Study On Preparation Of HCPT-chitosan Nanoparticles Targeted Folate

The research of camptothecin derivatives new formulation has showed favourable development prospect at home and abroad in recent years.At present,research emphasis mostly centralizes the study of targeting preparation,but it is far from reaching target medication in a real sense.Moreover,these researches must become main direction of tumor therapy.Folate receptor is deemed to be a preferable tumor marker.It is developed as marker of clinic diagnosis tumor at present.Chitosan is a excellent natural polymers.It has biodegradable property,biological adhesive and has no immunization with flesh.Because of these excellences,it can be as drug carrier system of targeting delivery while binding to folate.This text adopted SAS method to prepare HCPT nanoparticles.Because of the insoluble of HCPT in supercritical CO₂ and low critical temperature,innocuity,apyrous and low price of CO₂,this work used CO₂ as supercritical fluid and dimethyl sulfoxide(DMSO) as the solvent and the SAS method was used to prepare the HCPT ultrafine powder.It contained as follows:The range of particle size of HCPT nanoparticles using SAS method to prepare were less than 200nm.Besides,using the methods of LC/MS,FT-IR,XRD and DSC to prove,the HCPT nanoparticles after SAS process were taked on amorphous form and no solvent residue.The main purpose of this work was to prepare the slow-release drug nanoparticles having target therapeutic effect and without residual solvent,namely HCPT-chitosan nanoparticles targeted folate.Its preparation process as follows firstly,the activated folate ester.composed by folate and chitosan created folate-coupled chitosan.Under acidic condition,this conjugate acceding to sodium polyphosphate solution crosslinked,polymerized and enveloped HCPT nanoparticles made from supercritical anti-solvent processes to generate target nanoparticles.Via response value namely drug loading,entrapment efficiency,yield rate and particle size,this article also used Design-Expert 7.0 experimental design software to analyse the influencing factors(the concentration of folate-coupled chitosan and TPP,HCPT addition amount and the reaction time) from preparation process of HCPT-chitosan nanoparticles targeted folate educe each optimal process condition and the synthesis optimal process condition.The results indicated that:Under process condition:the concentration of folate-coupled chitosan and TPP were 2.00mg/mL and 7.75 mg/mL,respectively;the quality of HCPT nanoparticles was 8.24mg;the reaction time was 47.5min,the entrapment efficiency,drug loading,yield rate,and particle size of HCPT-chitosan nanoparticles targeted folate simultaneously reaching a systematically optimize result were 87.96%,72.78%,33.02%and 353.6nm,respectively.The preparation method of targeted nanoparticles used in this study offers experimental basis for the preparation of other materials.HCPT-chitosan nanoparticles targeted folate also offer effective research foundation for medication study in vitro and vivo hereafter.