Abstract
Background: Diclofenac and curcumin is anticipated to have synergistic action. Hence, topical route of administration can be used in minimizing the issues with oral administration of both drugs.
Objective: This research aims at formulation of controlled release dosage form containing curcumin microspheres and diclofenac diethylamine and then incorporating it into gel formulation for treatment of inflammation associated with rheumatoid arthritis.
Methods: Curcumin microspheres were prepared, optimized and assayed. Gel containing microspheres was formulated and evaluated for physicochemical parameters like spreadability and viscosity. In vitro and ex vivo diffusion studies were carried out followed by evaluation of efficacy. Efficacy of the developed formulation was evaluated for anti-inflammatory activity.
Results: Particle size, Zeta potential, pH, spreadability and viscosity of optimized Batch F1 was found to be in range 0.5 µm - 5 µm,-27.9 mV, 6.2, 105 g cm/s and 7500 cps respectively. In vitro diffusion of developed gel of diclofenac diethylamine and curcumin was found to be 92.16 ± 0.0040 % in 3 h and 92.54 ± 0.0036 % in 12 h as compared to 79.57 ± 0.004 % diffusion in 2 h for marketed gel, thus showing controlled delivery of curcumin.
Conclusion: Decreased inflammation in formulation treated group by 72.53% and 50.75% in marketed treated group was seen. Thus the formulation developed showed prolonged activity as well as better anti-inflammatory activity.
Keywords: Curcumin microspheres, diclofenac diethylamine, o/w emulsion, inflammation, rheumatoid arthritis, formulation.
Graphical Abstract
[http://dx.doi.org/10.1128/MMBR.27.2.117-154.1963] [PMID: 13989977]
[http://dx.doi.org/10.1016/j.ejmech.2009.12.041] [PMID: 20079558]
[http://dx.doi.org/10.1016/j.ejmech.2007.02.008] [PMID: 17467123]
[http://dx.doi.org/10.2174/138161209788186308] [PMID: 19442187]
[http://dx.doi.org/10.1002/anr.1780321217] [PMID: 2597213]
[http://dx.doi.org/10.1016/S0092-8674(00)81109-5] [PMID: 8616886]
[http://dx.doi.org/10.1002/art.10705] [PMID: 12528103]
[http://dx.doi.org/10.2165/00003495-200060030-00004] [PMID: 11030467]
[http://dx.doi.org/10.2174/1874609810902010003] [PMID: 20021395]
[PMID: 20729960]
[http://dx.doi.org/10.1016/j.phymed.2014.06.015] [PMID: 25442263]
[http://dx.doi.org/10.1093/bja/aet176] [PMID: 23719767]
[http://dx.doi.org/10.1016/j.neulet.2011.07.054] [PMID: 21855605]
[http://dx.doi.org/10.3344/kjp.2012.25.4.221] [PMID: 23091682]
[http://dx.doi.org/10.1016/j.neuropharm.2011.08.050] [PMID: 21945716]
[http://dx.doi.org/10.1016/S0091-3057(03)00214-4] [PMID: 13679232]
[http://dx.doi.org/10.2147/JPR.S36916] [PMID: 23429763]
[http://dx.doi.org/10.22270/jddt.v2i3.127]
[http://dx.doi.org/10.3390/pharmaceutics2020209] [PMID: 27721352]
[http://dx.doi.org/10.1080/10717540490280750] [PMID: 15200010]
[http://dx.doi.org/10.1002/jps.3030450406] [PMID: 13319092]
[PMID: 15758488]
[http://dx.doi.org/10.1038/sj.bjp.0705650] [PMID: 15155540]