Preparation of Drug-Ioaded Porous Poly-L-Iactide Microspheres Using Compressed C02 Antisolvent Process，第六届亚欧研讨会上处理和性能增强聚合物会议文集（2013.6.2-6 武汉）-中国聚合物网,论文下载

Preparation of Drug-Ioaded Porous Poly-L-Iactide Microspheres Using Compressed C02 Antisolvent Process

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compressed c02 poly-l-iactide porous microspheres pulmonary drug
delivery

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分子表征

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第六届亚欧研讨会上处理和性能增强聚合物会议文集（2013.6.2-6 武汉）

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.

作者：

A. Chen, C. Zhao, S. Wang, Y. Liu

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2013-06-28 17:09:05

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