Effect of Alginate and Surfactant on Physical Properties of Oil Entrapped Alginate Bead Formulation of Curcumin
Oil entrapped floating alginate beads of curcumin were developed and characterized. Cremophor EL, Cremophor RH and Tween 80 were utilized to improve the solubility of the drug. The oil-loaded floating gel beads prepared by emulsion gelation method contained sodium alginate, mineral oil and surfactant. The drug content and % encapsulation declined as the ratio of surfactant was increased. The release of curcumin from 1% alginate beads was significantly more than for the 2% alginate beads. The drug released from the beads containing 25% of Tween 80 was about 70% while a higher drug release was observed with the beads containing Cremophor EL or Cremohor RH (approximately 90%). The developed floating beads of curcumin powder with surfactant provided a superior drug release than those without surfactant. Floating beads based on oil entrapment containing the drug solubilized in surfactants is a new delivery system to enhance the dissolution of poorly soluble drugs.
[1] B. Gander, K. Ventouras, R. Gurny and E. Doelker. "In vitro dissolution medium with supramicellar surfactant concentration and its relevance for in vivo absorption,” Int. J. Pharm., Vol. 27, no. 1, pp. 117–124, Nov. 1985.
[2] P. Somparn, C. Phisalaphong, S. Nakornchai, S. Unchern and N. P. Morales. "Comparative antioxidant activities of curcumin and its demethoxy and hydrogenated derivatives,” Biol. Pharm. Bull., Vol. 30, no. 1, pp. 74-78, Jan. 2007.
[3] X. Wang, Y. Jiang, Y. Wang, M. Huang, C. Ho and Q. Huang. "Enhancing anti-inflammation activity of curcumin through O/W nanoemulsions,” Food. Chem., Vol. 108, no. 2, pp. 419-424, May. 2008.
[4] N. Chainani-Wu. "Safety and anti-inflammatory activity of curcumin: a component of tumeric (Curcuma longa),” J. Altern. Complement. Med., Vol. 9, no. 1, pp. 161-168, Feb 2003.
[5] K. J. Kim, H. H. Yu, J. D. Cha, S. J. Seo, N. Y. Choi and Y. O. You. "Antibacterial activity of Curcuma longa L. against methicillin-resistant Staphylococcus aureus," Phytother. Res., Vol. 19, no. 7, pp. 599-604, Jul. 2005.
[6] S. Mahattanadul, T. Nakamura, P. Panichayupakaranant, N. Phdoongsombut, K. Tungsinmunkong and P. Bouking. "Comparative antiulcer effect of bisdemethoxycurcumin and curcumin in a gastric ulcer model system,” Phytomedicine, Vol. 16, no. 4, pp. 342-351, Apr. 2009.
[7] U. M. Viradia, A. M. Shenoy, M. S. Rajan, A. R. Shabaraya, A. D. Kothadia and N. H. Patel. "Effect of leukotriene receptor antagonist montelukast along with curcumin against gastric ulceration,” Int. J. Pharm. Sci. Rev. Res., Vol. 3, no. 3, pp. 184-187, 2011.
[8] A. Goel, A. B. Kunnumakkara, B. B. Aggarwal. "Curcumin as "Curecumin": from kitchen to clinic,” Biochem. Pharmacol., Vol. 75, no. 4, pp. 787-809, Feb. 2008.
[9] P. Yoysungnoen, P. Wirachwong, C. Changtam, A. Suksamrarn and S. Patumraj. "Anti-cancer and anti-angiogenic effects of curcumin and tetrahydrocurcumin on implanted hepatocellular carcinoma in nude mice,” World. J. Gastroenterol., Vol.14, no. 13, pp. 2003-2009, Arp.2008.
[10] P. Anand, A. B. Kunnumakkara, R. A. Newman, B. B. Aggarwal. "Bioavailability of curcumin: problems and promises,” Mol. Pharm., Vol. 4, no. 6, pp. 807-818, Nov.-Dec. 2007.
[11] P. Ratanajiajaroen, M. Ohshima. "Synthesis, release ability and bioactivity evaluation of chitin beads incorporated with curcumin for drug delivery applications,” J. Microencapsul., Vol. 29, No. 6, pp. 549-558, 2012.
[12] S. Song, Z. Wang, Y. Qian, L. Zhang and E. Luo, "The release rate of curcumin from calcium alginate beads regulated by food emulsifiers," J. Agric. Food. Chem., Vol. 60, no. 17, pp. 4388-4395, May. 2012.
[13] S. Arora, J. Ali, A. Ahuja, R. K. Khar, and S. Baboota. "Floating drug delivery systems: a review,” AAPS Pharm. Sci. Tech., Vol. 6, no. 3, pp. E372–E390, Sep. 2005.
[14] A. D. Khan, M. Bajpai. "Floating drug delivery system: an overview,” Pharm. Tech., Vol. 2, no. 4, pp. 2497-2505, Oct-Dec 2010.
[15] B. N. Singh, K.H. Kim. "Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention,” J. Control. Release., Vol. 63, No. 3, pp. 235-259, Feb. 2000.
[16] Shishu, N. Gupta and N. Aggarwal. "Bioavailability enhancement and targeting of stomach tumors using gastro-retentive floating drug delivery system of curcumin—"a technical note”,” AAPS Pharm. Sci. Tech., Vol. 9, No. 3, pp. 810–813, Sep. 2008.
[17] A. K. Singhal, N. Nalwaya, E. E. Jarald and S. Ahmed. "Colon targeted curcumin delivery using guar gum,” Phcog. Res., Vol 2, no. 2, pp. 82-85, 2010.
[18] R. K. Das, N. Kasoju, U. Bora. "Encapsulation of curcumin in alginate-chitosan-pluronic composite nanoparticles for delivery to cancer cells” Nanomedicine., Vol. 6, no. 1, pp. 153-160, Feb. 2010.
[19] S. Mishra, K. Pathak. "Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine,” Acta. Pharm., Vol. 58, no. 2, pp. 187–197, Jun. 2008.
[20] I. Singh, P. Kumar, H. Singh, M. Goyal and V. Rana. "Formulation and evaluation of domperidone loaded mineral oil entrapped emulsion gel (MOEG) buoyant beads,” Acta. Pol. Pharm., Vol. 68, no. 1, pp. 121-126, Jan.-Feb. 2011.
[21] S. Setthacheewakul, S. Mahattanadul, N. Phadoongsombut, W. Pichayakorn, R. Wiwattanapatapee. "Development and evaluation of self-microemulsifying liquid and pellet formulations of curcumin, and absorption studies in rats,"Eur. J. Pharm. Biopharm., Vol. 76, no. 3, pp. 475-485, Nov. 2010.
[1] B. Gander, K. Ventouras, R. Gurny and E. Doelker. "In vitro dissolution medium with supramicellar surfactant concentration and its relevance for in vivo absorption,” Int. J. Pharm., Vol. 27, no. 1, pp. 117–124, Nov. 1985.
[2] P. Somparn, C. Phisalaphong, S. Nakornchai, S. Unchern and N. P. Morales. "Comparative antioxidant activities of curcumin and its demethoxy and hydrogenated derivatives,” Biol. Pharm. Bull., Vol. 30, no. 1, pp. 74-78, Jan. 2007.
[3] X. Wang, Y. Jiang, Y. Wang, M. Huang, C. Ho and Q. Huang. "Enhancing anti-inflammation activity of curcumin through O/W nanoemulsions,” Food. Chem., Vol. 108, no. 2, pp. 419-424, May. 2008.
[4] N. Chainani-Wu. "Safety and anti-inflammatory activity of curcumin: a component of tumeric (Curcuma longa),” J. Altern. Complement. Med., Vol. 9, no. 1, pp. 161-168, Feb 2003.
[5] K. J. Kim, H. H. Yu, J. D. Cha, S. J. Seo, N. Y. Choi and Y. O. You. "Antibacterial activity of Curcuma longa L. against methicillin-resistant Staphylococcus aureus," Phytother. Res., Vol. 19, no. 7, pp. 599-604, Jul. 2005.
[6] S. Mahattanadul, T. Nakamura, P. Panichayupakaranant, N. Phdoongsombut, K. Tungsinmunkong and P. Bouking. "Comparative antiulcer effect of bisdemethoxycurcumin and curcumin in a gastric ulcer model system,” Phytomedicine, Vol. 16, no. 4, pp. 342-351, Apr. 2009.
[7] U. M. Viradia, A. M. Shenoy, M. S. Rajan, A. R. Shabaraya, A. D. Kothadia and N. H. Patel. "Effect of leukotriene receptor antagonist montelukast along with curcumin against gastric ulceration,” Int. J. Pharm. Sci. Rev. Res., Vol. 3, no. 3, pp. 184-187, 2011.
[8] A. Goel, A. B. Kunnumakkara, B. B. Aggarwal. "Curcumin as "Curecumin": from kitchen to clinic,” Biochem. Pharmacol., Vol. 75, no. 4, pp. 787-809, Feb. 2008.
[9] P. Yoysungnoen, P. Wirachwong, C. Changtam, A. Suksamrarn and S. Patumraj. "Anti-cancer and anti-angiogenic effects of curcumin and tetrahydrocurcumin on implanted hepatocellular carcinoma in nude mice,” World. J. Gastroenterol., Vol.14, no. 13, pp. 2003-2009, Arp.2008.
[10] P. Anand, A. B. Kunnumakkara, R. A. Newman, B. B. Aggarwal. "Bioavailability of curcumin: problems and promises,” Mol. Pharm., Vol. 4, no. 6, pp. 807-818, Nov.-Dec. 2007.
[11] P. Ratanajiajaroen, M. Ohshima. "Synthesis, release ability and bioactivity evaluation of chitin beads incorporated with curcumin for drug delivery applications,” J. Microencapsul., Vol. 29, No. 6, pp. 549-558, 2012.
[12] S. Song, Z. Wang, Y. Qian, L. Zhang and E. Luo, "The release rate of curcumin from calcium alginate beads regulated by food emulsifiers," J. Agric. Food. Chem., Vol. 60, no. 17, pp. 4388-4395, May. 2012.
[13] S. Arora, J. Ali, A. Ahuja, R. K. Khar, and S. Baboota. "Floating drug delivery systems: a review,” AAPS Pharm. Sci. Tech., Vol. 6, no. 3, pp. E372–E390, Sep. 2005.
[14] A. D. Khan, M. Bajpai. "Floating drug delivery system: an overview,” Pharm. Tech., Vol. 2, no. 4, pp. 2497-2505, Oct-Dec 2010.
[15] B. N. Singh, K.H. Kim. "Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention,” J. Control. Release., Vol. 63, No. 3, pp. 235-259, Feb. 2000.
[16] Shishu, N. Gupta and N. Aggarwal. "Bioavailability enhancement and targeting of stomach tumors using gastro-retentive floating drug delivery system of curcumin—"a technical note”,” AAPS Pharm. Sci. Tech., Vol. 9, No. 3, pp. 810–813, Sep. 2008.
[17] A. K. Singhal, N. Nalwaya, E. E. Jarald and S. Ahmed. "Colon targeted curcumin delivery using guar gum,” Phcog. Res., Vol 2, no. 2, pp. 82-85, 2010.
[18] R. K. Das, N. Kasoju, U. Bora. "Encapsulation of curcumin in alginate-chitosan-pluronic composite nanoparticles for delivery to cancer cells” Nanomedicine., Vol. 6, no. 1, pp. 153-160, Feb. 2010.
[19] S. Mishra, K. Pathak. "Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine,” Acta. Pharm., Vol. 58, no. 2, pp. 187–197, Jun. 2008.
[20] I. Singh, P. Kumar, H. Singh, M. Goyal and V. Rana. "Formulation and evaluation of domperidone loaded mineral oil entrapped emulsion gel (MOEG) buoyant beads,” Acta. Pol. Pharm., Vol. 68, no. 1, pp. 121-126, Jan.-Feb. 2011.
[21] S. Setthacheewakul, S. Mahattanadul, N. Phadoongsombut, W. Pichayakorn, R. Wiwattanapatapee. "Development and evaluation of self-microemulsifying liquid and pellet formulations of curcumin, and absorption studies in rats,"Eur. J. Pharm. Biopharm., Vol. 76, no. 3, pp. 475-485, Nov. 2010.
@article{"International Journal of Medical, Medicine and Health Sciences:65842", author = "Arpa Petchsomrit and Namfa Sermkaew and Ruedeekorn Wiwattanapatapee", title = "Effect of Alginate and Surfactant on Physical Properties of Oil Entrapped Alginate Bead Formulation of Curcumin", abstract = "Oil entrapped floating alginate beads of curcumin were developed and characterized. Cremophor EL, Cremophor RH and Tween 80 were utilized to improve the solubility of the drug. The oil-loaded floating gel beads prepared by emulsion gelation method contained sodium alginate, mineral oil and surfactant. The drug content and % encapsulation declined as the ratio of surfactant was increased. The release of curcumin from 1% alginate beads was significantly more than for the 2% alginate beads. The drug released from the beads containing 25% of Tween 80 was about 70% while a higher drug release was observed with the beads containing Cremophor EL or Cremohor RH (approximately 90%). The developed floating beads of curcumin powder with surfactant provided a superior drug release than those without surfactant. Floating beads based on oil entrapment containing the drug solubilized in surfactants is a new delivery system to enhance the dissolution of poorly soluble drugs.
", keywords = "Alginate, curcumin, floating drug delivery, oil entrapped bead.", volume = "7", number = "12", pages = "868-5", }
