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Preparation of Drug-Ioaded Porous Poly-L-Iactide Microspheres Using Compressed C02 Antisolvent Process  
Preparation of Drug-Ioaded Porous Poly-L-Iactide Microspheres Using Compressed C02 Antisolvent Process
资料类型: PDF文件
关键词: Compressed  C02  Poly-L-Iactide  Porous  microspheres  Pulmonary  drug  
delivery  
资料大小: 77K
所属学科: 通用高分子材料
来源: 来源网络
简介:
Byvirtueofexcellentaerodynamicproperties,porousmicrospheres(PMs)havebeenconsideredasaneffectiveinhalabledrugcarrier.Comparedwithtraditionalmethods,supercriticalC02fluidtechnologieshaveshowngreatadvantagesinpreparingPMscl].However,thesizeandporosityoftheresultingPMsusuallycouldnotsimultaneouslymeettherequirementsofpulmonarydrugdelivery.Inourstudy,ammoniumbicarbonate(AB)wasusedasaporogen,poly-L-lactide(PLLA)baseddrug-loadedPMsdevelopedbyanemulsion-combinedC02antisolventprocess.Awater-in-oilemulsion,includingPLLAsolutionindichloromethane(DCM)astheoilphaseandABaqueoussolutionasthewaterphase,wasfirstpreparedbyultrasonication.ThenthecompressedC02at8MPaand300CwasutilizedasanantisolventtoremoveDCMfromthesprayeddroplets,thusprecipitatingPLLAmicrosphereswhichcontainedmicrodropletsofABsolution.PLLAPMswerefinallyobtainedbyvacuumdrying.Takingmethotrexate(MTX)andlysozymeasthesmall-moleculeandbiomacromoleculemodeldrugsrespectively,drug-loadedPLLAPMscouldalsobefabricatedusingthementionedmethod.Theproductsallexhibitedhighlyporousmorphology,withgeometricmeandiameter(Dg)of5-25ym,aerodynamicdiameter(Da)lessthan4.7ym,andporositymorethan70%.Thedrugswereuniformlydispersedinthematrixandtheencapsulationefficienciesofbothdrugswerewithintherangeof50%一80%,withnoburstrelease.FouriertransforminfraredspectroscopyandinvestigationofvitroantitumorefficacyalsorevealedthatboththestructureandfunctionofMTXwerewellmaintainedaftertheloadingprocess;circulardichroismspectrumandenzymaticactivitymeasurementsalsoindicatedthatenvironmental-sensitivebiomacromoleculescouldalsobewellloadedbytheprocess.Theresultsdemonstratethattheprocessusedinthisstudywouldbeapromisingmethodforproducingdrug-loadedPMsforpulmonarydrugdelivery.
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