• Yogesh Pore Department of Pharmaceutical Chemistry, Government College of Pharmacy, Ratnagiri, Maharashtra, 415 612, India
  • Madhuri Mane Department of Biopharmaceutics, Government College of Pharmacy, Karad, Maharashtra, 415 124, India.
  • Vaishnavi Mangrule Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, 415 124, India
  • Atul Chopade Department of Pharmacology, Rajarambapu College of Pharmacy, Kasegaon, Maharashtra, 415 404, India
  • Pankaj Gajare Department of Pharmaceutics, Rajaram and Tarabai Bandekar College of Pharmacy, Farmagudi, Ponda, Goa, 403 401, India


Objective: The objective of this study was to prepare and characterize etoricoxib (ECB) loaded Soluplus® nanocomposites to improve its physicochemical properties. The effect of polymer and surfactant concentration on particle size, in vitro percentage dissolution efficiency and the anti-inflammatory activity of nanocomposites were also investigated.

Methods: The nanocomposites were prepared by using a freeze-drying technique. The analytical evidence for the formulation of lyophilized nanocomposites in solid state were generated and confirmed by differential scanning calorimetry (DSC), fourier transformation infrared spectroscopy (FTIR), x-ray powder diffractometry (XPRD) and scanning electron microscopy (SEM). The in vitro drug release profile of nanocomposites was compared with pure ECB powder.

Results: The nanocomposites of ECB were contained in a nano range with particle size and zeta potential of 63.5 nm and 46.5 mv, respectively. The solubility and dissolution of the nanocomposites were significantly (p<0.001) improved as compared to ECB alone, evidenced by decreased log P values (1.90±0.002) of the nanocomposites. The characterization studies revealed the formation of amorphous nanocomposites of ECB with existence of physical interactions between drug and polymer. The anti-inflammatory activity of nanocomposites evaluated by carrageenan-induced rat paw edema model demonstrated nonsignificant (p>0.05) increase in anti-inflammatory activity as compared to pure ECB.

Conclusion: From the results, it could be concluded that the formation of ECB nanocomposites with Soluplus® could be an effective and alternative approach to modify the physicochemical properties of ECB.

Keywords: Etoricoxib, Soluplus®, Nanocomposites, Physicochemical properties, Anti-inflammatory activity


1. Chowdary KPR, Rao KSP, Madhuri D. Formulation and evaluation of etoricoxib tablets employing cyclodextrin-poloxamer 407-PVP K 30 inclusion complexes. Int J Appl Biol Pharm 2011;2:43-8.
2. Raja RK, Abbulu K, Sudhakar M, Vishwanadham M, Syama MT. Studies on dissolution enhancement of Lovaststin using soluplus by solid dispersion technique. Int J Pharm Pharm Sci 2012;4:124-8.
3. Kasar PM, Kale KS, Phadtare DP. Nanoplex: a review of nanotechnology approach for solubility and dissolution rate enhancement. Int J Curr Pharm Res 2018;10:6-10.
4. Amidon GL, Lennernas H, Shaha VP, Crison JR. A theoretical basis for biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12:413-20.
5. Patel RN, Bahareh M, Patel S. Modification of physical and chemical properties of BCS II drug. Int J Pharm Pharm Sci 2012;4:290-302.
6. Muralidhar SM, Rao GD, Murthy MK, Kumar KK, Teja KK, Nawaj S, et al. Enhancement of dissolution rate of etoricoxib through solid dispersion technique. J Appl Pharm Sci 2011;1:129-32.
7. Cochrane DJ, Jarvis B, Keating GM. Etoricoxib. Drugs 2002;62:2637-51.
8. Schott H, Kwan LC, Feldman S. The role of surfactant in the release of very slightly soluble drugs from tablets. J Pharm Sci 1982;71:1038-42.
9. Veiga F, Teixeria Dias JJC, Kedzeierewicz F, Sousa A, Maincent P. Inclusion complexation of tolbutamide with β-cyclodextrin and hydroxypropyl-β-cyclodextrin. Int J Pharm 1996;129:63-71.
10. Longxiao L, Suyan Z. Preparation and characterization of inclusion complexes of prazosin hydrochloride with β-cyclodextrin and hydroxypropyl-β-cyclodextrin. J Pharm Biomed Anal 2006;28:122-7.
11. Henck JO, Griesser UJ, Burger A. Polymorphie von arzneistoffen eine wirtschaftliche herausforderung. Pharm India 1997;59:165-9.
12. Hancock BC, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci 1997;86:1-12.
13. Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971;60:1281-302.
14. Serajuddin ATM. Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs. J Pharm Sci 1999;88:1058-66.
15. Patnaik S, Aditha SK, Rattan T, Kamisetti V. Aceclofenac-soluplus®Nanocomposites for increased bioavailability. SNL 2015;5:13-20.
16. BASF. Technical Information soluplus, BASF. Pharm Ingredients and Services; 2010. p. 1-8.
17. Agrawal NGB, Porras AG. Dose proportionality of oral etoricoxib, a highly selective cyclooxygenase-2 inhibitor, in healthy volunteers. J Clin Pharmacol 2001;41:1106-10.
18. Rodrigues AD, Halpin RA, Geer LA. Absorption, metabolism, and excretion of etoricoxib, a potent and selective cyclooxygenase-2 inhibitor, in healthy male volunteers. Drug Metab Dispos 2003;31:224-32.
19. Suhagia BN, Patel HM, Shah SA, Rathod I, Parmar VK. Preparation and characterization of etoricoxib-polyethylene glycol 4000 plus polyvinylpyrrolidone k30 solid dispersions. Acta Pharm 2006;56:285-98.
20. Chauhan B, Shimpi S, Paradkar A. Preparation and characterization of etoricoxib solid dispersions using lipid carriers by spray drying technique. AAPS Pharm Sci Tech 2005;6:E405-12.
21. Karekar P, Vyas V, Shah M, Sancheti P, Pore YV. Physicochemical investigation of the solid dispersion systems of etoricoxib with poloxamer 188. Pharm Dev Tech 2009;14:373-9.
22. Shimpi SL, Chauhan B, Mahadik KR, Paradkar A. Stabilization and improved in vivo performance of amorphous etoricoxib using gelucire 50/13. Pharm Res 2005;22:1727-34.
23. Shimpi SL, Mahadik KR, Paradkar AR. Study on the mechanism for amorphous drug stabilization using gelucire 50/13. Chem Pharm Bull 2009;57:937-42.
24. Shimpi S, Mahadik K, Takada K, Paradkar K. Application of polyglycolized glycerides in the protection of an amorphous form of etoricoxib during compression. Chem Pharm Bull 2007;55:1448-51.
25. Shah M, Karekar P, Sancheti P, Vyas V, Pore Y. Effect of PVP K30 and/or L-arginine on stability constant of etoricoxib-HP--CD inclusion complex: preparation and characterization of etoricoxib-HP--CD binary system. Drug Dev Ind Pharm 2009;35:118-29.
26. Patel HM, Suhagia BN, Shah SA, Rathod I, Parmar VK. Preparation and characterization of etoricoxib-β-cyclodextrin complexes prepared by the kneading method. Acta Pharm 2007;57:351-9.
27. Dash R, Acharya AK, Swain S, Barg M, Choudhary HK, Meher K. Formulation and evaluation of spherical crystal of etoricoxib. Int J Pharm Biol Arch 2011;2:1123-9.
28. Higuchi T, Connors K. Phase-solubility techniques. Adv Anal Chem Instr 1965;4:117-2.
29. Desai PS, Pore YV. Physicochemical characterization of spray dried cefixime polymeric nanoparticles using a factorial design approach. J Appl Pharm Sci 2016;6:124-32.
30. Khade S, Pore YV. Formulation and evaluation of neusiln® US2 adsorbed amorphous solid self-micro emulsifying delivery system of atorvastatin calcium. Asian J Pharm Clin Res 2016;9:1-8.
31. Jadhav P, Pore YV. Physicochemical, thermodynamic and analytical studies on binary and ternary inclusion complexes of bosentan with hydroxypropyl-β-cyclodextrin. Bull Fac Pharm (Cairo Univ) 2016;55:147-54.
32. Naidu G, Madhavi E, Konda VGR, Ramana V. Comparative study of the anti-inflammatory activity of newer macrolides with etoricoxib. J Evol Med Dent Sci 2014;3:2413-9.
33. Ferrero Milianni L, Nielsen OH, Andersen PS. Chronic inflammation: the importance of NOD2 and NALP3 in interleukin–l beta generation. Clin Exp Immunol 2007;147:227-35.
34. Mishara D, Ghosh G, Kumar P, Panda P. Anti-inflammatory and antipyretic activity of selective COX-2 inhibitor with conventional NSAIDS. Int J Pharm Sci Res 2010;1:103-9.
35. Jafar M, Mhg D, Shareef A. Enhancement of dissolution and anti-inflammatory effect of meloxicam using solid dispersion. Int J Appl Pharm 2010;2:22-7.
36. Niazi J, Gupta V, Chakarborty P, Kumar P. Anti-inflammatory and antipyretic activity of aleuritis moluccana leaves. Asian J Pharm Clin Res 2010;3:35-6.
37. Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol 1975;27:48-9.
38. Mooter G, Augustijins, Blaton N, Kinget R. Physico-chemical characterization of solid dispersions of temazepam with polyethylene glycol 6000 and PVP K30. Int J Pharm 1998;164:67-80.
39. Ruan LP, Yu BY, Fu GM, Zhu D. Improving the solubility of ampelopsin by solid dispersions and inclusion complexes. J Pharm Biomed Anal 2005;38:457-64.
40. Bhosale P, Pore YV, Sayyad F. Preparation of amorphous carvedilol polymeric microparticles for improvement of physicochemical properties. J Pharm Investig 2012;42:335-44.
71 Views | 117 Downloads
How to Cite
Pore, Y., Mane, M., Mangrule, V., Chopade, A., & Gajare, P. (2018). PREPARATION, CHARACTERIZATION, AND EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF ETORICOXIB LOADED SOLUPLUS® NANOCOMPOSITES. International Journal of Applied Pharmaceutics, 10(6), 268-274.
Original Article(s)