With exquisite biological, physical and chemical properties, cellulose nanocrystals (CNCs) have been considered as an ideal drug carrier. A novel prodrug was prepared by the covalent attachment of the tosufloxacin tosylate (TFLX) onto the surface of maleated cellulose nanocrystals (MA-CNCs) with L-leucine as a spacer. The successful coupling of MA-CNCs and TFLX was detected by fourier transformation infrared spectroscopy (FTIR). The satisfactory coverage of MA- CNCs on TFLX is shown in FE- SEM micrographs. The release behaviors of TFLX- A- MA- CNCs in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF) were investigated. The relationship between the accumulative drug release and the fluorescence response has been evaluated. The results show that the drug was efficiently entrapped by MA-CNCs carrier and presents excellent behavior for colon specificity and may be considered as a potential material for a colon-specific drug delivery system.
TANG Lirong
,
HUANG Biao
,
LI Tao
,
LU Qilin
,
CHEN Xuerong
. Functionalized Cellulose Nanocrystals as a Carrier for Colon-targeted Drug Delivery System[J]. Science & Technology Review, 2014
, 32(4-5)
: 22
-28
.
DOI: 10.3981/j.issn.1000-7857.2014.h1.002
[1] Verma S, Kumar V, Mishra D N, et al. Colon targeted drug delivery: current and novel perspectives[J]. International Journal of Pharmaceutical Sciences and Research, 2012, 3(5): 1274-1284.
[2] Chourasia M K, Jain S K. Pharmaceutical approaches to colon targeted drug delivery systems[J]. Journal of Pharmacy and Pharmaceutical Sciences, 2003, 6(1): 33-66.
[3] Patel M, Shah T, Amin A. Therapeutic opportunities in colon-specfic drug-delivery systems[J]. Critical Reviews in Therapeutic Drug Carrier Systems, 2007, 24(2): 147-202.
[4] Sinha V R, Kumria R. Microbially triggered drug delivery to the colon[J]. European Journal of Pharmaceutical Sciences, 2003, 18(1): 3-18.
[5] Jose S, Dhanya K, Cinu T A, et al. Colon targeted drug delivery: Different approaches[J]. Journal of Young Pharmacists, 2009, 1(1): 13- 19.
[6] Kumar R S, Kumar M, Ganesh G N, et al. Formulation and evaluation of pectin- hydroxypropyl methylcellulose coated curcumin pellets for colon delivery[J]. Asian Journal of Pharmaceutics, 2009, 3(2): 138-142.
[7] SivakumarB,AswathyRG,NagaokaY,etal.Multifunctionalcarboxymethyl cellulose-based magnetic nanovector as a theragnostic system for folate receptor targeted chemotherapy, imaging, and hyperthermia against cancer[J]. Langmuir, 2013, 29(10): 3453-3466.
[8] Cai X, Yang L Q, Zhang L M, et al. Synthesis and anaerobic biodegradation of indomethacin- conjugated cellulose ethers used for colon- specific drug delivery[J]. Bioresource Technology, 2009, 100(18): 4164-4170.
[9] Hussain M A, Badshah M, Iqbal M S, et al. HPMC- salicylate conjugates as macromolecular prodrugs: Design, characterization, and nano- rods formation[J]. Journal of Polymer Science Part A: Polymer Chemistry, 2009, 47(16): 4202-4208.
[10] Shiose Y, Kuga H, Ohki H, et al. Systematic research of peptide spacers controlling drug release from macromolecular prodrug system, carboxymethyldextran polyalcohol-peptide-drug conjugates[J]. Bioconjugate Chemistry, 2009, 20(1): 60-70.
[11] Huynh V T, Quek J Y, de Souza P L, et al. Block copolymer micelles with pendant bifunctional chelator for platinum drugs: Effect of spacer length on the viability of tumor cells[J]. Biomacromolecules, 2012, 13 (4): 1010-1023.
[12] Rautio J. Prodrugs and targeted delivery. Towards better ADME properties[M]. Weinheim: Wiley-VCH Verlag GmbH & Co. KGaA, 2011.
[13] 冯波, 何仲贵, 张秀荣, 等. 沙丁胺醇包合物缓释片的释药机制研究[J]. 吉林医药学院学报, 2005, 26(3): 125-127. Feng Bo, He Zhonggui, Zhang Xiurong, et al. Study on release mechanism of salbutamol- ethylated β- cyclodextrins complexes sustained release tablets[J]. Journal of Jilin Medical College, 2005, 26 (3): 125-127.
[14] Peppas N A. Analysis of Fickian and non-Fickian drug release from polymers[J]. Pharmaceutica acta Helvetiae, 1985, 60(4): 110-111.
[15] 吕凤娇, 许小平. 阿霉素纳米粒体外释放模型的拟合研究[J]. 计算机 与应用化学, 2010, 27(7): 915-918. Lv Fengjiao, Xu Xiaoping. A study on fitting models of the vitro release of Doxorubicin-nanoparticles[J]. Computers and Applied Chemistry, 2010, 27(7): 915-918.
[16] 徐玉福, 姚日生, 邓胜松, 等. 淀粉微凝胶对阿司匹林片体外释药的 影响[J]. 中国药学杂志, 2006, 41(19): 1479-1482. Xu Yufu, Yao Risheng, Deng Shengsong, et al. Effect of starch microgels on aspirin release from tablets in vitro[J]. Chinese Pharmaceutical Journal, 2006, 41(19): 1479-1482.
[17] Deng F, Liu Y. Study of the interaction between tosufloxacin tosylate and bovine serum albumin by multi-spectroscopic methods[J]. Journal of Luminescence, 2012, 132(2): 443-448.
[18] Galindo- Rodríguez S A, Allémann E, Fessi H, et al. Polymeric nanoparticles for oral delivery of drugs and vaccines: A critical evaluation of in vivo studies[J]. Critical Reviews in Therapeutic Drug Carrier Systems, 2005, 22(5): 419-463.