Chitosan hydrogel containing tacrolimus-loaded nanoliposome for ocular drug delivery: Physicochemical analysis and stability evaluation

Objective(s): Recently, the use of tacrolimus in treating eye diseases has received much attention. Although this drug is powerful in treating eye diseases, however for various reasons, it lacks the necessary efficacy for multiple reasons. This research investigated the development of Tacrolimus encapsulated liposomes, optimization, loading effectiveness, increasing drug efficiency through absorption, controlled release, drug targeting, and reducing drug side effects such as nephropathy.Materials and Methods: Two agents, liposome and chitosan, have been chosen to transport the drugs used in this study. Nanoliposomes were synthesized through the heating method and chitosan nanoparticles were by reversing the micelle method. A field emission scanning electron microscope(FESEM) was used to prepare images and a zeta sizer was used to measure the average size and distribution of particles. Drug release for ۱۸ days was checked by in vitro and ex-vivo(Franz diffusion) tests. The MTT method was used to evaluate the cytotoxic effect of nanoparticles loaded with tacrolimus drug.Results: The molar ratio of the drug to liposome and chitosan was chosen to be ۰.۰۰۲. A drug loading effectiveness of (۸۸-۹۵%) was obtained. Tacrolimus drug loading efficiency in liposomes (EPC۱۰۰, EPC۸۰, DPPC۶۰, DPPC۱۰۰) value (۸۸.۹۵-۹۵-۷۴%) was obtained for its entrapment in liposome core with passive loading strategy. The difference in drug release rate for EPC ۸۰/chitosan liposome and EPC ۱۰۰/chitosan was ۸۳.۶% and ۹۳.۱%, respectively, and for DPPC۶۰/chitosan and DPPC۱۰۰/chitosan liposomes, ۷۲.۸% and ۷۸.۸%, respectively.Conclusion: With this study, it can be concluded that DPPC liposome was good for drug loading. The results of the test (FT-IR) showed that the loading of the drug was successful. The results of electron microscope tests in both samples (EPC, DPPC) indicated the synthesis of drug delivery systems with a spherical morphology with a diameter of less than ۱۰۰ nanometers. The release results showed that the highest release rate was related to EPC liposomes. In the MTT test, it was observed that nanocarriers without tacrolimus drugs do not show any toxic effect on cells.

کلیدواژه ها:

Tacrolimus ، Nanoparticles ، Ophthalmic ، Chitosan ، Hydrogel