Production and Drug Release Assesment of Melatonin-Loaded Alginate/Gum Arabic Beads

Year 2016, Volume: 3 Issue: 3, 205 - 216, 08.01.2017

Rukiye Yavaşer Bernis Girgin Onur Korkmaz Arife Alev Karagözler

https://doi.org/10.18596/jotcsa.30880

Cited By: 4

Abstract

Melatonin containing alginate-gum arabic beads were produced by ionotropic gelation. The most suitable alginate-gum arabic ratio for bead production was optimized. To the optimized beads the loading of changing amounts of melatonin was conducted to produce the beads with the best melatonin entrapment and release. Entrapment efficiency of the beads as melatonin carrier was calculated to be approximately 70%. Release profiles of melatonin from the beads were generated using in vitro gastric fluid (pH 1.5) and intestinal fluid (pH 7.4). According to results obtained, following a burst in the first half hour, melatonin release from the beads in pH 1.5 medium was approximately 45% in the first 5 hours whereas the release was approximately 50% in pH 7.4 medium. The results indicate that the beads manufactured may be used as carriers for controlled release of melatonin.

Keywords

Melatonin, alginate, gum arabic; bead; controlled drug release

References

• Bruschi, ML.. Strategies to modify the drug release from pharmaceutical systems. Woodhead Publishing. 2015. ISBN: 978-0-08-100112-7.
• Siegel RA., Rathbone MJ. Overview of controlled release mechanisms. Fundamentals and Applications of Controlled Release Drug Delivery. Springer US, 2012; 19-43. DOI:10.1007/978-1-4614-0881-9_2.
• Şanlı O, Ay N, Işıklan N. Release characteristics of diclofenac sodium from poly (vinyl alcohol)/sodium alginate and poly (vinyl alcohol)-grafted-poly (acrylamide)/sodium alginate blend beads. European Journal of Pharmaceutics and Biopharmaceutics. 2007; 65(2), 204-214. DOI:10.1016/j.ejpb.2006.08.004.
• Lee B‐J, Min G‐H, Cui J‐H. Correlation of drug solubility with trapping efficiency and release characteristics of alginate beads. Pharmacy and Pharmacology Communications. 1999; 5(2): 85-89. DOI: 10.1211/146080899128734505.
• Nizam El-Din HM, Khafaga MR, El-Naggar, AWM. Physico-Chemical and Drug Release Properties of Poly (Vinyl Alcohol)/Gum Arabic/TiO2 Nanocomposite Hydrogels Formed by Gamma Radiation. Journal of Macromolecular Science, Part A. 2015; 52(10): 821-829. DOI: 10.1080/10601325.2015.1067040.
• Altındal DÇ, Gümüşderelioğlu M. Melatonin releasing PLGA micro/nanoparticles and their effect on osteosarcoma cells. Journal of Microencapsulation. 2016; 33(1): 53-63. http://dx.doi.org/10.3109/02652048.2015.1115901.
• Garfinkel D, Laudon M, Nof D, Zisapel N. Improvement of sleep quality in elderly people by controlled-release melatonin. The Lancet. 1995; 346(8974): 541-544. DOI:10.1016/S0140-6736(95)91382-3.
• Mihailiasa M, Caldera F, Li J, Peila R, Ferri A, Trotta F. Preparation of functionalized cotton fabrics by means of melatonin loaded β-cyclodextrin nanosponges. Carbohydrate polymers, 2016;142: 24-30. DOI:10.1016/j.carbpol.2016.01.024.
• Malakar M,Nayak AK, Pal D, Jana P. Potato starch blended alginate beads for prolonged release of tolbutamide: Development by statistical optimization and in vitro characterization. Asian Journal of Pharmaceutics. 2013; 7: 43-51. DOI: 10.4103/0973-8398.110935.
• Nayak AK, Das B, Maji R. Calcium alginate/gum arabic beads containing glibenclamide: Development and in vitro characterization. International Journal of Biological Macromolecules. 2012; 51(5): 1070-1078. DOI:10.1016/j.ijbiomac.2012.08.021.
• Dubey V, Mishra D, Asthana A, Jain, NK. Transdermal delivery of a pineal hormone: melatonin via elastic liposomes. Biomaterials. 2006; 27(18): 3491-3496. DOI:10.1016/j.biomaterials.2006.01.060.
• Schaffazick SR, Pohlmann AR, Mezzaliraa G, Guterres SS. Development of nanocapsule suspensions and nanocapsule spray-dried powders containing melatonin. Journal of The Brazilian Chemical Society, 2006. 17(3):562–569. http://dx.doi.org/10.1590/S0103-50532006000300020.
• Lee, B. J., Min, G. H., & Kim, T. W. Preparation and in vitro release of melatonin-loaded multivalent cationic alginate beads. Archives of Pharmacal Research. 1996; 19(4): 280-285. DOI:10.1007/BF02976241.
• Lee BJ, Choe JS, Kim CK. Preparation and characterization of melatonin-loaded stearyl alcohol microspheres. Journal of Microencapsulation. 1998; 15(6): 775-787. DOI:10.3109/02652049809008260.
• Østberg T, Lund EM, Graffner C. Calcium alginate matrices for oral multiple unit administration: IV. Release characteristics in different media. International Journal of Pharmaceutics. 1994; 112(3): 241-248. DOI:10.1016/0378-5173(94)90360-3.
• Fathy M, Safwat SM, El-Shanawany SM, Tous SS, Otagiri M. Preparation and evaluation of beads made of different calcium alginate compositions for oral sustained release of tiaramide. Pharmaceutical Development and Technology. 1998; 3(3): 355-364. DOI:10.3109/10837459809009863.