SOLUBILITY ENHANCEMENT OF CELECOXIB BY SOLID DISPERSION TECHNIQUE AND INCORPORATION INTO TOPICAL GEL
Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux.
Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release.
Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol.
Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.
2. Vyas J, Vyas P, Sawant K. Formulation and evaluation of topical niosomal gel of erythromycin. Int J Pharm Pharm Sci 2011;3:123-6.
3. Primo FT, Fröehlich PE. Celecoxib identification methods. Acta Farm Bonaerense 2005;24:421-5.
4. Chawla G, Gupta P, Thilagavathi R, Chakraborti AK, Bansal AK. Characterization of solid-state forms of celecoxib. Eur J Pharm Sci 2003;20:305-17.
5. Rao M, Mandage Y, Thanki K, Bhise S. Dissolution improvement of simvastatin by surface solid dispsersion technology. Dissol Technol 2010;2010;27-34.
6. Aejaz A, Azmail K, Sanaullah S, Mohsin A.A. Studies on aceclofenac solid dispersion incorporated gels: Development, characterization and in vitro evaluation. Int J Pharm pharm Sci 2010;2:111-5.
7. Lakshmi PK, Kumar MK, Sridharan A, Bhaskaran S. Formulation and evaluation of ibuprofen topical gel: A novel approach for penetration enhancement. Int J Appl Pharm 2011;3:25-30.
8. Patil SR, Kumar R, Patil MB, Paschapur MS, Rao VS. Enhancement of dissolution rate of aceclofenac by solid dispersion technique. Int J Pharma Tech Res 2009;1:1198-204.
9. Muralimohanbabu GV, Gourishankar V, Himashankar K, Seshasayana A, Kishorekumar N, Ramanamurthy KV. Development of dissolution medium for a poorly water soluble drugs celecoxib. Indian J Pharm Sci 2002;64:588-91.
10. Sankar V, Chandrasekaran K, Durga S, Prasanth KG, Nilani P, Geetha G, et al. Formulation and stability evaluation of diclofenac sodium ophthalmic gels. Indian J Pharm Sci 2005;67:473-6.
11. Panograha L, Ghosal SK, Pattanaik S, Mahasana L, Barik BB. Effect of permeation enhancer on the release and permeation kinetics of lincomycin hydrochloride gel formulation through mouse skin. Indian J Pharm Sci 2006;68:205-11.
12. Gupta GD, Goud RS. Release rate of tenoxicam from acrypol gels. Indian Pharmt 2005;2005:69-75.
13. Brian KR, Walters KA, Walkinson AC. Investigation of skin permeation in vitro. In: Roberts MS, Walters KA, editors. Drugs and Pharmaceutical Sciences. Vol. 91. New York: Dermal Absorption and Toxicity Assessment; 1993. p. 164-5.
14. Daravath B, Tadikonda RR. Formulation and evaluation of meclizine hydrochloride fast dissolving tablets using solid dispersion method. Asian J Pharm Clin Res 2014;7:98-102.
15. Dua K, Ramanna MV, Sara UV, Himaja M, Garg V. Dissolution enhancement of aceclofenac through solid dispersions. Indian Pharm 2006;34:70-2.
16. Anwar E, Harmita DR. Formulation and evaluation of gel and emulgel of chili extract (Capsicum frutescens L.) As topical dosage forms. Int J Pharm Pharm Sci 2014;6:13-6.
17. Jagdale S, Dangat Y, Kuchekar B. Improvement of dissolution rate of ramipril by solid dispersion technique and devlopement of buccal patch. Int J Pharm Pharm Sci 2012;4 Suppl 5:309-18.
18. Pandey A, Jagtap JV, Polshettiwar SA. Formulation and evaluation of in vitro antimicrobial activity of gel containing essential oils and effect of polymer on their antimicrobial activity. Int J Pharm Pharm Sci 2011;3:234-7.
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.