Prolonged Anti-Inflammatory Activity of Topical Melatonin by Niosomal Encapsulation

Abstract:

Melatonin, encapsulated and non-encapsulated, in a topical gel, was comparatively investigated for its in vitro permeation and in vivo anti-inflammatory properties. An average size of the melatonin-encapsulated niosomes of 197 nm with a zeta potential of-78.8 mV and an entrapment efficiency of 92.7% was incorporated into a gel base. In vitro skin permeation of the same gel base incorporated with non-encapsulated melatonin or melatonin niosomes at 5% was comparatively evaluated through porcine skin using Franz diffusion cells and analyzed by spectroflurometry at λ_ex 278 and λ_em 348 nm. From the same gel base, the permeation rate of non-encapsulated melatonin was about 2.5 times greater than that of melatonin-encapsulated niosomes. In comparison to piroxicam gel and hydrocortisone cream used as the positive controls, topical applications of melatonin and melatonin niosome gels tested in croton oil-induced ear edema in mice suggested that its anti-inflammatory activities were prolonged by the niosomal encapsulation. Similarly, analgesic effect of melatonin was prolonged by niosomal encapsulation using tail flick test in mice. Therefore, its immediate permeation through the skin was retarded by niosomal encapsulation which could also prolong its rapid decline in exerting anti-inflammatory and analgesic activities in vivo.

• Periodical: Advanced Materials Research (Volume 902)
• Pages: 70-75
• DOI: https://doi.org/10.4028/www.scientific.net/AMR.902.70
• Online since: February 2014
• Authors: Aroonsri Priprem*, Vassana Netweera, Pramote Mahakunakorn, Nutjaree Pratheepawanit Johns, Jeffrey Roy Johns
• Keywords: Anti-Inflammatory, Encapsulation, Melatonin, Niosomes

References

[1] I.F. Uchegbu, A.T. Florence, Non-ionic surfactant vesicles (Niosomes): physical and pharmaceutical chemistry, Adv. Colloid. Interfac. Vol. 58 (1995), pp.1-55. 59.

DOI: 10.1016/0001-8686(95)00242-i

[2] J.D. Yadav, P.R. Kulkarni, K.A. Vaidya and G.T. Shelke, Niosome: A Review, J. Pharm. Res. Vol. 4(3) (2011), pp.632-636. 59.

[3] N.B. Mahale, P.D. Thakkar, R.G. Mali, D.R. Walunj and S.R. Chaudhari, Niosomes: Novel sustained release nonionic stable vesicular systems - An overview, Adv. Colloid. Interfac. Vol. 183-184 (2012), pp.46-54. 59.

DOI: 10.1016/j.cis.2012.08.002

[4] A. Manosroi, P. Khanrin, W. Lohcharoenkal, R. G. Werner, F. Gotz, W. Manosroi and J. Manosroi,  Transdermal absorption enhancement through rat skin of gallidermin loaded in niosomes, Int. J. Pharm. Vol. 392 (2010), pp.304-310. 59.

DOI: 10.1016/j.ijpharm.2010.03.064

[5] R. Muzzalupo, L. Tavano, R. Cassano, S. Trombino, T. Ferrarelli and N. Picci, A new approach for the evaluation of niosomes as effective transdermal drug delivery systems, Eur. J. Pharm. Biopharm. Vol 79 (2011), pp.28-35. 59.

DOI: 10.1016/j.ejpb.2011.01.020

[6] R.J. Reiter, J.R. Calvo, M. Karbownik, W. Qi and D.X. Tan, Melatonin and its relation to the immune system and inflammation, Ann. N. Y. Acad Sci. Vol. 917 (2000), pp.376-386. 59.

DOI: 10.1111/j.1749-6632.2000.tb05402.x

[7] A. Slominski, D.J. Tobin, M.A. Zmijewski, J. Wortsman and R. Paus, Melatonin in the skin: synthesis, metabolism and functions, Trends Endocrin. Met. Vol. 19(1) (2008), pp.17-24. 59.

DOI: 10.1016/j.tem.2007.10.007

[8] B. Claustrat, J. Brun and G. Chazot, The basic physiology and pathophysiology of melatonin, Sleep Med. Rev. Vol. 9(1) (2005), pp.11-24. 59.

DOI: 10.1016/j.smrv.2004.08.001

[9] T.B. Grivas and O.D. Savvidou, Melatonin the light of night in human biology and adolescent idiopathic scoliosis, Scoliosis. Vol. 2 (2007), pp.1-14. 59.

DOI: 10.1186/1748-7161-2-6

[10] S. Andega, N. Kanikkannan and M. Singh, Comparison of the effect of fatty alcohols on the permeation of melatonin between porcine and human skin, J. Control. Release. Vol. 77(1-2) (2001), pp.17-25. 59.

DOI: 10.1016/s0168-3659(01)00439-4

[11] F. Radogna, M. Diederich and I. Ghibelli, Melatonin: a pleiotropic molecule regulating inflammation, Biochem. Pharmacol. Vol. 80 (2010), pp.1844-52. 59.

DOI: 10.1016/j.bcp.2010.07.041

[12] F.T. Guilford, U.S. Patent 0020436 (2011).

[13] N. Kanikkannan, T. Jackson, M.S. Shaik and M. Singh, Evaluation of skin sensitization potential of melatonin and nimesulide by murine local lym, Eur. J. Pharm. Sci. Vol. 14(3) (2001), pp.217-20. 59.

DOI: 10.1016/s0928-0987(01)00176-2

[14] L. Kikwai, N. Kanikkannan, R.J. Babu and M. Singh, Effect of vehicles on the transdermal delivery of melatonin across porcine skin in vitro. J. Control. Release. Vol. 83(2) (2002), pp.307-311. 59.

DOI: 10.1016/s0168-3659(02)00202-x

[15] W.A.M. Mulla, S.D. More, S.B. Jamge, A.M. Pawar, M.S. Kazi and M.R. Varde, Evaluation of antiinflammatory and analgesic activities of ethanolic extract of roots Adhatoda vasica Linn, Int. J. Pharm. Tech. Res. Vol. 2(2) (2010), pp.1364-68. 59.

[16] M. Manconia, J. Pendas, N. Ledon, T. Moreira, C. Sinico, L. Saso and A.M. Fadda, Phycocyanin liposomes for topical anti-inflammatory activity: in-vitro in-vivo studies, J. Pharm. Pharmacol. Vol. 61 (2009), pp.423-430. 59.

DOI: 10.1211/jpp.61.04.0002

[17] A. Tubaro, P. Dri, M. Melato, G. Mulas, P. Bianchi, P. Del Negro and R. D. Loggia, In the croton oil ear test the effects of non steroidal antiinflammatory drug (NSAIDs) are dependent on the dose of the irritant, Agent. Act.  Vol. 19 (1986).

DOI: 10.1007/bf01971259