| BackgroundAt present,the incidence of neovascular eye disease continues keep rising ?Bevacizumab is a monoclonal antibodytherapeutics for the treatment of neovascular eye disease.Due to the existence of various barriers to the eye,dropped routine eye drops alone can not reach the effective concentration in the eye.The current clinical use of vitreous injection of these drugs to treat Intraocular neovascular diseases.At present,vitreous injection are used for the treatment of neovascular retinal choroidal lesions.But multiple vitreous injections may produce some serious complications.Recent studies have shown that the use of Annexin A5 liposomes as a carrier can a great improveof the abilityof bevacizumab through the cornea,which has the potential of become a new noninvasive approach for treat intraocular neovascular.Therefore,the study of the Pharmacokinetics of topically applied bevacizumab with annexin A5-associated liposomes in the rabbit eyes will help the clinical treatment of intraocular neovascular diseases.Objectives In order to reduce the ocular complications and improve the ocular permeability of the local application of the drug,this study preparing a new type of bevacizumab annexin A5 lipid eye drops,applied it in the rabbit eyes and study it'sOcular pharmacokinetics,for rovided experimental basis and theoretical basis to the clinical treatment of retinal vein neovascular disease through.Methods 1.Preparation of drugs: bevacizumab comes from the finished product.Bevacizumab liposomes are made from liposomal microbubbles and bevacizumabs by double hydration.Bevacizumab Annexin A5 liposomes were prepared bybevacizumab liposomes and enzyme A5 by low-speed rotation in a stirrer.2.Experimental animal grouping:105 healthy New Zealand rabbits were divided into experimental group,control group 1,control group 2,35 rats in each group,Each group was randomly divided into 7 subgroups,each subgroup 5,respectively,corresponding to the administration of 7 time points.3.Administration and sample collection:The experimental group of New Zealand white rabbits received bevacizumab resistance Annexin A5 liposome local eye 50?L in monocular;In the control group A,New Zealand rabbits received 50 ?L of bevacizumab liposomes in monocular.The control group B New Zealand white rabbits monocular received 50 ?L bevacizumab in monocular.Observe the anterior segment with a flashlight after administration.Animals were sacrificed at different time points after administration,and the eyeballs were taken from the aqueous humor and the vitreous and retinal choroidal specimens,took off the eyeballs,get aqueous humor and vitreous,retinal choroidal specimens,Ready for use.4.Obtain pharmacokinetic parameters and statistical data:The concentration of each sample was calculated by enzyme-linked immunosorbent assay.DAS 2.1.1 software was used to calculate the pharmacokinetic parameters of each drug,and the curve was fitted.SPSS 19.0 software was used for statistical analysis.Statistical analysis was performed by ANOVA and LSD test.Results1.The concentrations of allotropeptide Annexin A5 liposomes were significantly higher than those of control group 1 and control group 2 at each measured time point(P<0.05).2.Bevacizumab in the retinal choroidal tissue of experimental group has a higher concentration than the IC50 of bevacizumabin to hVEGF in vitro ConclusionsBevacizumab Annexin A5 liposomes are expected to be a new formulation for thetreatment of Ocular neovascular disease,which prevents ocular injections and reduces complications by administration mode of topically apply. |
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