Bodor N, Varga M
Center for Drug Design and Delivery, College of Pharmacy, University of Florida, Gainesville 32610.
Exp Eye Res. 1990 Feb;50(2):183-7. doi: 10.1016/0014-4835(90)90229-n.
The effect of a 'soft' anti-inflammatory corticosteroid on the corneal wound healing was investigated in rabbits. Albino rabbits were treated with soft steroid and dexamethasone after linear perforating corneal incision. Soft drug design is aimed to control and direct the drug activity and in vivo metabolism to nontoxic moieties. These drugs are rapidly deactivated after they reach the general circulation. While having good local activity, they thus possess high therapeutic indexes without systemic side effects. The wound healing process was evaluated qualitatively by histology. Photomicrographs are presented to show that the soft steroid is as or more effective than dexamethasone in minimizing scarring in addition to its advantageous metabolic properties. This soft steroid may be an efficient anti-inflammatory and anti-allergic agent in topical application without the majority of unwanted activities of traditional drugs by deliberately simplifying their disposition.
在兔子身上研究了一种“软性”抗炎皮质类固醇对角膜伤口愈合的影响。白化兔在角膜线性穿孔切口后接受软性类固醇和地塞米松治疗。软性药物设计旨在控制并引导药物活性以及体内代谢至无毒部分。这些药物进入体循环后会迅速失活。因此,它们在具有良好局部活性的同时,拥有高治疗指数且无全身副作用。通过组织学对伤口愈合过程进行定性评估。提供的显微照片显示,除了具有有利的代谢特性外,软性类固醇在使瘢痕形成最小化方面与地塞米松一样有效或更有效。通过刻意简化其处置方式,这种软性类固醇可能是一种有效的局部应用抗炎和抗过敏药物,而不会产生传统药物的大多数不良作用。