Preparation Of Thermosensitive In Situ Gel Containing Moxifloxacin Hydrochloride Chitosan Nanoparticle For Ophthalmic Use

Objective::Eye drops and oculentum are the traditional eye medication dosage form,however their disadvantages are short treating time,low bioavailability,repeated administration,and blurred vision which leads to poor patient compliance.with the development of biopharmaceutics and ocular drug pharmacokinetics research,the new ocular drug delivery system(NODS)has become an advanced research hotspot.Among which the nanoparticle system and the situ gel system received widespread attention for their low toxicity,obviously sustained-release and controlled-release effect,perfect biodegradability and biocompatibility.In this paper,we have designed a preparation of thermosensitive in Situ Gel Containing Moxifloxacin Hydrochloride Chitosan Nanoparticle for Ophthalmic Use.Methods:This thesis contains three parts of methods.The first part is the preparation of drug-loading nanoparticles.We adopt Ionic crosslinking method to prepare nanoparticles,using chitosan(CTS)and sodium tripolyphosphate(TPP)as materials,and moxifloxacin hydrochloride as the model drug.Nanoparticle size is our main evaluation index and we investigate the factors affecting the preparation of nanoparticle,determine the optimal preparation technology.Secondly,we invest the properties of drug-loading nanoparticles from the nanoparticle size,morphology,drug-oading,encapsulation efficiency,etc.The third part is to design the temperature sensitive in situ gel formulation and nanoparticles in situ gel in vitro release test.Poloxamer407 and poloxamer188 were chosen as temperature sensitive in situ gel and set up different concentration ratio of prescription.In addition,we observed the tempreture in different composition of poloxamer.Results: The SEM image demonstrated that the NPs were well separated into individual particles with normal shape.The diameter of mean was 207.2±6.9nm(PDI=0.157±0.030)and the zeta potencial was 32.1±1.5 mV.The entrapment efficiency was 41.6%±1.7%.The best percentage of P407 and P188 was 20% and 5%.The releasing curve of the thermosensitive in situ gel chitosan nanoparticle showed that there was no phenomenon of sudden release and the sustained-release effect was the most obvious.The nanoparticles' particle diameter between 100 to 300 nm with good spherical shape ?The best percentage of P407 and P188 was 20% and 5%.This is the first study to prepare thermosensitive in situ gel containing moxifloxacin hydrochloride chitosan nanoparticle for ophthalmic use.This study combines the advantages of nanoscopic drug carrier and in situ gel,which could make the bioavailability more effective and decrease the side effect of drug and increase the patients' compliance.It has some reference value of the development and application for new ocular drug delivery system.