Preparation and evaluation of a novel biodegradable long‐acting intravitreal implant containing ligustrazine for the treatment of proliferative vitreoretinopathy. (31st December 2014) - Zhang, Xuemei
Abstract Objectives It is challenging to deliver the therapeutic drug effectively to the posterior ocular disease location with optimized exposure and long‐term effects when treating proliferative vitreoretinopathy (PVR). The objective of this study is to develop a novel biodegradable and long‐acting ocular implant for PVR therapy with ligustrazine as the active ingredient. Methods The ligustrazine implants were prepared with poly(DL‐lactide‐co‐glycolide) using a hot‐melting extrusion. The physicochemical properties of the implants were characterized. The effectiveness of the selected ligustrazine implants was evaluated in a PVR rabbit model. Furthermore, the in‐vitro drug release profile and pharmacokinetics were compared, and in‐vitro/in‐vivo correlations were evaluated. Key findings The optimal implants had an ideal zero‐order in‐vitro drug release profile, which was correlated with the in‐vivo drug absorption fraction in the vitreous bodies of the rabbits. The sustained‐release ligustrazine implants significantly reduced the development of PVR in the animal model. Conclusions Ligustrazine implants can be used to treat posterior ocular disease in rabbit animal models, and it provides more choices for medical research on posterior ocular disease.