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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
資料類型: PDF文件
關(guān)鍵詞: compressed  c02  poly-l-iactide  porous  microspheres  pulmonary  drug  
delivery  
資料大小: 105K
所屬學(xué)科: 分子表征
來(lái)源: 第六屆亞歐研討會(huì)上處理和性能增強(qiáng)聚合物會(huì)議文集(2013.6.2-6 武漢)
簡(jiǎn)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.
作者: A. Chen, C. Zhao, S. Wang, Y. Liu
上傳時(shí)間: 2013-06-28 17:09:05
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