肝靶向米托蒽醌白蛋白微球的研究

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);T_1/2α=3.250h,T_1/2β=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。     

顺铂缓释多囊脂质体的制备和体外释放性能研究

目的 制备包封率高和缓释作用好的顺铂缓释多囊脂质体,并与反相蒸发法制备的顺铂普通脂质体比较其体外释药性能。方法 用复乳法制备顺铂多囊脂质体,非火焰原子吸收分光光度法测定顺铂含量,磷脂酶试剂法测定脂质体中磷脂的浓度。测定包封率和体外释药性。结果顺铂多囊脂质体平均粒径为16.6 μm,跨距为1.0。顺铂包封率可高达80%以上。顺铂缓释多囊脂质体的体外释药符合一级释药规律, 释药t_1/2为37.7 h,比反相蒸发法制备的顺铂普通脂质体延长8.4倍。经差示热分析发现辅助膜稳定剂有明显的膜稳定作用。结论顺铂多囊脂质体包封率高,并具有良好的缓释作用。     

新型抗肝损伤化合物XXH-32脂质体的制备及其药剂学性质研究

目的 制备新型抗肝损伤化合物XXH-32脂质体,并对其药剂学性质进行研究。方法 采用薄膜分散法制备脂质体,正交试验设计考察影响制备工艺的因素,用扫描电镜观察脂质体表面形态,对制备的XXH-32脂质体的粒径、载药量、包封率等性质及体外释放特性进行了研究。结果 XXH-32脂质体的最佳制备工艺稳定,脂质体形态圆整,粒径分布适宜。优化工艺制得的脂质体平均粒径为（175.2±2.55）nm,多分散系数为0.262±0.01,载药量为（2.60±0.12）%,包封率为（95.05±1.06）%,体外释放符合一级动力学方程,ln（100-Q）=-0.06t+4.79（R²=0.979 4）。结论 本实验获得了较理想的新型抗肝损伤化合物XXH-32脂质体,其体外释药特性符合缓释制剂特征。     

星点设计法优化盐酸小檗碱树脂复合胃黏附给药系统的研究

本文以离子交换树脂(IER)作为载体吸附盐酸小檗碱，通过包衣将其制成胃黏附微囊，并以胃黏附微囊的载药量，胃滞留时间和体外释药时间作为评价指标，对处方进行优化。考察不同型号载体与不同浓度、温度和pH值的药物溶液对IER载药量的影响；以卡伯姆934与IER的比例(X₁)、丙烯酸树脂(Eudragit)与IER的比例(X₂)、Eudragit RL与Eudragit RS的比例(X₃)为自变量，以制剂累计释放量85%的时间点(Y₁)、制剂在大鼠胃体外黏附滞留百分比(Y₂)为因变量，通过星点设计—效应面法优化胃黏附包衣处方。优化后载药工艺为在37 ℃、pH 5左右条件下，用IRP88离子交换树脂对1.0 mg·mL^-1盐酸小檗碱溶液载药；优化后的包衣液组成为X₁=0.75、 X₂=0.9、 X₃=0.6，所得制剂单位质量载药量高，可在300 min左右达到累计释放总量的85%，同时在所设计条件范围内胃黏附作用最强。     

紫杉醇壳聚糖聚合物胶束的制备及表面电荷对其在小鼠体内组织分布的影响

目的紫杉醇壳聚糖聚合物胶束的制备及表面电荷对其在小鼠体内组织分布的影响。方法采用透析法分别制备紫杉醇阳离子(PTX-CCM)和阴离子(PTX-ACM)壳聚糖聚合物胶束；昆明种小鼠分别尾静脉注射20 mg·kg^-1的PTX-CCM和PTX-ACM，HPLC法测定各组织中不同时间的药物含量，以各组织药代动力学参数(AUC，MRT，T_max和C_max)评价其体内分布。结果PTX-CCM和PTX-ACM粒径分别为164和180 nm，zeta电位分别为+23.7和-28.0 mV，载药量分别为26.4%和34.6%(w/w)，包封率分别为76.2%和89.9%。PTX-CCM和PTX-ACM肝中最大药物分布量分别达给药量的64.72%和91.84%，MRT分别为5.50和51.39 h；PTX-CCM和PTX-ACM脾中最大药物分布量达给药量的7.08%和5.16%，MRT分别为9.04和26.82 h；PTX-CCM肺部AUC和C_max分别为PTX-ACM的2.71和5.87倍；PTX-CCM和PTX-ACM心脏最高药物分布量仅为给药量的0.36%和0.24%，肾脏仅为给药量的0.75%和0.33%。结论PTX-CCM和PTX-ACM表面分别带正负电荷，具有优良的载药性能，两者皆显示出对肝脾的高度亲和性和滞留特性，尤以PTX-ACM更为显著；PTX-CCM较PTX-ACM具有更好的肺靶向性，但肺部滞留性相对较弱；两者在心、肾的分布均极少，可有效降低PTX对这些器官的毒副作用。     

2种骨架材料制备盐酸小檗碱囊泡的比较

目的 比较胆固醇和β-谷甾醇作为囊材制备的盐酸小檗碱囊泡的特性和体外释药差异。方法 采用薄膜蒸发法用2种囊材分别制备盐酸小檗碱囊泡,光学显微镜观察比较囊泡形态,微粒分析仪评价囊泡粒径分布差异;采用HPLC测定盐酸小檗碱囊泡包封率和载药量,比较2种囊泡的体外释放情况,并考察温度对囊泡稳定性的影响。结果 镜下观察2种囊材制备的囊泡圆整度均较好,粒径分布范围比较相似;用胆固醇和β-谷甾醇制备的囊泡包封率分别为28.5%和25.21%,载药量分别为1.32%和1.26%;体外释放试验中,在人工肠液和人工胃液中的胆固醇囊泡12 h累积释放百分率在50%左右,而β-谷甾醇囊泡的累积释放百分率>70%;40℃以下放置8 h,温度对2种小檗碱囊泡的包封率影响较小,当温度高于40℃时,2种小檗碱囊泡的包封率均显著降低。结论 用薄膜分散法制备的2种小檗碱囊泡镜下形态相似,包封率近似;用β-谷甾醇制备的囊泡释药快,释药量多;40℃以下放置稳定性均较好。β-谷甾醇作为载体材料制备囊泡具有可行性。     

N-辛基-O,N-羧甲基壳聚糖聚合物胶束对紫杉醇的增溶、缓释及其安全性初步评价

本文合成了一系列两亲性壳聚糖衍生物N-辛基-O,N-羧甲基壳聚糖(OCC)，以透析法制备紫杉醇(PTX)-OCC载药聚合物胶束，并考察疏水烷基取代度对包封率、载药量、粒径和zeta电位的影响，通过透射电镜(TEM)观察其形态结构，并以市售制剂为对照；通过体外溶血实验、豚鼠急性过敏实验及小鼠尾静脉注射急性毒性实验初步评价其安全性。结果表明，OCC对PTX有良好的增溶效果，在疏水基取代度为37.9%～58.6%时，载药量为24.9%～34.4%，包封率为56.3%～89.3%，且随着疏水辛基取代度的增加，载药量和包封率皆显著提高。疏水烷基链进一步提高则可能破坏胶束亲水疏水平衡而导致载药能力降低；载药胶束粒径为186.4～201.1 nm，随疏水烷基取代度的增加而减小， zeta电位为-47.5～-50.9 mV，疏水烷基取代度对其无显著影响，TEM照片显示该聚合物胶束为规则球形结构，粒径分布均匀。OCC对紫杉醇具有优良的缓释效果，未见突释，15 d累计药物释放量在60%～95%，缓释能力随疏水基取代度的增加而增强。溶血实验、 豚鼠急性过敏实验和小鼠尾静脉注射急性毒性实验结果表明，PTX-OCC溶血性和急性过敏反应低于市售制剂， PTX-OCC小鼠尾静脉注射的LD₅₀及95%可信限为134.4(125.0～144.6) mg·kg^-1，为市售制剂LD₅₀的2.7倍。初步认为PTX-OCC是安全可靠的静脉注射用纳米制剂。     

肝靶向氟尿嘧啶类脂纳米粒的研究

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d_av=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：V_c=0.04336 L.kg^-1,T_1/2β=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。     

pH响应纳米载药系统DOX@MIL-101(Fe)-NH2/HA的制备及靶向抗肿瘤作用研究

目的 制备透明质酸(hyaluronan acid，HA)修饰的纳米金属有机框架MIL-101(Fe)-NH₂载药系统，并进行体外抗肿瘤活性评价。方法 采用溶剂热法制备MIL-101(Fe)-NH₂，通过物理吸附法制备HA修饰载阿霉素的DOX@MIL-101(Fe)- NH₂/HA(DMNH)。并利用扫描电子显微镜、X射线衍射仪、氮气吸附-脱附法等对所合成材料及载药系统进行表征。采用透析法考察了载药系统的体外释药行为，并利用激光共聚焦显微镜观察HepG2细胞对其摄取情况。结果 MIL-101(Fe)-NH₂形貌为规则的正八面体，比表面积和粒径分别为1 061.45 m²·g^-1和200 nm。载药后DMNH的尺寸均一，比表面积为205.84 m²·g^-1，粒径为300 nm。MIL-101(Fe)-NH₂的最佳载药率为65.3%，根据药物释放曲线，从装有阿霉素的MIL-101(Fe)-NH₂载药体系(DMN)、DMNH中释放阿霉素显示出时间和pH依赖性。细胞摄取试验结果显示DMNH较其他组别可以运输更多的阿霉素进入HepG2细胞。细胞毒性的结果证实在相同的药物浓度下，DMNH表现出更高的肿瘤细胞杀伤效率。结论 本研究制备的DMNH载药系统结构稳定、载药量和释药效率高，同时具有优异的肿瘤细胞靶向性及pH响应释放特性，在抗肿瘤药物靶向传输方面具有应用前景。     

肝靶向羟基喜树碱缓释毫微粒的研究

采用吸附—包裹法制备了聚乙烯吡啶烷酮包被的羟基喜树碱聚氰基丙烯酸正丁酯毫微粒。研究了该毫微粒的形态、粒径及粒径分布、载药量、体外释药特征、动物体内的分布与药代动力学参数。结果表明平均粒径dav=81.2nm,载药量为1.22%,体外释药速率符合Higuchi方程:Q=0.0615+0.0940t,静脉注射后15min,即有68.2%羟基喜树碱浓集于肝脏。血浆药浓—时间曲线符合二室开放药动学模型。主要药动学参数为:Vc=3.548L,T_1/2β=146.99h,CL=0.1788L·h^-1。说明该载药毫微粒具有明显的肝靶向和缓释作用。本文报道的吸附─包裹法对水、脂不溶性药物聚氰基丙烯酸酯毫微粒的制备具有一定参考价值。     

Increasing bioavailability of silymarin using a buccal liposomal delivery system: preparation and experimental design investigation

Silymarin is a natural lipotropic agent of low bioavailability from oral products. The aim of our study is to prepare buccal liposomal delivery system of silymarin with higher bioavailability. The effect of lecithin:cholesterol molar ratio on the percentage drug encapsulated was investigated. The influence of fluctuating the amount of added drug was also determined. The effect of additives such as positive charge inducer, negative charge inducer and surfactants was studied using two different 2(3) full factorial designs. Furthermore, additives used to optimize liposomal product were also investigated for their optimal concentrations, release properties and in vitro permeation and absorption through chicken cheek pouch. Optimal liposomal encapsulation efficiency was found at 7:4 lecithin to cholesterol molar ratio. A decrease in entrapment efficiency with increasing cholesterol content was observed. Tween 20 or Tween 80 beyond 0.5 molar ratio decreased the entrapment efficiency. Positively charged liposomes showed superior entrapment efficiency over neutral and negatively charged liposomes. Release studies as well as permeation and absorption studies showed that hybrid liposomes prepared according to formula 3 containing lecithin, cholesterol, stearyl amine and Tween 20 in 9:1:1:0.5 molar ratio, respectively, gave the best drug absorption and permeation. It showed steady state permeation through chicken cheek pouch for 6h. This is expected to improve the bioavailability of silymarin in the developed liposomal buccal delivery system, as the results show an increase in drug penetration compared to free drug powder.     

Elastic liposomes mediated transdermal delivery of an anti-hypertensive agent: propranolol hydrochloride

One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present investigation ultradeformable lipid vesicles, that is, elastic liposomes were prepared incorporating propranolol hydrochloride for enhanced transdermal delivery. Elastic liposomes bearing propranolol hydrochloride were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. In vitro flux, enhancement ratio (ER), and release pattern of propranolol hydrochloride were calculated for transdermal delivery. In vivo study conducted on male albino rats (Sprague Dawley) was also taken as a measure of performance of elastic liposomal, liposomal, and plain drug solution. The better permeation through the skin was confirmed by confocal laser scanning microscopy (CLSM). Results indicate that the elastic liposomal formulation for transdermal delivery of propranolol hydrochloride provides better transdermal flux, higher entrapment efficiency, ability as a self-penetration enhancer and effectiveness for transdermal delivery as compared to liposomes.     

Preparation,In Vitro Characterization,and In Vivo Pharmacokinetic Evaluation of Respirable Porous Microparticles Containing Rifampicin

This study aimed to prepare and evaluate rifampicin microparticles for the lung delivery of rifampicin as respirable powder. The microparticles were prepared using chitosan by the spray-drying method and evaluated for aerodynamic properties and pulmonary drug absorption. To control the drug release, tripoly-phosphate in different concentrations 0.6, 0.9, 1.2, and 1.5 was employed to get a sustained drug release profile. The microparticles were evaluated for drug loading, % entrapment efficiency, tapped density, morphological characteristics, and in vitro drug release studies. Aerosol properties were determined using the Andersen cascade impactor. Porous microparticles with particle sizes (d_0.5) less than 10 μm were obtained. The entrapment of rifampicin in microparticles was up to 72%. In vitro drug release suggested that the crosslinked microparticles showed sustained release for more than 12 hrs. The drug release rate was found to be decreased as the TPP concentration was increased. The microparticles showed a fine particle fraction in the range of 55–63% with mass median aerodynamic diameter (MMAD) values below 3 μm. The in vivo pulmonary absorption of the chitosan microparticles suggested a sustained drug release profile up to 72 hrs with an elimination rate of 0.010 per hr. The studies revealed that the spray-dried porous microparticles have suitable properties to be used as respirable powder in rifampicin delivery to the lungs.     

主动载药法制备硫酸卷曲霉素脂质体及其质量评价

目的制备硫酸卷曲霉素脂质体,建立含量和包封率的测定方法,初步考察其体外释放规律。方法采用pH梯度法制备硫酸卷曲霉素脂质体,超滤法分离脂质体与游离药物,RP-HPLC测定脂质体的含量和包封率,透析法考察脂质体的体外释放行为。结果超滤法能很好地将脂质体与游离药物分离,测定硫酸卷曲霉素脂质体的含量为10.27mg/ml,包封率为47.8%,脂质体的体外释放规律符合一级动力学过程。结论pH梯度法适于制备硫酸卷曲霉素脂质体,超滤法可用于硫酸卷曲霉素脂质体包封率的测定,制备的脂质体具有一定的缓释效果。     

Skin delivery of oestradiol from deformable and traditional liposomes: mechanistic studies

Deformable vesicles and traditional liposomes were compared as delivery systems for oestradiol to elucidate possible mechanisms of drug delivery through human skin. Accordingly, epidermal permeation of oestradiol from optimized deformable vesicles and traditional liposome formulations was studied under low dose non-occluded conditions. Five mechanisms were investigated. A free drug mechanism compared low-dose permeation through skin with drug release determined after separation of the free drug. Penetration enhancement was researched by studying skin pretreatment with empty vesicles. Improved drug uptake by skin was monitored by dipping stratum corneum into different formulations for 10 min and determining drug uptake. The possibility that intact vesicles permeate through the epidermis was tested by comparing permeation from 136-nm vesicles with that from >500-nm vesicles, assuming that penetration depends on vesicle size. The possibility that different entrapment efficiencies in alternative formulations could be responsible for the difference in delivery was also evaluated. Lipid vesicles improved the skin delivery of oestradiol compared with delivery from an aqueous control. Maximum flux (Jmax) was increased 14- to 17-fold by use of deformable vesicles and 8.2- to 9.8-fold by use of traditional liposomes. Deformable vesicles were thus superior to traditional liposomes. Drug release was negligible over the period during which skin flux was maximum. Pretreatment with empty vesicles resulted in an enhancement ratio of 4.3 for pure phosphatidylcholine (PC) vesicles but the enhancement ratio ranged from only 0.8 to 2.4 for other formulations. Vesicles increased drug uptake into the stratum corneum 23- to 29-fold. Relative flux values obtained from small and large vesicles were similar. No correlation was found between entrapment efficiency and skin delivery. The results showed no evidence of a free drug mechanism, but revealed a possible penetration-enhancing effect for pure PC vesicles, although this was not the only mechanism operating. The positive uptake suggested that lipid vesicles increased drug partitioning into the skin. The data provided no evidence for in-vitro liposome penetration through skin as distinct from vesicle penetration into the stratum corneum.     

Formulation and in vitro evaluation of rifampicin loaded porous microspheres

Rifampicin (RIF) is a major component in fixed dose combination therapy for the treatment of tuberculosis. RIF has low solubility and high permeability with high dose and hence it is classified as class II drug in Biopharmaceutical Classification System (BCS). RIF has poor and variable bioavailability because of its poor solubility, acid decomposition and, drug and food interaction. The present investigation was aimed to develop RIF loaded porous microspheres as a controlled release dosage form. Eudragit based porous microspheres of RIF were prepared by emulsion solvent diffusion method. Prepared porous microspheres were evaluated for its entrapment efficacy, morphology, thermal behavior, crystalline nature, in-vitro drug release and stability in simulated gastric fluid. The entrapment efficacy of drug loaded microspheres was found to be in the range of 19.04a74.57%. Surface morphology revealed the porous and spherical structure of microspheres. Differential scanning calorimetric studies confirmed that formulation process altered the crystalline nature of RIF. In vitro drug release studies indicated that drug to polymer ratio of 2:1 showed more than 85% drug release over the period of 3 h. Stability studies in simulated gastric fluid (SGF) indicated that low relative decomposition of 18.5% was achieved with high drug to low polymer ratio of 1:4. The results obtained from the present investigation concluded that RIF loaded porous microspheres are suitable for developing oral controlled release dosage form of RIF that can prevent acid decomposition and provide better biopharmaceutical properties. Further more the microspheres can be evaluated for preventing the interaction with isoniazid, other drugs and foodstuffs.     

槲皮素前体脂质体的质量考察

目的制备液体型槲皮素前体脂质体,并对制剂质量进行考察。方法采用一种新型前体脂质体制备方法制备液体型槲皮素前体脂质体,将脂质体膜材和药物等以一定比例溶于分散介质中,形成一种无水的澄明溶液。考察其水合后粒子形态、粒径、电位、包封率及自组装速度等理化性质,并评价其体外释药性质。结果槲皮素前体脂质体遇水即可快速自组装成纳米级含药脂质体混悬液,水合后形态多为类球形,平均粒径为228.7nm,Zeta电位为21.2 mV,包封率可达90%以上,体外释药符合Higuchi方程。结论槲皮素口服前体脂质体制备工艺简单可行,包封率高,具有一定的缓释效果。     

Effect of various formulation variables on the encapsulation and stability of dibucaine base in multilamellar vesicles

Formulation of local anesthetics in liposomal topical drug delivery system could provide a sustained and localized anesthesia. The aim of this study was to develop a liposomal dibucaine base (DB) local anesthetic delivery system. DB-loaded multilamellar vesicles (MLVs) were prepared through varying lipid composition, induced charge and pH of the hydration medium. Liposomes were characterized for morphology, size, entrapment efficiency (EE), in vitro drug release and stability including leakage stability. The percentage of drug entrapped in liposomes was found to be hydration medium pH dependent and charge dependent and more pronounced for negatively charged liposomes prepared using hydration medium of pH 9. In vitro release studies of liposomes have shown a sustained release of entrapped dibucaine compared to control solution. Results revealed that adjusting the various formulation variables of dibucaine base MLVs could yield stable and effective topical liposomal local anesthetic formulations.     

Co-encapsulation of isoniazid and rifampicin in liposomes and characterization of liposomes by derivative spectroscopy

Taking into consideration the benefits of the combined therapy of isoniazid (INH) and rifampicin (RIF), this study focused on co-encapsulation of INH and RIF in the same liposome formulation. INH was incorporated in the aqueous phase and RIF in the lipid layer. Liposomes containing either INH or RIF were also prepared. All liposome formulations were compared for their loading capacity, encapsulation percentage and release properties. Drug amounts in the liposomes were estimated using peak-to-peak first-order derivative UV spectroscopy. Among the liposome formulations DPPC:chol liposomes showed the highest loading capacity (106.70 +/- 0.12 for INH and 18.17 +/- 0.06 (x 10(-3)) for RIF) and encapsulation percentage (73.84 +/- 0.78 for INH and 81.53 +/- 2.06 for RIF) compared to EPC:chol liposomes (loading capacity 93.36 +/- 0.58 for INH and 17.87 +/- 0.11 (x 10(-3)) for RIF; encapsulation percentage 64.61 +/- 0.51 for INH and 74.45 +/- 0.48 for RIF). Co-encapsulation of INH and RIF increased their individual encapsulation percentage and extended drug release compared to the formulations containing drug alone (Table 2). Results of this study support the conclusion that lipid and water soluble drugs can be successfully co-encapsulated in the same liposome formulation and also show that derivative UV spectroscopy is a sensitive method for direct and accurate quantification of these co-encapsulated drugs.     

Preparation and evaluation of N(3)-O-toluyl-fluorouracil-loaded liposomes

This study was aimed at developing a liposome delivery system for a new and potential antitumor lipophilic prodrug of 5-fluorouracil (5-Fu)-N(3)-O-toluyl-fluorouracil (TFu), intended to improve the bioavailability and therapeutic efficacy of 5-Fu by oral and intravenous administration. TFu-loaded liposomes were prepared by a modified film dispersion-homogenization technique, the formulation and manufacture parameters were optimized concerning the drug encapsulation efficiency. TFu-loaded liposomes were characterized according to particle size, size distribution, zeta potential, drug entrapment efficiency, drug loading and physical stability, respectively. In vitro release characteristics, in vivo pharmacokinetic properties and bioavailabilities were also investigated. The formulated liposomes were found to be relatively uniform in size (400.5 +/- 9.6 nm) with a negative zeta potential (-6.4 +/- 0.8 mV). The drug entrapment efficiency and loading were (88.87 +/- 3.25%) and (8.89 +/- 0.19%), respectively. The physical stability experiments results indicated that lyophilized TFu-loaded liposomes were stable for at least 9 months at 4 degrees C. In vitro drug release profile of TFu-loaded liposomes followed the bi-exponential equation. The results of the pharmacokinetic studies in mice indicated that the bioavailability of TFu-loaded liposomes was higher than the suspension after oral administration, and was bioequivalent comparing with TFu 50% alcohol solution after intravenous (i.v.) administration. These results indicated that TFu-loaded liposomes were valued to develop as a practical preparation for oral or i.v. administration.