spectroscopy, surface tension measurements and particle size analysis. Int J Pharm 1993;96:147–55.
10. Abhijit AD, Neha D, Rahul D, Mangal N. Self nano emulsifying drug delivery systems: formulation insights, applications, and advances. Nanomedicine 2010;5:1595-616.
11. Sheikh S, Faiyaz S, Sushma T, Farhan J, Ahmad RK, Khar MA. Development and bioavailability assessment of ramipril nanoemulsion formulation. Eur J Pharm Biopharm 2007;66:227–43.
12. Yong MY, Fu DC, Min KC, Jung SK, Suk JC. Docetaxel microemulsion for enhanced oral bioavailability: preparation and in vitro and in vivo evaluation. J Controlled Release 2009;140:86–94.
13. 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.
14. Gu CH, Rao D, Gandhi RB, Hilden J, Raghavan K. Using a novel multicompartment dissolution system to predict the effect of gastric pH on the oral absorption of weak bases with poor intrinsic solubility. J Pharm Sci 2005;94:199–208.
15. Ogata H, Aoyagi N, Kaniwa N. Gastric acidity dependent bioavailability of cinnarizine from two commercial capsules in healthy volunteers. Int J Pharm 1986;29:113–20.
16. Kommuru TR, Gurley B, Khan MA. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q 10: formulation development and bioavailability assessment. Int J Pharm 2001;212:233–46.
17. Zhang P, Liu Y, Feng N. Preparation and evaluation of self-micro-emulsifying drug delivery system of oridonin. Int J Pharm 2008;355:269–76.
18. Jain AK, Thanki K, Jain S. Solidified self-nano emulsifying formulation for oral delivery of combinatorial therapeutic regimen: part I. Formulation development, statistical optimization, and in vitro characterization. Pharm Res 2014;31:923–45.
19. Yin YM, Cui FD, Mu CF, Choi MK, Kim JS, Chung SJ, et al. Docetaxel microemulsion for enhanced oral bioavailability: preparation and in vitro and in vivo evaluation. J Controlled Release 2009;140:86–94.
20. Hassan TH, Metz H, Mäder K. Novel semisolid SNEDDS based on PEG-30-dipolyhydroxystearate: development and characterization. Int J Pharm 2014;477:506-18.
21. Patil P, Patil V, Paradkar A. Formulation of a self-emulsifying system for oral delivery of simvastatin: in vitro and in vivo evaluation. Acta Pharm 2007;57:111–22
22. Obitte NC, Lisa CR, Chistianah MA. The utility of self-emulsifying oil formulation to improve the poor solubility of the anti HIV drug CSIC. AIDS Res Ther 2013;10:14, 1–9.
23. Ahuja G, Pathak K. Porous carriers for controlled/modulated drug delivery. Indian J Pharm Sci 2009;71:599–607.
24. Ramesh CN, Devendra NR, Pandit JK. In vitro release kinetics and bioavailability of gastro retentive cinnarizine hydrochloride tablet. AAPS PharmSciTech 2010;11:294-303.
25. Hasan SM, Elmosallamy AF, Abbas AB. LC and TLC determination of cinnarizine in pharmaceutical preparations and serum. J Pharm Biomed Anal 2002;28:711–9.
26. Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Delivery Rev 2000;45:89–121.
27. Constantinides PP, Scalart JP, Lancaster C, Marcello J, Marks G, Ellens H, et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium chain glycerides. Pharm Res 1994;11:1385–90.
28. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004;58:173–82.
29. Levy MY, Benita S. Drug release from submicronized o/w emulsion: a new in vitro kinetic evaluation model. Int J Pharm 1990;66:29–37.
30. Baboota S, Shakeel F, Ahuja A, Ali J, Shafiq S. Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib. Acta Pharm 2007;57:315–32.
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How to Cite
Aboutaleb, H. A., R. M. Kharshoum, and H. R. Ismail. “FORMULATION AND OPTIMIZATION OF SOLID SELF-NANOEMULSIFYING SYSTEM USING POROUS CARRIERS FOR ORAL DELIVERY OF CINNARIZINE”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 8, no. 1, Dec. 2015, pp. 433-8,
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