载药眼科用 N,O-羧甲基壳聚糖水凝胶的制备、体外及体内评价。
Ophthalmic drug-loaded N,O-carboxymethyl chitosan hydrogels: synthesis, in vitro and in vivo evaluation.
机构信息
Institute of Polymer Science, School of Chemistry and Chemical Engineering, China.
出版信息
Acta Pharmacol Sin. 2010 Dec;31(12):1625-34. doi: 10.1038/aps.2010.125. Epub 2010 Nov 1.
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.
目的
研究载药 N,O-羧甲基壳聚糖（CMCS）水凝胶在青光眼滤过手术后调节伤口愈合的能力。
方法
以京尼平为交联剂，在 5-氟尿嘧啶（5FU）或贝伐单抗存在的情况下，原位合成载药 CMCS 水凝胶。通过傅里叶变换红外光谱（FTIR）、紫外-可见（UV-vis）光谱和扫描电子显微镜（SEM）对其结构进行了表征。进行了体外药物释放实验和兔体内评价。
结果
FTIR、UV-vis 光谱和 SEM 分析结果表明，5FU 被包封到由京尼平交联的 CMCS 水凝胶中。体外药物释放实验表明，载药水凝胶在 8 h 内几乎 100%释放了 5FU，但在 53 h 后仅释放了不到 20%的贝伐单抗。兔体内评价表明，载药 CMCS 水凝胶对角膜无毒，并且在眼睛中逐渐生物降解。此外，载药 CMCS 水凝胶有效抑制了青光眼滤过手术后的结膜瘢痕形成，并控制了术后眼内压（IOP）。
结论
载药 CMCS 水凝胶为提高青光眼滤过手术的疗效提供了很好的机会。
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