Sustained release of levofloxacin from thermosensitive chitosan‐based hydrogel for the treatment of postoperative endophthalmitis

Abstract

In the field of ophthalmology, postoperative endophthalmitis (POE) is a serious surgical complication, which may lead to poor visual outcome even after the infection has been controlled. In the study, we develop a sustained drug releasing system loaded with levofloxacin which is expected to be effective against common pathogens responsible for POE for at least 7 days after single application at the end of surgery. The results of study showed that the sol–gel transition temperature of the levofloxacin‐loaded chitosan‐gelatin‐based solution was ~34°C. The gelation time of the developed formulation was ~81 s at 34°C. The results showed that the osmolality of developed hydrogel was 304 mOsm/L. The in vitro drug release studies revealed that levofloxacin release from the developed hydrogel displayed a sustained‐release profile. The long‐term antibacterial property of the developed hydrogel has been demonstrated. The biocompatibility of the developed hydrogel was evaluated in vitro. These results suggest that the levofloxacin‐containing hydrogel could be applied to ocular surface at the end of ophthalmic surgery, without the risks of intracameral injection of antibiotics. © 2019 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater 108B:8–13, 2020.

Development of topical chitosan/ β-glycerophosphate-based hydrogel loaded with levofloxacin in the treatment of keratitis: An ex-vivo study

“…The chitosan-gelatin based levofloxacin-loaded hydrogels were prepared as described previously [ 45 ]. In brief, we first prepared the chitosan/gelatin/β-glycerophosphate solution.…”

“…However, none were applicated with chitosan/gelatin/β-glycerophosphate hydrogel. In our previous in vitro study [ 45 ], we have developed a levofloxacin-loaded chitosan/gelatin/β-glycerophosphate hydrogel that increases the retention time of drugs on the ocular surface, which is important for maintaining an effective therapeutic drug concentration. It was optimized no matter in temperature for sol-gel transition on ocular surface, or osmolarity suitable for topical use [ 46 ].…”

Hydrogels as Emerging Materials for Cornea Wound Healing

“…[ 96 ] The hydrogel also showed two‐step release behavior, a burst release of nepafenac due to desorption and diffusion of drug from the surface, followed with a slow and sustained release behavior. The potential of CTS hydrogels for delivery of various drugs such as Nepafenac, [ 96,97 ] Moxifloxacin and Gentamicin, [ 98 ] 5‐fluorouracil (5FU), [ 99–101 ] Ascorbic acid, [ 102 ] Levofloxacin, [ 103,104 ] Baicalin [ 105 ] and Quercetin [ 106 ] to the defected cornea was also recently confirmed. Table 4 reviews the recent (2010 to 2020) in vitro (Table 4A), in vivo (Table 4B) and cell/drug delivery (Table 4C) investigations and their outcomes on the potential of CTS‐based hydrogels for cornea tissue engineering.…”

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

“…It was shown that the curcumin-containing formulation could decrease the oxidative stress-mediated damage in TM cells. Finally, levofloxacin was also loaded in the CS/gelatin/β-GP hydrogel [248]. In vitro drug release studies evidenced a prolonged release over a 7-day period, while in vitro antibacterial studies against S. aureus and Staphylococcus epidermidis, which can cause endophthalmitis and other ocular infections, showed a clear zone of growth inhibition for at least 7 days.…”

“…C. J. Liu, Y-C Cheng, S-H Chiou, and their coworkers prepared a series of thermosensitive CS/gelatin (type A)/β-GP hydrogels for the ocular delivery of several APIs [ 245 , 246 , 247 , 248 ]. Gelatin was used in order to improve the mechanical strength and gelation properties of CS [ 248 ]. The concentrations of CS and gelatin were 2–2.5% w/v and 0.2–1% w/v , respectively, T gel was around 34 °C, and the gelation time ranged from 40 to 80 s depending on the concentration of the polymers.…”