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THE PHARMA REVIEW (AUGUST 2008)

Effect of Collagen Cross-linking in Collagen Corneal Shields on Sustained Release and ex vivo Antimicrobial Efficacy of Gatifloxacin Sesquehydrate

Ritu Mehra Gilhotra, Neeraj Gilhotra and D N Mishra

Abstract: Non cross-linked and cross-linked collagen corneal shields pre-soaked in Gatifloxacin sesquehydrate were studied for in vitro drug absorption. Dissolution study and ex-vivo antimicrobial efficacy testing against S. aureus was carried out. Drug content in collagen corneal shield corresponded to its soaking duration in drug solution. Collagen shields remained intact and were successful in sustaining the drug. Drug release depending on the degree of cross linking in the collagen shields. Most of the drug was released within 0.5 - 4hr of dissolution of shield. Optimized formulations were found to possess significant antimicrobial efficacy. Appropriate dissolution duration and antimicrobial efficacy of collagen corneal shields propose them to be the potential useful drug carriers.

Introduction
Collagen shields are biologically inert, structurally stable and biocompatible polymeric substances that may be well used as drug delivery system. They have been found to act as drug reservoir, which can deliver both hydrophilic as well as hydrophobic drugs, increase the contact time between drug and cornea as they can reversibly bind drug molecules and release them in delayed mode. Moreover, the cost of production of corneal shields is low. Collagen shields are generally manufactured from porcine or bovine collagen and three different collagen shields are currently available with dissolution times of 12, 24, and 72 hours. Presoaking the collagen shield in a pharmacological agent represents the most efficacious method of utilizing collagen shields for drug delivery. They have been observed to enhance drug delivery, promote epithelial and stromal healing, neutralize collagenases, and reduce corneal inflammation in different ophthalmic pathologies like microbial keratitis, conjunctivitis and glaucoma

In the present study, a fourth generation fluoroquinolone Gatifloxacin sesquehydrate (varying concentrations) has been loaded on the Soft Shield® (a marketed collagen corneal shield) with dissolution times of 12-HOUR, 24-HOUR and 72-HOUR. The objective of the study was to explore individual potential of these shields to sustain the antibiotic release and to compare the non cross-linked 12-HOUR shields with the cross-linked 24-HOUR and 72-HOUR shields with reference to in vitro drug release and ex vivo antimicrobial efficacy.

 

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