Synthesis and characterization of a novel pH-sensitive complex for drug release

Dongying Xu1, Guangji Li1, Zhengfu Liao2, Xudong Chen3
1Department of Polymer Science and Engineering, South China University of Technology, Guangzhou, China
2Faculty of Materials and Energy, Guangdong University of Technology, Guangzhou, China
3School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, China

Tóm tắt

A novel pH-sensitive complex was prepared by using oxidized konjac glucomannan and 4-aminosalicylic acid (4-ASA) through glutaraldehyde as a cross-linking agent. The product was characterized by FTIR and 13C NMR spectra, and the thermogravimetric analysis was also studied. The drug release studies in vitro showed that the amount of 4-ASA released from the complex was about 4%, 56% and 17% after 12 h at pH 1.2, 6.8 and 7.4, respectively. The data demonstrate that the rate of the drug release of the complex can be more effectively controlled by pH value. The results showed that the novel pH-sensitive complex could be potentially useful for colon-targeting drug delivery system.

Tài liệu tham khảo

V R Sinha, R Kumria. Polysaccharides in Colon-Specific Drug Delivery[J]. Int. J. Pharm., 2001, 224(1–2): 19–38 J Nunthanid, K Huanbutta, M Luangtana-anan, et al. Development of Time-, pH-, and Enzyme-Controlled Colonic Drug Delivery Using Spray-Dried Chitosan Acetate and Hydroxypropyl Methylcellulose[J]. Eur. J. Pharm. & Biopharm., 2008, 68(2): 253–259 S Salmaso, A Semenzato, S Bersani, et al. Cyclodextrin/PEG Based Hydrogels for Multi-Drug Delivery[J]. Int. J. Pharm., 2007, 345(1–2): 42–50 Y H Huang, H Q Yu, C B Xiao. pH-Sensitive Cationic Guar Gum/Poly (acrylic acid) Polyelectrolyte Hydrogels: Swelling and in Vitro Drug Release[J]. Carbohyd. Polym., 2007, 69(4): 774–783 V Ramesh Babu, K S V Krishna Rao, M Sairam, et al. pH Sensitive Interpenetrating Network Microgels of Sodium Alginate-Acrylic Acid for the Controlled Release of Ibuprofen[ J]. J. Appl. Polym. Sci., 2006, 99(5): 2 671–2 678 C Jantarat, N Tangthong, S Songkro, et al. S-Propranolol Imprinted Polymer Nanoparticle-on-Microsphere Composite Porous Cellulose Membrane for the Enantioselectively Controlled Delivery of Racemic Propranolol[J]. Int. J. Pharm., 2008, 349(1-2): 212–225 L G Chen, Z L Liu, R X Zhuo. Synthesis and Properties of Degradable Hydrogels of Konjac Glucomannan Grafted Acrylic Acid for Colon-Specific Drug Delivery[J]. Polymer, 2005, 46(16): 6 274–6 281 J Du, J Dai, J L Liu, et al. Novel pH-Sensitive Polyelectrolyte Carboxymethyl Konjac Glucomannan-Chitosan Beads as Drug Carriers[J]. React. & Funct. Polym., 2006, 66(10):1 055–1 061 H Zhang, M Yoshimura, K Nishinari, et al. Gelation Behaviour of Konjac Glucomannan with Different Molecular Weights[J]. Biopolymer, 2001, 59(1): 38–50 U J Kim, S Kuga, M Wada, et al. Periodate Oxidation of Crystalline Cellulose[J]. Biomacromolecules, 2000, 1(3): 488–492 K Y Lee, K H Bouhadir, D J Mooney. Degradation Behavior of Covalently Cross-Linked Poly (aldehyde guluronate) Hydrogels[J]. Macromolecules, 2000, 33(1): 97–101