Formulation and development of Liposomal tacrolimus for treatment of various ocular diseases

Zahra Alimohammadi, Azadeh Abreshteh, Zohreh Ebrahimi, Seyedehmohadeseh Hosseini, Mehrsa edalat

Liposome, Tacrolimus, sustained released, ocular therapy, Corneal graft.

Corneal transplantation is one of the most successful tissue/organ transplant procedures. While approximately 40,000 are performed each year. Tacrolimus (FK 506) is a potent macrolide lactone immunosuppressive agent that exhibit excellent therapeutic efficacy in suppressing abnormal immune responses and prevention of rejection in transplantation. In spite of its success in ensuring graft survival, therapeutic use of tacrolimus is restricted due to its narrow therapeutic index and a poor oral bioavailability because of its poor solubility and liver first pass effect. The purpose of this study was to develop tacrolimus encapsulated liposomes, to optimize the loading efficiency and to achieve a sustained release profile.

Tacrolimus encapsulated liposomes were prepared by thin film hydration method, and extruded to large unilamellar vesicles (LUVs) with mean particle size (Z ave~ 100 nm) by high-pressure extrusion technique. Drug loading efficiencies (78 - 98%) achieved with high final drug/lipid ratio. the effects of liposomal structure and drug/ lipid ratio have been investigated on the loading efficiency. Developed formulations were found to have in vitro sustained drug release up to 14days. furthermore, the stability of liposome in size and shape was confirm for at least one month. The investigation provides a practical approach for direct delivery of tacrolimus encapsulated in liposomes for controlled and prolonged retention at the site of action.

https://dx.doi.org/10.31873/IJEAS.11.01.01