Design, Characterization, and Cytotoxic Evaluation of Tacrolimus Encapsulated Nanoliposomes
Maryam Malakouti Nejad1 , Dina Morshedi 1 *, Hassan Bardania 2 , Alireza Baradaran-Rafii 3
- Bioprocess Engineering Department, Institute of Industrial and Environmental Biotechnology, National Institute of Genetic Engineering and Biotechnology, Tehran, Iran
- Clinical Research Development Unit, Imamsajad Hospital, Yasuj University of Medical Sciences, Yasuj, Iran
- Ocular Tissue Engineering Research Center, Shahid Beheshti University of Medical Sciences, No 23, Paydarfard-9th Boostan St., Pasdaran Ave, Tehran, Iran
Abstract: Tacrolimus (FK506) is a hydrophobic immunosuppressive agent especially against T lymphocytes proliferation and immune responses, so it has been widely applied after transplantation surgeries such as corneal transplantation. However, the conventional pharmaceutical formulation of tacrolimus limits its applications in ocular therapy. To overcome the drawbacks, we recruited nanoliposomes due to their low immunogenicity and great biocompatibility, particularly for ocular diseases.
Methods: The fabricated nanoliposomes containing tacrolimus (NLP-TAC) were prepared via the dehydration-rehydration method. After homohomogenizing the size of nanoliposomes by mini extruder, the final formulated nanoliposomes were characterized using DLS and TEM in terms of size, zeta potential, and polydispersity index (PDI). The drug release from nanoliposomes was assessed by dialysis technique and HPLC. Furthermore, to evaluate the effect of NLP-TAC on adult retinal pigment epithelial cells (ARPE19), cell proliferation was determined by using the cell viability assay. Hemocompatibility of the formulation was evaluated on the blood agar plates.
Results: The developed NLP-TAC showed the size of 169/36±4/21 nm, PI < 0.49, with zeta potential around 0 mV, with an entrapment efficiency of 90/42%±12/21. 79/08% of tacrolimus was released from the NLP-TAC in the presence of tween 20 (0.25%) during 11 days. The release index showed a slow and sustained manner. NLP-TAC was not cytotoxic with no sign of hemolysis on the blood cells.
Conclusion: Our results showed that the formulated NLP-TAC was safe and non-toxic and could be a promising candidate for ocular delivery of tacrolimus.
