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1.
肝靶向氟尿嘧啶类脂纳米粒的研究   总被引:31,自引:0,他引:31  
目的 为了提高氟尿嘧啶(5-Fu)的疗效,降低其毒副作用,制备具肝靶向的5-Fu类脂纳米粒。方法 利用氟尿嘧啶与硬脂酰氯进行反应,制备了5-Fu前体药物N1-硬脂酰-5-Fu,通过红外光谱及核磁共振谱对合成的目标化合物进行结构确认。同时研究了前体药物的性质及稳定性。采用物理凝聚法制备类脂纳米粒,并研究其形态、粒径及粒径分布、载药量、体外释药特征、动物体内分布与药代动力学参数等。结果 平均粒径dav=240.19 nm,载药量为20.53%。体外释药速率符合一级动力学模型。与5-Fu水针剂比较,类脂纳米粒组在肝脏中药物含量平均增加了一倍以上。家兔体内主要药动学参数为:Vc=0.04336 L.kg-1,T1/2β=1.2834 h,CL=0.1632 L.h-1。结论 利用前体药物可提高药物的脂溶性,首次以物理凝聚法制备类脂纳米粒,小鼠体内分布研究表明类脂纳米粒有明显的肝靶向,有一定的优越性和参考价值。  相似文献   

2.
李志荣 《中国药师》2012,15(2):157-160
摘 要 目的:研究汉黄芩素固体脂质纳米粒在大鼠体内的药动学及组织分布情况。方法: 大鼠随机分成汉黄芩素注射液组和汉黄芩素固体脂质纳米粒组,分别于给药后不同时间采血测定汉黄芩素含量,并测定两组大鼠心、肝、脾、肺、肾中汉黄芩素含量,计算靶向效率以评价其在大鼠体内的组织分布及靶向性。结果:汉黄芩素固体脂质纳米粒在大鼠体内的药动学模型符合二室模型,主要药动学参数为:t1/2α=(0.551 0±0.124 7)h, t1/2β=(14.589 1±1.563 8)h, CL=(0.006 4±0.001 4) ml·h·Kg-1, AUC0→∞=(125.76±9.5728) mg·h·L-1,其在肝脏、脾脏、心脏、肺脏及肾脏的靶向效率分别为2.003、1.789、0.634、0.707、0.259。结论:与汉黄芩素溶液相比,汉黄芩素固体脂质纳米粒能提高对肝脏、脾脏的趋向性,有利于提高其治疗作用。  相似文献   

3.
蛇床子素在兔体内药物代谢动力学   总被引:9,自引:1,他引:9  
目的研究蛇床子素在兔体内的药物代谢动力学。方法用高效液相色谱法,以丹皮酚为内标,以甲醇-水(80∶20)为流动相,测定兔血液中蛇床子素(iv,10 mg·kg-1)的含量。采用3P87程序计算药物代谢动力学参数。结果蛇床子素iv药代动力学符合二房室开放模型,T1/2α=5.81 min,T1/2β=42.2 min,K21=0.036 0·min-1,K12=0.045 0·min-1,K10=0.054 0·min-1,AUC=235 mg·min·L-1,CLs=0.043 0 L·min-1·kg-1,VC=0.780 L·kg-1。结论蛇床子素在兔体内分布及消除较快  相似文献   

4.
目的:建立大鼠血浆中水黄皮素的定量分析方法,并对其药代动力学进行研究。方法:通过灌胃给予SD大鼠水黄皮素(10 mg·kg-1),血浆样品经蛋白沉淀法处理后进行HPLC-MS/MS定量分析,以五味子醇甲为内标,采用Agilent Poroshell 120 EC-C18(50 mm×3.0 mm,2.7 μm)色谱柱,乙腈(A)-0.1%甲酸溶液(B)为流动相,流速0.3 mL·min-1,梯度洗脱;采用电喷雾离子源(ESI),正离子多反应监测模式(MRM)扫描,水黄皮素[M+H]+ m/z 293.1→277.0,五味子醇甲[M+H]+ m/z433.2→384.2;使用DAS软件计算相关药代动力学参数。结果:在1.5625~1600 ng·mL-1浓度范围内,水黄皮素线性关系良好(r=0.9997),定量下限为1.5625 ng·mL-1,精密度RSD和准确度RE均小于20%;低、中、高质控样品精密度RSD和准确度RE均小于15%,提取回收率在91.70%~100.28%,基质效应在88.35%~97.55%,稳定性RSD均小于15%。水黄皮素在雌性SD大鼠体内Tmax、t1/2、Cmax和AUC0→t分别为3 h、1.95 h、1214.85 ng·mL-1和11920.43 ng·mL-1·h;在雄性SD大鼠体内Tmax、t1/2、Cmax和AUC0→t分别为3 h、1.19 h、1221.57 ng·mL-1和9983.40 ng·mL-1·h。结论:所建方法符合生物样品定量分析的基本要求,可用于水黄皮素在大鼠血浆中的含量测定及其药代动力学评价;水黄皮素在雌性SD大鼠体内的生物利用度更高。  相似文献   

5.
泻心汤黄酮类成分在大鼠体内的药代动力学研究   总被引:3,自引:1,他引:3  
研究泻心汤中黄酮类成分在大鼠体内药代动力学规律。大鼠灌胃给予泻心汤12 g·kg-1,给药前及给药后不同时间采集血样或尿样,HPLC法测定黄酮类成分浓度,血药浓度-时间数据和尿药排泄量-时间数据用DAS软件进行动力学分析。采用大鼠肾匀浆温孵法,进行黄芩苷的体外代谢研究。结果显示,黄芩苷、汉黄芩苷血药浓度迅速达峰,药时曲线呈现双峰现象,消除T1/2均为6 h左右;黄芩苷、汉黄芩苷、黄芩素、汉黄芩素在尿中均有排泄,尿中排泄量占给药量均<10%,尿排泄T1/2在6~8 h;大鼠肾匀浆可将黄芩苷代谢生成黄芩素,酶动力学参数Vmax=702 nmol·min-1·g-1(protein),Km=135 μmol·L-1。可见,泻心汤中黄酮类成分可迅速吸收进入体内;黄芩苷、汉黄芩苷、黄芩素、汉黄芩素均可从尿排泄,但尿药排泄量较少;肾脏可将黄芩苷代谢成黄芩素。  相似文献   

6.
目的 采用与静脉注射对比的方式,研究聚乙二醇-聚乳酸-α-细辛脑纳米粒(PEG-PLA-α-细辛脑纳米粒)鼻腔给药后在大鼠体内的药物动力学。方法 以大鼠为动物模型,采用血药动力学、脑药动力学及荧光标记法对比研究PEG-PLA-α-细辛脑纳米粒经鼻腔给药与静脉注射后药物/纳米粒在大鼠体内的分布情况。结果 PEG-PLA-α-细辛脑纳米粒静脉注射及鼻腔给药后血浆中的AUC(0-∞)分别为(11032.4±1 827.1)ng·mL-1·min及(5 992.9±717.5)ng·mL-1·min,Cmax分别为(421.9±100.2)ng·mL-1及(171.7±26.3)ng·mL-1,PEG-PLA-α-细辛脑纳米粒鼻腔给药后的绝对生物利用度F为54.3%。PEG-PLA-α-细辛脑纳米粒静脉注射后α-细辛脑在脑组织中的Cmax与鼻腔给药后α-细辛脑在脑组织中的浓度Cmax分别为(217.9±29.9)ng·mL-1及(334.2±62.7)ng·mL-1,PEG-PLA-α-细辛脑纳米粒静脉注射与鼻腔给药后的AUCbrain/AUCplasma值分别为1.37和2.85,且两者具有统计学意义。PEG-PLA-α-细辛脑纳米粒鼻腔给药后的药物脑靶向效率及鼻-脑传递百分比分别为208.03%及52.01%。荧光标记法结果显示,PEG-PLA-α-细辛脑纳米粒鼻腔给药后脑靶向性比静脉注射后更强。结论 PEG-PLA-α-细辛脑纳米粒适合于鼻腔给药治疗脑部疾病。  相似文献   

7.
雷公藤内酯醇在Beagle犬体内的药代动力学   总被引:6,自引:0,他引:6  
雷公藤内酯醇(triptolide,TP)是雷公藤的主要有效成分之一。研究不同剂量TP在Beagle犬灌胃给药时的绝对生物利用度和药代动力学, 可望为其临床研究提供参考。以泼尼松龙作内标, 用乙酸乙酯液液萃取, 建立LC-APCI/MS选择性离子监测方法测定血浆TP浓度。Beagle犬分别静脉注射TP 0.05 mg·kg-1、 灌胃TP 0.05,0.08和0.1 mg·kg-1进行药代动力学和绝对生物利用度研究。结果表明, TP在1~200 ng·mL-1呈良好线性关系(r=0.999 7),批内和批间精密度RSD均小于10%,准确度在95.0%~105.0%,提取回收率大于75%。静注0.05 mg·kg-1 TP后,T1/2β为(2.5±0.8) h。3个剂量灌胃组,TmaxT1/2αT1/2β,经检验无统计学差异。AUC和Cmax与剂量之间线性相关。灌胃0.05 mg·kg-1后,TP在Beagle犬体内绝对生物利用度为(75±17)%。可见,LC-APCI/MS法灵敏、可靠、专属性强,可用来测定Beagle犬血浆TP的浓度;TP在Beagle犬体内消除较快,灌胃给药生物利用度较高。  相似文献   

8.
番茄红素微囊的体内外药剂学行为   总被引:5,自引:1,他引:5  
目的考察番茄红素微囊的体外释放、番茄红素原料及番茄红素微囊在家犬体内的药代动力学、体外释放和体内吸收的相关性。方法用分光光度法测定释放介质中番茄红素的含量。用HPLC法测定家犬体内的番茄红素含量,数据用3P87程序处理,得到各主要药代动力学参数。体内吸收与体外释放进行点点相关。结果微囊体外释放呈肠溶性,原料及番茄红素微囊的T1/2α分别为7.30和15.06 h;T1/2β分别为28.10和46.76 h;Tmax分别为22.32和41.03 h;AUC0-∞分别为1.67和2.08 μg·h·L-1。体内外相关性良好。结论微囊较原料药呈现缓释特征,体内外相关性结果表明可以根据体外释放情况预测体内的吸收。  相似文献   

9.
肝靶向米托蒽醌白蛋白微球的研究   总被引:15,自引:0,他引:15  
用乳化—热固化法制备了米托蒽醌白蛋白微球,并对其形态、大小及其分布、微粉学性质、载药性能、体外释药、稳定性和体内分布进行了研究。结果表明,该载药微球的平均算术径为0.99μm,平均表面径为1.24μm,平均容积径为1.44μm;表观载药量为2.558%±0.101%;有效载药量为1.503%±0.127%;包封率为92.82%±4.60%;体外释药符合双相动力学规律,释药方程为1-Q=0.6428e-0.2132t+0.3988e-000150t(γ1=-0.9951,γ2=-0.9982);T1/2α=3.250h,T1/2β=461.7h;室温放置3个月,微球形态、药物含量等均无明显变化。HPLC测定表明,小鼠尾iv该微球20min内即有77.6%±1.38%的药物浓集于肝脏,具有明显的肝靶向性。提示米托蒽醌白蛋白微球有可能提高米托蒽醌的抗肝癌效果和降低其全身毒副作用。  相似文献   

10.
诺氟沙星注射剂和胶囊剂的人体药代动力学   总被引:1,自引:0,他引:1  
栾立标  朱家壁 《药学学报》2000,35(2):147-150
目的:考察自制的肌注诺氟沙星注射剂在体内的动态行为,并与诺氟沙星胶囊剂进行比较。方法:用HPLC法测定这两种制剂在人体的血药浓度,并用非线性最小二乘法迭代程序进行数据处理。结果:注射剂在体内的过程可用开放型二室模型描述,其主要体内参数为:AUC=5.84 h.μg.mL-1,Tmax=0.35 h,Cmax=1.14 μg.mL-1,MRT=7.32 h;而胶囊剂则符合一室模型,主要体内参数为:AUC=4.29 h.μg.mL-1,Tmax=1.28 h,Cmax=0.72 μg.mL-1,MRT=6.16 h。结论:注射剂较胶囊剂生物利用度高,起效快,峰浓度高,作用持久。  相似文献   

11.
紫杉醇长循环固态脂质纳米粒的制备和体内外研究   总被引:32,自引:0,他引:32  
目的以硬脂酸为载体材料制备紫杉醇的长循环脂质纳米粒,并考察其体内外性质。方法用“乳化蒸发-低温固化”法制备Brij78固态脂质纳米粒(Brij78-SLN)和Poluromic F68固态脂质纳米粒(F68-SLN);用透射电镜考察了紫杉醇纳米粒的形态;建立了脂质纳米粒和血清中测定紫杉醇的HPLC方法;考察了纳米粒于30%乙醇溶液中的体外药物释放;以市售紫杉醇注射剂对照,测定了两种纳米粒于小鼠体内的药物动力学参数。结果脂质纳米粒基本呈圆球状或椭圆球状,大小比较均匀。激光散射法测定Brij78-SLN粒径为(104±29) nm。F68-SLN粒径为(220±98) nm。Brij78-SLN和F68-SLN包封率分别为47%和75%。两种纳米粒都缓慢地释放药物,24 h后分别释放药物总量的8%和20%。两种纳米粒都可以延长紫杉醇的体内滞留时间,Brij78-SLN,F68-SLN和紫杉醇注射剂的消除半衰期分别为4.88,10.06和1.36 h。结论硬脂酸纳米粒可能成为一种新型的药物载体。  相似文献   

12.
目的:制备延胡索乙素固体脂质纳米粒缓释片,并研究延胡索乙素固体脂质纳米粒缓释片的释药模型和释药机理。方法:乳化-溶剂挥发法制备延胡索乙素固体脂质纳米粒,以乳糖作为冻干剂,羟丙基甲基纤维素(HPMC)为缓释材料进一步制备缓释片。在单因素考察的基础上,设计正交试验优化延胡索乙素固体脂质纳米粒缓释片处方,并对缓释片体外释药模型和释药机理进行探讨。结果:延胡索乙素固体脂质纳米粒缓释片最佳处方为缓释材料HPMC K4M和HPMC K15M比例为1:1,用量为40 mg,PEG 4000的用量为20 mg,硬脂酸镁用量为片芯质量的0.5%。延胡索乙素固体脂质纳米粒缓释片最佳处方的体外释放行为符合Higuchi释药模型,释药方程为:Mt/M=0.286 8 t1/2-0.073 8(r=0.990 8),12 h内累积释放度为93.56%,缓释片释药机理为扩散和溶蚀共存。结论:制备的延胡索乙素固体脂质纳米粒缓释片,工艺重复性较好,其释药行为符合Higuchi释药模型。  相似文献   

13.
To enhance the liver targeting and reduce the side effects of 5-fluorouracil (5-Fu), it was acylated by stearyl chloride to obtain N1-stearyl-5-Fu (5-FuS). The chemical structure of the prodrug was confirmed by Nuclear Magnetic Resonance and Infrared Spectrometry. 5-FuS was incorporated into solid lipid nanoparticles (SLN), which were prepared by the physical agglomeration method. The mean diameter of 5-FuS-SLN was 240.19 nm and the drug loading was 20.53%. The release characteristics in vitro of 5-FuS-SLN were fitted to the first-order pharmacokinetic model. Compared with 5-Fu injection, a study on the distribution of 5-FuS-SLN in mice showed that 5-FuS-SLN could double 5-Fu concentration in mice livers. The main pharmacokinetic parameters of 5-FuS-SLN in rabbits is shown as follows: Vd=0.04336 L/kg, T(1/2) beta=1.2834 h, CL=0.1632 L/h. In conclusion, 5-FuS-SLN has significant liver targeting properties. The employment of a prodrug to enhance drug liposoluble properties and the preparation method presented in this paper, seem to be an alternative strategy to the traditional colloidal delivery system.  相似文献   

14.
目的:探讨冬凌草甲素对体内外卵巢癌生长的影响及其作用机制。方法:冬凌草甲素作用人卵巢癌细胞株HO-8910PM后,MTT法检测细胞增殖;流式细胞术检测细胞凋亡;Westernblot检测卵巢癌细胞中核因子(NF)-κB和X连锁凋亡抑制蛋白(XIAP)表达;建立起裸鼠卵巢癌皮下移植瘤模型,观察冬凌草甲素对裸鼠卵巢癌皮下移植瘤生长的影响;免疫组织化学法检测肿瘤组织中Ki-67、NF-κB和XIAP的阳性表达。结果:HO-8910PM细胞经不同浓度冬凌草甲素(10、20、40μmol·L-1)作用24h后,细胞存活率分别为(80.14±9.84)%、(71.68±6.51)%和(64.58±5.24)%,均低于对照组(96.12±4.23)%,差异有统计学意义(P<0.05)。冬凌草甲素(40μmol·L-1)作用HO-8910PM细胞24h后,诱导(15.9±3.4)%的HO-8910PM细胞发生早期凋亡,高于对照组的(1.7±0.3)%,差异有统计学意义。3种浓度(10、20、40μmol·L-1)的冬凌草甲素作用24h,均可抑制HO-8910PM细胞中NF-κB的表达;而低浓度(10μmol·L-1)冬凌草甲素对HO-8910PM细胞中XIAP蛋白无明显抑制作用,高浓度冬凌草甲素(20和40μmol·L-1)明显抑制XIAP蛋白的表达。冬凌草甲素可显著抑制裸鼠卵巢癌皮下移植瘤生长,实验组中Ki-67、NF-κB和XIAP的表达强度均低于对照组(P<0.01)。结论:冬凌草甲素可显著抑制体内外卵巢癌的生长,该作用机制可能是冬凌草甲素通过抑制NF-κB及其调控蛋白XIAP的表达来抑制卵巢癌的生长。  相似文献   

15.
Zhu Y  Xie L  Chen G  Wang H  Zhang R 《Die Pharmazie》2007,62(6):439-444
Oridonin, an active ditepenoid component isolated from Rabdosia rubescens which is currently one of the most important Chinese traditional herbs, has been reported to exhibit anti-tumor effects in vitro. In this study, the anti-proliferation effect of oridonin against the human colorectal carcinoma cells HT29 was investigated both in vitro and in vivo. MTT assay showed that oridonin inhibited HT29 cells in a time- and dose-dependent manner. Flow cytometric analysis demonstrated that oridonin induced a G2/M phase arrest. Apoptotic bodies were observed by Hoechst 32258 fluorescence staining. Notable apoptosis and decrease of mitochondrial membrane potentials was also detected by flow cytometry. In the in vivo experiments, oridonin (10, 15, 20 mg kg(-1) of body weight, on days 1-12) was injected intraperitoneally into mice 24 h after the mice were incubated with HT29 cells. Inhibition of the solid tumor was observed. As a result, oridonin could inhibit the proliferation of HT29 cells both in vitro and in vivo, and induce apoptosis partly via the mitochondrial pathway.  相似文献   

16.
The purpose of present study is to examine effect of binary lipid matrix (combination of lipids) on the entrapment and storage stability of repaglinide (RG) loaded solid lipid nanoparticles (SLN). Solid lipid nanoparticles were prepared by modified solvent injection method for oral delivery to improve the bioavailability of RG, an antidiabetic drug. The stearic acid and tristearin were used to form lipid core materials, and Pluronic-F68 was used as a stabilizer. Nanoparticles were characterized by evaluating their particle size, zeta potential, entrapment efficiency, drug loading, solid-state studies (differential scanning calorimetry, X-ray diffraction), in vitro drug release, particle surface (transmission electron microscopy analysis with electron diffraction pattern), stability study in gastrointestinal fluids (GIFs) and storage stability at 30 °C/65% RH for 3 months. The characterization of SLN suggested that binary lipid matrix based nanoparticles had better drug entrapment and loading, desired release characteristics, stable in GIFs and significantly higher storage stability compared with single lipid formulations. Pharmacodynamic (blood glucose, blood cholesterol, blood triglyceride levels) and pharmacokinetic (AUC, T(max), peak plasma concentrations, K, t(1/2), mean residence time and relative bioavailabilities) studies were performed for the selected formulations. These studies indicate that the formulation based on binary lipid matrix significantly improves the oral bioavailability of RG.  相似文献   

17.
DEET (N,N-diethyl m-toluamide) is a lipophilic compound which has a common use as an insect repellent and causes not only skin irritation but also systemic side effects at high concentrations in long-term skin application. In this study, DEET is incorporated into solid lipid particles, a colloidal drug delivery system, in order to reduce the percutaneous permeation and avoid toxic effects and also maintain drug effectiveness on the skin surface for a long duration of insect repellence. Solid lipid particles were prepared based on emulsion systems at different concentrations and after the characterization studies, the formulation with 20% lipid phase and 1:1 drug:lipid ratio was carried to in vitro release and skin permeation studies. Solid lipid particles with DEET were compared to free DEET using cream and hydrophilic gel vehicles. Results showed that incorporation of DEET into solid lipid particles reduced the release rate and skin permeation of DEET. Imaging studies using scanning electron microscopy showed that there were still solid lipid particles on skin surface after 2 h indicating that DEET could be present for a longer time on the application site.  相似文献   

18.
基于固体脂质的纳米粒(Solid lipid - based nanoparticles,SLBNs)作为新型药物传递系统比常规的药物传递系统存在优势。通常,基于固体脂质的纳米粒可以分成两种形态,即固体脂质纳米粒( Solid lipid nanoparticles, SLNs)和纳米结构脂质载体(Nanostructured lipid carriers,NLCs)。但固体脂质纳米粒与纳米结构脂质载体在基质的组成上不同,本文就基于固体脂质的纳米粒的制备技术、表征方法及应用的最新研究进展进行总结,为基于固体脂质的纳米粒进一步研究提供参考依据。  相似文献   

19.

Objective:

The present study was undertaken to evaluate the antitumor and antioxidant status of ethanol extract of Terminalia catappa leaves against Ehrlich ascites carcinoma (EAC) in Swiss albino mice.

Materials and Methods:

The leaves powder was extracted with Soxhlet apparatus and subjected to hot continuous percolation using ethanol (95% v/v). Tumor bearing animals was treated with 50 and 200 mg/kg of ethanol extract. EAC induced in mice by intraperitoneal injection of EAC cells 1 × 106 cells/mice. The study was assed using life span of EAC-bearing hosts, hematological parameters, volume of solid tumor mass and status of antioxidant enzymes such as lipid peroxidation (LPO), reduced glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT) activities. Total phenolics and flavonoids contents from the leaves extract were also determined.

Results:

Total phenolics and flavonoids contents from the leaves extract were found 354.02 and 51.67 mg/g extract. Oral administration of ethanol extract of T. catappa (50 and 200 mg/kg) increased the life span (27.82% and 60.59%), increased peritoneal cell count (8.85 ± 0.20 and 10.37 ± 0.26) and significantly decreased solid tumor mass (1.16 ± 0.14 cm2) at 200 mg/kg as compared with EAC-tumor bearing mice (P < 0.01). Hematological profile including red blood cell count, white blood cell count, hemoglobin (11.91 ± 0.47 % g) and protein estimation were found to be nearly normal levels in extract-treated mice compared with tumor bearing control mice. Treatment with T. catappa significantly decreased levels of LPO and GSH, and increased levels of SOD and CAT activity (P < 0.01).

Conclusion:

T. catappa exhibited antitumor effect by modulating LPO and augmenting antioxidant defense systems in EAC bearing mice. The phenolic and flavonoid components in this extract may be responsible for antitumor activity.KEY WORDS: Antioxidant, Ehrlich ascites carcinoma, flavonoids, Terminalia catappa, total phenolic  相似文献   

20.
This work systematically studied the intravenous injection formulation of solid lipid nanoparticles (SLNs) loaded with actarit, a poor water soluble anti-rheumatic drug. The goal of this study was to design passive targeting nanoparticles which could improve therapeutic efficacy and reduce side-effects such as nephrotoxicity and gastrointestinal disorders commonly associated with oral formulations of actarit. Based on the optimized results of single-factor and orthogonal design, actarit-loaded SLNs were prepared by a modified solvent diffusion-evaporation method. The formulated SLNs were found to be relatively uniform in size (241+/-23 nm) with a negative zeta potential (-17.14+/-1.6 mV). The average drug entrapment efficiency and loading were (50.87+/-0.25)% and (8.48+/-0.14)%, respectively. The actarit-loaded SLNs exhibited a longer mean retention time in vivo (t(1/2(beta)), 9.373 h; MRT, 13.53 h) compared with the actarit 50% propylene glycol solution (t(1/2(ke)), 0.917 h; MRT, 1.323 h) after intravenous injection to New Zealand rabbits. The area under curve of plasma concentration-time (AUC) of actarit-loaded SLNs was 1.88 times greater than that of the actarit in 50% propylene glycol solution. The overall targeting efficiency (TE(C)) of the actarit-loaded SLNs was enhanced from 6.31% to 16.29% in spleen while the renal distribution of actarit was significantly reduced as compared to that of the actarit solution after intravenous administration to mice. These results indicated that injectable actarit-loaded solid lipid nanoparticles were promising passive targeting therapeutic agents for rheumatoid arthritis.  相似文献   

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