环孢素A眼用纳米脂质载体的制备及表征.pdf

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1、环孢素A眼用纳米脂质载体的制备及表征肖衍宇，鲍晓，沈洁，平其能，陈志鹏(1．中国药科大学药剂学教研室，南京210009；2．南京中医药大学药剂教研室，南京210046)摘要：目的制备适于眼部给药的环孢素A纳米脂质载体(cyclosporineA—loadednanostructuredlipidcarriers，CsA—NLC)，并考察其理化性质和眼局部刺激性。方法采用熔融一乳化法制备CsA—NLC，通过正交实验筛选出最优处方。考察CsA—NLC的粒径、形态，包封率、栽药量及在人工泪液中的释药行为，采用差示扫描量热法(differentialscanningcalorimetry

2、，DSC)确证CsA在载体中的分散状态，利用家免研究其眼局部刺激性。结果优化条件下制备的CsA—NLC多为类球形粒子，平均粒径(35．9±0．21)nm，Zeta电位(一13．9±0．21)mV，包封率、载药量分别为(97．5±0．58)％和(16．2-4-0．09)mg·mL～。DSC表明药物以非结晶状分散于纳米粒中。CsA—NLC具有明显的缓释特征，其体外释药行为符合单指数模型。CsA—NLC对家兔眼部无刺激性。结论制备的CsA—NLC粒径小，载药量高，刺激性小，体外释放具有明显的缓释特征，有望实现药物眼部控释递送，提高药物的眼用生物利用度。关键词：环孢素A；纳米脂质栽体；眼

3、部递药系统；制备；理化性质；眼局部刺激性中图分类号：R944文献标志码：A文章编号：1001—2494(2012)05—0362—05PreparationandinVitroCharacterizationsofCyclosporineAOcularNanostructuredLipidCarriersXIAOYan—yu’，BAOXiao，SHENJie，PINGQi．neng，CHENZhi．peng(1．DepartmentofPharmaceutics，Chin0PharmaceuticalUniversity，Nanjing210009，China；2．Departm

4、entofPharmacy，№ngUniversityofTraditionalChineseMedicine，ng210046，China)ABSTRACT：OBJECTIVETodevelopanappropriatenanostructuredlipidcarrier(CsA—NLC)foroculardrugdeliveryofcyclospo—rineAanditsinvitrophysicochemicalpropertiesandocularirritationstudieswereinvestigated．METHODSThemelt—emulsification

5、methodwaschosentoprepareCsA—NLC．Theformulationwasoptimizedbyorthogonaldesign．ThemorphologyofCsA—NLCwasob—servedbytransmissionelectronmicroscopy(TEM)．ThemeanparticlesizeandZetapotentialweremeasuredbylaserparticlesizeana—lyzer．ThestateofdruginNLCwasconfirmedbyDSC．Drugloadingandencapsulationefic

6、iencyweredeterminedbyHPLC．Dialysismethodat34℃wasemployedtoinvestigatetheinvitroreleaseofCsA—NLC．ThetopicalocularirritationstudyofCsA—NLCwasmadeinrabbits．RESULTSTheobtainedCsA—NLCwasapproximatelysphericalinshapewithaverageparticlesizeof(35．9±0．21)timandzetapotentialof(一13．9±0．21)mV．Thedrugload

7、ingandencapsulationeficiencywere(16．2±0．09)％and(97．5±0．58)％，respectively．TheinvitroreleaseofCsA—NLCwassloweddownandfittedwellsingleexponentialdistributionmode1．TherewasnoiritationforCsA—NLCtorabbitseye．CONCLUSIONCsA—NLCwithsmallparticlesizesa