Long-acting liposomal corneal anesthetics.
Long-acting liposomal corneal anesthetics.
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DOI：
10.1016/j.biomaterials.2018.07.054
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发表时间：
2018-10
期刊：
影响因子：
14
通讯作者：
Kohane DS
中科院分区：
文献类型：
--
作者：
Zhan C;Santamaria CM;Wang W;McAlvin JB;Kohane DS
产生长效眼部麻醉的滴眼剂对于角膜疼痛管理是期望的。在这里，我们提出了基于脂质体的制剂，以实现单滴眼液滴注后非常长的眼部麻醉效果。脂质体用琥珀酰-伴刀豆球蛋白A（sConA-Lip）官能化，其可以结合角膜聚糖部分，以显著延长脂质体在角膜上的停留时间。sConA-Lip负载有河豚毒素和右美托咪啶（sConA-Lip/TD），并为两者提供持续释放。在角膜上单次局部滴注sConA-Lip/TD可实现105 min的密集镇痛和540 min的部分镇痛，这显著长于丙美卡因、河豚毒素/右美托咪定溶液或含有河豚毒素和右美托咪定的未修饰脂质体的镇痛。sConA-Lip/TD在体外对人角膜缘上皮细胞和角膜基质细胞无细胞毒性。局部施用sConA-Lip/TD提供了延长的角膜麻醉而不延迟角膜伤口愈合。这种制剂可用于急性手术和非手术角膜疼痛的管理，或用于治疗其它眼表面疾病。
Eye drops producing long-acting ocular anesthesia would be desirable for corneal pain management. Here we present liposome-based formulations to achieve very long ocular anesthetic effect after a single eye drop instillation. The liposomes were functionalized with succinyl-Concanavalin A (sConA-Lip), which can bind corneal glycan moieties, to significantly prolong the dwell time of liposomes on the cornea. sConA-Lip were loaded with tetrodotoxin and dexmedetomidine (sConA-Lip/TD), and provided sustained release for both. A single topical instillation of sConA-Lip/TD on the cornea could achieve 105 min of dense analgesia and 540 min of partial analgesia, which was significantly longer than analgesia with proparacaine, tetrodotoxin/dexmedetomidine solution or unmodified liposomes containing tetrodotoxin and dexmedetomidine. sConA-Lip/TD were not cytotoxic in vitro to human corneal limbal epithelial cells or corneal keratocytes. Topical administration of sConA-Lip/TD provided prolonged corneal anesthesia without delaying corneal wound healing. Such a formulation may be useful for the management of acute surgical and nonsurgical corneal pain, or for treatment of other ocular surface diseases.
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DOI：
10.1007/bf01939943
发表时间：
1990-07-15
期刊：
EXPERIENTIA
影响因子：
--
作者：
MCCALDEN, TA;LEVY, M
通讯作者：
LEVY, M
影响因子：
3.7
作者：
Kohane, DS;Lipp, M;Langer, R
通讯作者：
Langer, R
DOI：
10.1073/pnas.70.4.1012
发表时间：
1973-01-01
影响因子：
11.1
作者：
GUNTHER, GR;WANG, JL;EDELMAN, GM
通讯作者：
EDELMAN, GM
影响因子：
2.8
作者：
Nam, SM;Lee, HK;Seo, KY
通讯作者：
Seo, KY
影响因子：
2.8
作者：
LIU, JC;STEINEMANN, TL;BEUERMAN, RW
通讯作者：
BEUERMAN, RW