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1、環(huán)孢素A眼用納米脂質(zhì)載體的制備及表征肖衍宇，鮑曉，沈潔，平其能，陳志鵬(1．中國(guó)藥科大學(xué)藥劑學(xué)教研室，南京210009；2．南京中醫(yī)藥大學(xué)藥劑教研室，南京210046)摘要：目的制備適于眼部給藥的環(huán)孢素A納米脂質(zhì)載體(cyclosporineA—loadednanostructuredlipidcarriers，CsA—NLC)，并考察其理化性質(zhì)和眼局部刺激性。方法采用熔融一乳化法制備CsA—NLC，通過正交實(shí)驗(yàn)篩選出最優(yōu)處方。考察CsA—NLC的粒徑、形態(tài)，包封率、栽藥量及在人工淚液中的釋藥行為，采用差示掃描量熱法(differentialscanningcalorimetry

2、，DSC)確證CsA在載體中的分散狀態(tài)，利用家免研究其眼局部刺激性。結(jié)果優(yōu)化條件下制備的CsA—NLC多為類球形粒子，平均粒徑(35．9±0．21)nm，Zeta電位(一13．9±0．21)mV，包封率、載藥量分別為(97．5±0．58)％和(16．2-4-0．09)mg·mL～。DSC表明藥物以非結(jié)晶狀分散于納米粒中。CsA—NLC具有明顯的緩釋特征，其體外釋藥行為符合單指數(shù)模型。CsA—NLC對(duì)家兔眼部無刺激性。結(jié)論制備的CsA—NLC粒徑小，載藥量高，刺激性小，體外釋放具有明顯的緩釋特征，有望實(shí)現(xiàn)藥物眼部控釋遞送，提高藥物的眼用生物利用度。關(guān)鍵詞：環(huán)孢素A；納米脂質(zhì)栽體；眼

3、部遞藥系統(tǒng)；制備；理化性質(zhì)；眼局部刺激性中圖分類號(hào)：R944文獻(xiàn)標(biāo)志碼：A文章編號(hào)：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