Preparation Of Florfenicol Gelatin Nanoparticles And Its Preliminary Evaluation

Flufenicol is a kind of veterinary antibiotic of chloramphenicol.It has the advantages of broad spectrum,safety and high efficiency,which is widely used in veterinary clinic.However,florfenicol has some problems,such as poor water solubility,inconvenient medication and low bioavailability.From the point of pharmaceutics,flufenicol gelatin nanoparticles were prepared by using nano technology.Gelatin,which was cheap,safe and degradable,was selected in order to achieve high efficiency,sustained release,safety,less toxic and side effects,high bioavailability and biocompatibility,and reduce production costs.In this paper,the preparation technology of flufenicol-gelatin nanodrug was explored.The factors influencing the quality of flufenicol nanodrug,such as gelatin dosage,acetone dosage and flufenicol concentration,were screened.The optimal preparation process was optimized by investigating the particle size,encapsulation efficiency,drug loading and release of flufenicol nano-drug.Ultraviolet spectroscopy,infrared spectroscopy,transmission electron microscopy and laser particle size analysis were used to characterize the hydrogen bonding effect,morphology and particle size,and high performance liquid chromatography was used to analyze the encapsulation efficiency,drug loading and in vitro release.The relative toxicity,in vivo metabolic kinetics and relative bioavailability of commercial injections were investigated by MTT assay,pathological section analysis and liquid chromatography-mass spectrometry?LC-MS?with porcine pulmonary macrophages and mice as control.The optimum preparation conditions of nano-drug were determined as follows:the initial concentration of gelatin was 10%,the amount of solution and acetone was 1:1.5,and the concentration of florfenicol was 10%of the amount of gelatin.The average particle size of the prepared nano-drug was about 280 nm,encapsulation efficiency was 90%,drug loading was9%.In vitro release experiments showed that the total release rate of the nano-drug reached86.5%within 144 hours.MTT assay showed that the cytotoxicity of the self-made nano-drug was significantly lower than that of the commercial florfenicol injection.Pathological sections showed that the damage of mice tissues was lower than that of the commercial florfenicol injection.Compared with florfenicol injection,the peak time of nano-drug was lagged to 12hours,and the highest blood concentration of nano-drug was only 55%of that of commercial injection.However,there was a significant slow metabolic phenomenon,t_1/2/2 reached 48 hours,after 120 hours,it could still maintain the highest blood concentration of 10%,relative utilization reached 141%,which had a good sustained release effect.To optimize the preparation process of florfenicol gelatin nanoparticles.A method for the determination of florfenicol gelatin nanoparticles by high performance liquid chromatography was established.Flufenicol gelatin nanoparticles with uniform particle size distribution,high encapsulation efficiency and drug loading were prepared.The results of pharmacokinetics and relative bioavailability preliminarily showed that nano-drug still had a good sustained release effect in mice,which could ensure that florfenicol was in a relatively stable blood concentration range for a long time,reduce the peak and valley phenomena of commercial injection,and reduce the toxic and side effects caused by drug dosage.It improves the bioavailability,reduces the total dosage,and provides data for the determination of dosage and frequency of follow-up clinical medication.