Vaka Siva Ram Kiran, Sammeta Srinivasa Murthy, Day Lainy Baird, Murthy Satyanarayana Narasimha
Department of Pharmaceutics, School of Pharmacy, The University of Mississippi, University, Mississippi 38677, USA.
Curr Eye Res. 2008 Aug;33(8):661-7. doi: 10.1080/02713680802270945.
To investigate the feasibility of utilizing iontophoresis for delivery of ciprofloxacin hydrochloride to the anterior chamber of the eye and to carry out systematic studies to investigate the effect of electrical protocol on the transcorneal drug delivery.
Effect of current density (0.75 mA/cm(2) to 6.25 mA/cm(2) applied for 5 minutes) on drug permeation across the cornea and drug load in the cornea were investigated in vitro as well as ex vivo studies in porcine cornea model. Tolerability studies were carried out in rabbits. Cytotoxicity studies were conducted in cultured corneal tissue.
The drug loaded in the cornea increased with increasing current density. After 5 minutes of iontophoresis, the drug concentration in the receiver compartment fluid (in vitro) or in aqueous humor (ex vivo) was not significantly higher than control (in which electric current was not applied). However, waiting for 6-12 hours after iontophoresis for 5 minutes, the concentrations of drug in aqueous humor in ex vivo studies were approximately 6 and approximately 5-fold higher than control (130.12 +/- 78.99 ng/ml), respectively. Cytotoxicity studies demonstrated the safety of the technique. The application of 6.25 mA/cm(2) for 5 minutes (right eye) did not show any sign of loss of vision and abnormal discharge, redness of eye, or edema when compared to the control left eye.
Transcorneal iontophoresis is a potential method of delivering effective levels of ciprofloxacin hydrochloride into aqueous humor for the treatment of intraocular infections. This study unveils the ability of iontophoresis to rapidly drive ciprofloxacin into the cornea where a drug reservoir is formed, which eventually releases slowly into aqueous humor, eliciting sustained therapeutic effect.
研究利用离子电渗疗法将盐酸环丙沙星输送至眼前房的可行性，并进行系统研究以探讨电参数对经角膜药物递送的影响。
在体外以及猪角膜模型的离体研究中，考察了电流密度（0.75 mA/cm²至6.25 mA/cm²，施加5分钟）对药物透过角膜及角膜中药物负载量的影响。在兔子身上进行了耐受性研究。在培养的角膜组织中进行了细胞毒性研究。
角膜中的药物负载量随电流密度增加而增加。离子电渗疗法5分钟后，接受室液体（体外）或房水（离体）中的药物浓度并不显著高于对照组（未施加电流）。然而，离子电渗疗法5分钟后等待6至12小时，离体研究中房水中的药物浓度分别比对照组（130.12±78.99 ng/ml）高约6倍和约5倍。细胞毒性研究证明了该技术的安全性。与对照左眼相比，右眼施加6.25 mA/cm² 5分钟未出现任何视力丧失、异常分泌物、眼红或水肿迹象。
经角膜离子电渗疗法是一种将有效剂量的盐酸环丙沙星输送至房水以治疗眼内感染的潜在方法。本研究揭示了离子电渗疗法能够迅速将环丙沙星驱入角膜形成药物储库，该储库最终缓慢释放至房水，产生持续治疗效果。
