低分子肝素pH敏感巯基壳聚糖纳米粒的制备及体外黏膜透过性评价-论文.pdf

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1、低分子肝素pH敏感巯基壳聚糖纳米粒的制备及体外黏膜透过性评价孙川，邢洋，胡华颖，梁云星，范博，梁桂贤(山西医科大学药学院，太原030001)摘要：目的构建低分子肝素pH敏感巯基壳聚糖纳米粒并时其进行表征；考察所构建纳米粒药物的肠黏膜透过作用。方法采用离子交联法制备低分子肝素pH敏感巯基壳聚糖纳米粒，并对其体外特性进行表征；用Franz扩散池考察纳米粒的药物黏膜累积透过量。结果纳米粒形态为类圆球形；平均粒径(329．6±7．3)am，多相分散指数(0．185±0．01)；电势(34．5±2．25)mV；包封率(97．75±0．02)％，栽药量(1

2、2．463±O．003)u·mg-。；在pH1．0介质中24h累积释药：低分子肝素pH敏感巯基壳聚糖纳米粒<巯基壳聚糖纳米粒<药物溶液(P<0．05)；在pH6．8介质中24h累积释药：pH敏感巯基壳聚糖纳米粒、巯基壳聚糖纳米粒均<药物溶液(P<0．05)；体外8h药物肠黏膜累积透过量：pH敏感巯基壳聚糖纳米粒、巯基壳聚糖纳米粒>pH敏感壳聚糖纳米粒>药物溶液(P<0．05)，数值分别为(7．23±0．21)、(6．99±0．79)、(5．62±0．22)、(3．88±0．76)u·cm～。结论所构建的低分子肝素pH敏感巯基壳聚糖纳米粒包封率高

3、、粒径分布均匀，能增加低分子肝素肠黏膜透过率近1倍。关键词：低分子肝素；pH敏感；巯基壳聚糖；纳米粒；黏膜透过doi：10．11669／cpj．2014．16．012中图分类号：R944文献标志码：A文章编号：1001—2494(2014)16—1414—06Preparationand／nvitroMucosalPenetrationEvaluationofpH-SensitiveThiolatedChitosanNanoparticlesforLowMolecularWeightHeparinDeliverySUNChuan，XINGYan

4、g，HUHua—ying，LIANGYun—xing，FANBo，LIANGGui—xian(DepartmentofPharmaceutics，SchoolofPharmaceuticalScience，ShanxiMedicalUniversity，Taiyuan030001，China)ABSTRACT：OBJECTIVETodeveloppH—sensitivethiolatedehitosannanoparticlesandevaluatethemucosalpermeationeffectofthenanoparticlesforl

5、owmolecularweightheparin．METHODSThepH—sensitivethiolatedchitosannanoparticleswerepreparedbyioniccross—linkingreactionandcharacterizedfortheshape，particlesize，Zetapotential，drugentrapmenteficiencyandloadingcapacity．／nvitroreleaseoflowmolecularweightheparinfromthepreparednanop

6、articleswasevaluatedin0．1mol·L一‘HC1solutionandphosphatebufferedsaline(PBS)atpH6．8usingthedialysismethod．TheintestinalpermeabilitywasestimatedutilizingFranzdiffusioncellsys—tem．RESULTSTheobtainednanoparticleswerefoundtobeapproximatelysphericalwiththemeanparticlessizeof(329．64

7、-7．3)nmandapositiveZetapotentialof(34．54-2．25)mV；theentrapmenteficiencyandloadingcapacityoftheNPswere(97．75±0．02)％and(12．463±0．003)u·mg～，respectively．In0．1mol·LHC1solution(pH1．0)thereleaserateoflowmolecularweightheparinwithin24hfromthiolatedchitosannanoparticleswasfasterthan

8、thatfrompH-sensitivethiolatedchitosannanoparticleswithasignificantdifferenc