Ophthalmic drug-loaded N,O-carboxymethyl chitosan hydrogels: synthesis, in vitro and in vivo evaluation
Ophthalmic drug-loaded N,O-carboxymethyl chitosan hydrogels: synthesis, in vitro and in vivo evaluation
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DOI：
10.1038/aps.2010.125
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发表时间：
2010-12
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影响因子：
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通讯作者：
Li-qun Yang;Y. Lan;Hui Guo-;Liang-zheng Cheng;Jizhou Fan;Xiang Cai;Li‐Ming Zhang;Ru-fu Chen;Huai-sheng Zhou
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文献类型：
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作者：
Li-qun Yang;Y. Lan;Hui Guo-;Liang-zheng Cheng;Jizhou Fan;Xiang Cai;Li‐Ming Zhang;Ru-fu Chen;Huai-sheng Zhou
目的：探讨N，O-羧甲基壳聚糖(CMCS)载药水凝胶对青光眼滤过术后创面愈合的调节作用。方法：以京尼平为交联剂，在5-氟尿嘧啶(5FU)或贝伐单抗存在下，原位合成载药CMCS水凝胶。用红外光谱、紫外-可见光谱和扫描电子显微镜对其结构进行了表征。结果：FTIR、UV-Vis光谱和扫描电子显微镜分析结果表明，以京尼平为交联剂的CMCS水凝胶中5FU已被包埋。体外释药实验表明，载药水凝胶在8h内释放了近100%的5FU，53h后释放了不到20%的贝伐单抗，兔体内评价表明，该载药水凝胶对角膜无毒，在眼内逐渐被生物降解。此外，载药CMCS水凝胶能有效抑制青光眼滤过术后结膜瘢痕形成，控制术后眼压。结论：CMCS载药水凝胶为提高青光眼滤过手术的疗效提供了良好的契机。
Aim:To investigate the ability of drug-loaded N, O-carboxymethyl chitosan (CMCS) hydrogels to modulate wound healing after glaucoma filtration surgery.Methods:The drug-loaded CMCS hydrogels were in situ synthesized using genipin as the crosslinker in the presence of 5-fluorouracil (5FU) or bevacizumab. Their structures were characterized by FTIR, ultraviolet-visible (UV-vis) spectroscopy and scanning electron microscopy (SEM). In-vitro drug release experiments and in vivo evaluation in rabbits were performed.Results:The results of FTIR, UV-vis spectroscopy and SEM analyses indicated that 5FU was encapsulated into the CMCS hydrogels that were crosslinked by genipin. The in vitro drug release experiments showed that nearly 100% of 5FU was released from the drug-loaded hydrogels within 8 h, but less than 20% bevacizumab was released after 53 h. The in vivo evaluation in rabbits indicated that the drug-loaded CMCS hydrogels were nontoxic to the cornea and were gradually biodegraded in the eyes. Furthermore, the drug-loaded CMCS hydrogels effectively inhibited conjunctival scarring after glaucoma filtration surgery and controlled postoperative intraocular pressure (IOP).Conclusion:The drug-loaded CMCS hydrogels provide a great opportunity to increase the therapeutic efficacy of glaucoma filtration surgery.