Related Experiment Video
Updated: May 5, 2026
Combination of Microstereolithography and Electrospinning to Produce Membranes Equipped with Niches for Corneal Regeneration
Published on: September 12, 2014
Nanoparticle-hydrogel composite as dual-drug delivery system for the potential application of corneal graft rejection
Xiaoning Xu1, Yuqin Wu1, Ruiling Gu1
1National Engineering Research Center of Ophthalmology and Optometry, Eye Hospital, Wenzhou Medical University, Wenzhou 325027, China.
Abstract:
Immune rejection remains the major cause of corneal graft failure. Immunosuppressants (such as rapamycin; RAPA) adjunctive to antibiotics (such as levofloxacin hydrochloride; Lev) are a clinical mainstay after corneal grafts but suffer from poor ocular bioavailability associated with severe side effects. In this study, we fabricated a Lev@RAPA micelle loaded cationic peptide-based hydrogel (NapFFKK) as a dual-drug delivery system by integrating RAPA micelles with Lev into a cationic NapFFKK hydrogel to potentially reduced the risk of corneal graft rejection. The properties of the resulting hydrogels were characterized using transmission electronmicroscopy and rheometer. Lev@RAPA micelles loaded NapFFKK hydrogel provided sustained in vitro drug release without compromising their inherent pharmacological activities. Topical instillation of Lev@RAPA micelles loaded NapFFKK hydrogel resulted in the great ocular tolerance and extended precorneal retention over 60 min, thus significantly enhancing the ocular bioavailability of both Lev and RAPA. Overall, such dual-drug delivery system might be a promising formulation for the suppression of corneal graft failure.
Insights
A novel dual-drug hydrogel delivery system loaded with rapamycin (RAPA) and levofloxacin hydrochloride (Lev) enhances ocular bioavailability, potentially reducing corneal graft rejection and improving graft survival.
Area of Science:
- Ophthalmology
- Biomaterials Science
- Drug Delivery Systems
Background:
- Corneal graft failure is primarily caused by immune rejection.
- Current treatments using immunosuppressants like rapamycin (RAPA) and antibiotics like levofloxacin hydrochloride (Lev) have limited ocular bioavailability and side effects.
Purpose of the Study:
- To develop a dual-drug delivery system using a cationic peptide-based hydrogel (NapFFKK) loaded with rapamycin (RAPA) micelles and levofloxacin hydrochloride (Lev).
- To evaluate the potential of this system in reducing corneal graft rejection by enhancing ocular drug bioavailability.
Main Methods:
- Fabrication of a Lev@RAPA micelle loaded cationic peptide-based hydrogel (NapFFKK).
- Characterization of hydrogel properties using transmission electron microscopy and rheometry.
- Assessment of in vitro drug release, ocular tolerance, and precorneal retention time.
Main Results:
- The Lev@RAPA micelles loaded NapFFKK hydrogel demonstrated sustained in vitro drug release.
- The hydrogel exhibited excellent ocular tolerance and extended precorneal retention (>60 minutes).
- Significant enhancement in ocular bioavailability for both Lev and RAPA was observed.
Conclusions:
- The developed dual-drug delivery system shows promise for suppressing corneal graft rejection.
- This formulation may offer an improved therapeutic strategy for corneal transplantation by enhancing drug delivery and efficacy.
Related Concept Videos
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
01:23Ophthalmic Drug Delivery Systems