Preparation and characterization of mucoadhesive enteric-coating ginsenoside-loaded microparticles

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• 作者：Jong-Suep Baek ; Won-Gi Yeon ; Cho-A Lee ; Sung-Joo Hwang…
• 关键词：Ginsenoside ; Eudragit L100 ; 55 ; Microparticle ; Spray ; drying ; Mucoadhesive ; Oral delivery
• 刊名：Archives of Pharmacal Research
• 出版年：2015
• 出版时间：May 2015
• 年：2015
• 卷：38
• 期：5
• 页码：761-768
• 全文大小：814 KB
• 参考文献：Akbuga, J. 1991. Furosemide-loaded ethyl cellulose microspheres prepared by spherical crystallization technique. International Journal of Pharmaceutics 76: 193-98.View Article
  Benishin, C.G., R. Lee, L.C. Wang, and H.J. Liu. 1991. Effects of ginsenoside Rb1 on central cholinergic metabolism. Pharmacology 42: 223-29.View Article PubMed
  Bozdag, S., S. Calis, and M. Sumnu. 1999. Formulation and stability evaluation of enteric-coated omeprazole formulations. STP Pharma Sciences 9: 321-27.
  Chen, Y.M., X.W. Li, and G.H. Zhu. 2010. Analysis of 103 cases with adverse drug reactions induced by Panax notoginseng saponins injection. Chinese Herbal Medicine: Materia Medica 35: 237-39.
  Coon, J.T., and E. Ernst. 2002. Panax ginseng: A systematic review of adverse effects and drug interactions. Drug Safety 25: 323-44.View Article PubMed
  Eldrige, J.H., C.J. Hommond, J.A. Meulbroek, J.K. Staas, R.M. Gilley, and T.R. Tice. 1990. Controlled vaccine release in the gut-associated lymphoid tissues. Part 1. Orally administered biodegradable microspheres target the Peter’s patches. Journal of Controlled Release 11: 205-14.View Article
  Enayatifard, R., M. Saeedi, J. Akbari, and Y.H. Tabatabaee. 2009. Effect of hydroxypropyl methylcellulose and ethyl cellulose content on release profile and kinetics of diltiazem HCl from matrices. Tropical Journal of Pharmaceutical Research 8: 425-32.View Article
  Han, M., and X.L. Fang. 2006. Difference in oral absorption of ginsenoside Rg1 between in vitro and in vivo models. Acta Pharmacologica Sinica 27: 499-05.View Article PubMed
  Han, M., X. Sha, Y. Wu, and X. Fang. 2006. Oral absorption of ginsenoside Rb1 using in vitro and in vivo models. Planta Medica 72: 398-04.View Article PubMed
  Hasegawa, H., J.H. Sung, S. Matsumiya, and M. Uchiyama. 1996. Main ginseng saponin metabolites formed by intestinal bacteria. Planta Medica 62: 453-57.View Article PubMed
  Holman, L.E., and H. Leuenberger. 1988. The relationship between solid fraction and mechanical properties of compacts—The percolation theory model approach. International Journal of Pharmaceutics 46: 35-4.View Article
  Kanaoks, M., T. Akao, and K. Kobashi. 1994. Metabolism of ginseng saponins, ginsenoside, by human intestinal flora. Journal of Traditional Medicine 11: 241-46.
  Lai, C., Q. Zheng, M. Yang, P. Hu, J. Pan, and C. Peng. 2009. Preparation and prescription of enteric coated pellets of Panax notoginseng saponins pellets. Zhongguo Zhong Yao Za Zhi 34: 1359-363.PubMed
  Leuenberger, H., B.D. Rohera, and C. Haas. 1987. Percolation theory—A novel approach to solid dosage form design. International Journal of Pharmaceutics 38: 109-15.View Article
  Lim, J.H., S.K. You, J.S. Baek, C.J. Hwang, Y.G. Na, S.C. Shin, and C.W. Cho. 2012. Surface-modified gemcitabine with mucoadhesive polymer for oral delivery. Journal of Microencapsulation 29: 487-96.View Article PubMed
  Nah, S.Y., and E.W. McCleskey. 1994. Ginseng root extract inhibits calcium channels in rat sensory neurons through a similar path, but different receptor, as mu-type opioids. Journal of Ethnopharmacology 42: 45-1.View Article PubMed
  Odani, T., H. Tanizawa, and Y. Takino. 1983. Studies on the absorption, distribution excretion and metabolism of ginseng saponins II. Chemical and Pharmaceutical Bulletin 31: 292-98.View Article PubMed
  Rowe, R.C. 1992. Molecular weight dependence of the properties of ethyl cellulose and hydroxypropyl methyl cellulose films. International Journal of Pharmaceutics 88: 405-08.View Article
  Seo, J.Y., J.H. Lee, N.W. Kim, E. Her, S.H. Chang, N.Y. Ko, Y.H. Yoo, J.W. Kim, D.W. Seo, J.W. Han, Y.M. Kim, and W.S. Choi. 2005. Effect of a fermented ginseng extract, BST204, on the expression of cyclooxygenase-2 in murine macrophages. International Immunopharmacology 5: 929-36.View Article PubMed
  Shaikh, N.A., S.E. Abidi, and L.H. Block. 1987. Evaluation of ethyl cellulose as a matrix for prolonged release formulations Part 1. Water soluble drugs-acetaminophen theophylline. Drug Development and Industrial Pharmacy 14: 1345-369.View Article
  Takeuchi, H., J. Thongborisute, and Y. Matsui. 2005. Novel mucoadhesion tests for polymers and polymer-coated particles to design optimal mucoadhesive drug delivery systems. Advanced Drug Delivery Reviews 57: 1583-594.View Article PubMed
  Takino, Y., T. Odani, H. Tanizawa, and T. Hayashi. 1982. Studies on the absorption, distribution, excretion and metabolism of ginseng saponin I. Chemical and Pharmaceutical Bulletin 30: 2196-201.View Article PubMed
  Tyler, V.E. 1995. Herbal remedies. The Journal of Pharmacy Technology 11: 214-20.
  
• 作者单位：Jong-Suep Baek (1)
  Won-Gi Yeon (1)
  Cho-A Lee (1)
  Sung-Joo Hwang (2)
  Jeong-Sook Park (1)
  Dong-Chool Kim (1)
  Cheong-Weon Cho (1)
  
  1. College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 220 Gung-dong, Yuseong-gu, Taejon, 305-764, South Korea
  2. College of Pharmacy, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Inchon, 406-840, South Korea
  
• 刊物主题：Pharmacy; Pharmacology/Toxicology;
• 出版者：Springer Netherlands
• ISSN：1976-3786

文摘

Ginsenoside saponins are phytochemically extracted from red ginseng and have been regarded as the principal components manifesting the pharmacologic activities. Saponins are very soluble in water but poorly absorbed when orally administrated. Moreover, they have some disadvantages including the decomposition in acid medium. The aim of this study was to develop oral formulation of ginsenosides composed of enteric-coating polymer and mucoadhesive polymer considering the low stability in acid medium and the low permeability of saponins. Ginsenoside-loaded microparticles were prepared by spray dryer. The influences of various parameters such as the ratio of saponin to polymer, feed concentration, feed rate, inlet/outlet temperature and additional excipients during spray-drying were investigated. In vitro release profile of ginsenoside-loaded microparticles using additional excipients, ginsenoside saponin Rg1 or Rb1 showed an 18 or 13?% release in pH 1.2 when ethyl cellulose was added. Also, ginsenoside-loaded microparticles exhibited mucoadhesive properties in the presence of chitosan. The application of these polymers is being considered as the potential strategy for improvement of bioavailability in saponin delivery, orally.