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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.

DOI:10.1038/aps.2010.125
PMID:21042284
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4002939/
Abstract

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.

摘要

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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