米托蒽醌聚乳酸缓释毫微粒针剂的制备

在单因素实验的基础上用均匀设计优化了米托蒽醌聚乳酸缓释微粒的制备方法。空白和载药微粒的平均粒径分别为１２９．９６和１３３．１５ｎｍ;包封率为９９．２３％;载药量为１３．５６％;制备收率为９９．３％。以乳和支架剂制得的冻干针剂外型美观、理化性质稳定,再分散后平均粒径为１５２．０２ｎｍ。用动态透析系统考察了不同分子量聚乳酸毫微粒冻干针剂的体外释药特性,结果显示高分子量聚乳酸微粒的释药速度明显慢于低分子     

柔红霉素聚氰基丙烯酸正丁酯毫微粒制备工艺的优化

用乳液聚合法制备柔红霉素聚氰基丙烯酸正丁酯毫微粒,在单因素试验基础上,通过系统全面反馈动态技术优化,确定了处方和制备工艺。载药毫微粒平均粒径６０ｎｍ,分布范围３０～２２０ｎｍ,表观包封率９６．３６％,表观载药量５５．３３％（ｇ／ｇ）;有效包封率７４．１１％,有效载药量４２．２５％（ｇ／ｇ）。     

阿柔比星A PELGE纳米粒的制备及质量评价

目的研究阿柔比星A PELGE纳米粒的制备及质量评价。方法通过共沉淀法制备阿柔比星A PELGE纳米粒；考察阿柔比星A PELGE纳米粒的形态、粒径、包封率、载药量、Zeta电位和体外释药。结果阿柔比星A PELGE纳米粒在透射电镜下均呈圆球形，分布均匀，平均粒径为105～137nm，平均包封率为76％～86％，平均载药量为7．6％～8．6％，平均Zeta电位为-25～-33mV。纳米粒的体外释药曲线可分为突释和缓释两部分，体外释药曲线以Weibull方程拟合为好。PELGE共聚物中的PEG分子量和百分量改变对阿柔比星APELGE纳米粒的粒径、包封率、载药量、Zeta电位和释药速率的影响不明显。结论PELGE纳米粒作为传输药物的载体是可行的，并为PELGE纳米粒的进一步研究提供了实验依据。     

阿柔比星A聚乳酸毫微粒冻干针剂小鼠体内分布研究

对阿柔比星Ａ冻干针剂与阿柔比星Ａ聚乳酸毫微粒冻干针剂给予小鼠尾静脉注射后体内分布比较，采用ＨＯＬＣ法分别测定小鼠给药后血液及主要脏器中ＡＣＲＢ０Ａ浓度。结果阿柔比星Ａ聚乳酸毫微粒在小鼠肝脏中的浓度高于对照品浓度。     

眼用诺氟沙星毫微粒的质量研究

目的：通过对眼用诺氟沙星毫微粒的形态、大小及分布,载药性质,体外释药性质,初步稳定性和安全性的考察,对其质量进行评价。方法：以透射电镜和激光粒度分析仪考察形态性质;紫外分光光度法测定包封率和载药量;动态透析法考察体外释药性质;通过药物含量及卫生学指标变化评价其稳定性;眼刺激试验考察其刺激性。结果与结论：毫微粒大小均匀、外形圆整、不粘连,平均粒径dav=553um,包封率=90．14％,载药量=22．70％;体外释药性质符合双相动力学规律;室温放置3月药物含量无变化,卫生学指标符合规定;眼刺激试验经单次、多次给药,证实对眼无刺激性。     

氧化苦参碱聚氰基丙烯酸正丁酯毫微粒制备工艺研究

目的 优化氧化苦参碱聚氰基丙烯酸正丁酯毫微粒（OM-PBCA-NP）的处方和制备工艺。方法 以粒径、包封率和载药量为综合评价指标，通过单因素试验初选、均匀设计法精选，优化处方和制备工艺；以高效液相色谱法测定毫微粒中氧化苦参碱的含量。结果 确定了最佳制备工艺为三步法，最佳处方为：氧化苦参碱50mg，聚氰基丙烯酸正丁酯0．1ml，普流罗尼克F68200mg，右旋糖苷．70100mg，焦亚硫酸钠40mg；制得的氧化苦参碱毫微粒平均粒径为144．2nm，粒子圆整，载药量为17．8％，包封率为82．6％。结论 优化筛选后的处方工艺，为氧化苦参碱聚氰基丙烯酸正丁酯毫微粒的最佳制备工艺。     

顺铂聚乳酸微球的制备及体外释药

以聚乳酸为载体，用溶剂挥发法制得顺铂聚乳酸微球。选择聚乙二酵浓度、油／水相体积比、聚乳酸浓度、乳化时间、理论载药量5个因素，每个因素选择5个水平，用均匀设计安排实验。并以微球表面形态、粒径大小及分布、载药量、包封率为指标优化微球的制备工艺。按优化条件制得的微球算术平均径为48．62μm，载药量为15．1％，包封率为50．1％，体外释放符合一级动力学方程。     

SPG膜乳化法制备槲皮素缓释微球的工艺优化与表征及体外释放研究

目的 以槲皮素作为模型药物,制备聚乳酸-羟基乙酸共聚物(PLGA)缓释微球,考察其粒径及其分布、形态、包封率、载药量和体外释药性质.方法 采用SPG膜乳化法制备微球,单因素法初步优化制备处方;粒径分析仪检测微球的粒径及其分布;光学显微镜观察微球形态;通过紫外分光光度法测定微球的包封率和载药量;利用直接释药法和超速离心法...     

骨髓靶向柔红霉素毫微粒的研究

采用乳液聚合法制备了柔红霉素聚氰基丙烯酸正丁酯毫微粒（１）,并对其形态,粒径分布,载药性,动物体内经时变化过程及骨髓靶向性进行了研究。结果表明１平均微粒径为７０ｎｍ,分布范围３０－２２０ｎｍ,包封率为９７．０％,载药一达５５．７％;小鼠胸脉注射相同剂量１及柔红霉素后,前者股骨内峰浓度提高到１．６２倍,ＡＵＣ提高到４．８７倍,总靶向效率从５．１７％提高到２４．１９％,表明１具骨髓靶向性。     

氟尿嘧啶聚乳酸微球的制备工艺及体外释药特性

采用溶剂挥发法制得氟尿嘧啶聚乳酸微球。以载药量及包封率为评价指标，通过正交设计优化处方。制品外观圆整，表面有细小孔隙，平均粒径为80μm，平均载药量10％，包封率为84％，体外释药用双相动力学方程拟合效果较好，释药机理为溶蚀和扩散。     

阿柔比星A聚乳酸毫微粒冻干针剂的研制及体外药物释放规律的研究

研究阿柔比星Ａ聚乳酸毫微粒（ＡＣＲＢ－Ａ－ＰＬＡ－ＮＰ）冻干针剂的制备,并对其体外释药进行考察。根据低共熔点测定结果,以及外观、色泽、再分散性等质量参数为指标,制备出ＡＣＲＢ－Ａ－ＰＬＡ－ＮＰ冻干针剂,采用动脉透析法研究其体个释放规律。结果,制得的ＡＣＲＢ－ＡＰＬＡ－ＮＰ冻干针剂色泽均匀,再分散性良好。其体外释药可用３种方式表达。提示ＡＣＲＢ－Ａ－ＰＬＡ－ＮＰ冻干针剂有明显的缓释特征。     

伊曲康唑白蛋白纳米粒混悬液的制备与体外评价

目的 制备伊曲康唑白蛋白纳米粒混悬液,并优化其处方和制备工艺,同时对所优化的白蛋白纳米粒混悬液进行评价。方法 采用单因素实验法筛选超高压微射流技术制备伊曲康唑白蛋白纳米粒混悬液的处方和制备工艺,考察了白蛋白纳米粒混悬液的外观形态、粒径分布等理化性质以及体外释药情况。结果 制备的伊曲康唑白蛋白纳米粒混悬液呈圆整的球形或类球形分布,平均粒径为(108.1±32.8)nm,PdI为0.205,Zeta电位为(-47.6±1.7)mV;伊曲康唑白蛋白纳米粒在0.5%聚山梨酯-80磷酸盐缓冲液(pH7.4)中24h累积释放73.5%。结论 采用超高压微射流技术制备伊曲康唑白蛋白纳米粒混悬液,工艺简便可行,重现性好,有望工业化生产。     

均匀设计优化二元溶剂分散法制备莪术油纳米粒的研究

目的优化二元溶剂分散法制备莪术油纳米粒（ZTO-NP）的制备工艺技术条件，探讨其可行性。方法以形态、粒径、包封率为指标，采用均匀设计，考察分散剂浓度、载体材料用量、有机相体积和搅拌时间等影响因素，筛选出比较理想的制备工艺。结果最佳工作条件为：聚氧乙烯-聚氧丙烯共聚物（普朗尼克F68）0．1％，乳酸-乙醇酸共聚物（PLGA）0．01g，搅拌时间4h，丙酮体积1mL。所制得的纳米粒为圆整的类球形粒子，表面光滑，平均粒径为233．1nm（PDI值为0．047），zeta电位为-22．1mV，包封率为70．01％，载药量为57．55％。结论二元溶剂分散法可用于薮术油类液体药物纳米粒的制备。     

Polybutylcyanoacrylate magnetic nanoparticles as carriers of adriamycin

Objective: The present study was designed to prepare and evaluate adriamycin–polybutylcyanoacrylate magnetic nanoparticles (ADR–PBCA-MNPs) as novel carriers of adriamycin.

Methods: ADR–PBCA-MNPs was prepared by the?emulsion polymerization technique. Entrapment efficiency (ER) and drug load (DL) of nanoparticles, along with in vitro release were studied. Pharmacokinetic analysis was carried out in Kunming mice, with blood obtained at determined time points post administration. Biodistribution and recovery rate of ADR was measured and determined.

Results: Nanoparticles were visible as approximate spherical particles with good disparity, with an average diameter of 184.6 nm, a minimum diameter of 59.07?nm, and a maximum diameter of 291.66?nm as demonstrated by transmission electron microscopy. The ER and quantity of DL of ADR–PBCA-MNPs were 90.73 and 10.68%, respectively, measured by an ultraviolet–visible light spectrophotometer. In vitro study demonstrated that the release reached a balance after 72?h, with a total release rate of approximately 80%. As shown in pharmacokinetic studies in rats,the ADR–PBCA-MNPs group displayed a slowed doxorubicin release associated with better bioavailability. ADR–PBCA-MNPs reduced ADR accumulation at nontarget sites in the magnetic field, contributing to the reduced toxicity and side effects of ADR.

Conclusion: ADR–PBCA-MNPs was successfully prepared and had a satisfactory targeted effect under the magnetic field, which can increase ADR concentration at target sites but not at non-target sites. As a result, the therapeutic effect of ADR may be greatly enhanced with minimized drug toxicity and side effects.     

Biodegradable poly(epsilon -caprolactone) nanoparticles for tumor-targeted delivery of tamoxifen

To increase the local concentration of tamoxifen in estrogen receptor (ER) positive breast cancer, we have developed and characterized nanoparticle formulation using poly(epsilon -caprolactone) (PCL). The nanoparticles were prepared by solvent displacement method using acetone-water system. Particle size analysis, scanning electron microscopy, zeta potential measurements, and differential scanning calorimetry (DSC) were used for nanoparticle characterization. Biodegradation studies were performed in the presence and absence of Pseudomonas lipase in phosphate-buffered saline (PBS, pH 7.4) at 37 degrees C. Tamoxifen loading over different concentrations was analyzed by high-performance liquid chromatography (HPLC) and the optimum loading concentration was determined. In vitro release studies were performed in 0.5% (w/v) sodium lauryl sulfate (SLS) containing PBS at 37 degrees C. Cellular uptake and distribution of fluorescent-labeled nanoparticles was examined in MCF-7 breast cancer cells. SEM micrographs and Coulter analysis showed nanoparticles with spherical shape and uniform size distribution (250-300 nm), respectively. Zeta potential analysis revealed a positive surface charge of +25 mV on the tamoxifen-loaded formulation. Being hydrophobic crystalline polyester, PCL did not degrade in PBS alone, but the degradation was enhanced by the presence of lipase. The maximum tamoxifen loading efficiency was 64%. Initial burst release of tamoxifen was observed, probably due to significant surface presence of the drug on the nanoparticles. A large fraction of the administered nanoparticle dose was taken up by MCF-7 cells through non-specific endocytosis. The nanoparticles were found in the perinuclear region after 1 h. Results of the study suggest that nanoparticle formulations of selective ER modulators, like tamoxifen, would provide increased therapeutic benefit by delivering the drug in the vicinity of the ER.     

载基因壳聚糖纳米粒的制备及其相关性质的初步研究

目的制备壳聚糖载基因纳米粒,并对其体外相关性质进行初步研究。方法采用复凝聚法制备载基因纳米粒;用纳米粒度仪测量粒度分布、多分散性和Zeta电位;用透射电镜观察粒子的形态;用荧光分光光度法和比色法测定包封率和载药量,并对主要影响因素进行考察;用凝胶阻滞分析和电性结合分析对载药方式进行初步推测。结果所制备的载基因纳米粒形态规则,大多呈球形,平均粒径约150nm,PDI＜0．2,Zeta电位约20mV;包封率大于90％,载药量约30％;凝胶阻滞和电性结合分析结果表明,pDNA与壳聚糖分子间可通过电性结合作用而完全结合。结论采用复凝聚法可制备粒度分布均匀,形态规则,具有较高包封率和载药量的载基因壳聚糖纳米粒;电性结合作用是载基因壳聚糖纳米粒载药的主要方式。     

羟基喜树碱微球的制备及其小鼠体内分布研究

目的:制备肺靶向性羟基喜树碱(HCPT)微球,评价其体外释药特性及其在小鼠体内的肺靶向性。方法:以聚乳酸为主要辅料,采用溶剂挥发法制备微球,考察其粒径、包封率、载药量,比较微球及原料药的体外释药性;取12只小鼠分别尾静脉注射HCPT微球及原料药,30min后分别测定血浆及各组织的药物浓度并计算相对分布率。结果:所制微球粒径在7～30μm者达81.6%,平均粒径为(14.2±3.1)μm,包封率为72.36%,载药量为(40.6±3.6)%,微球及原料药体外释药参数T50分别为85、18min。微球给药组在肺中的药物浓度最高(32.2±2.48)μg.mL-1,相对分布率58.1%;原料药给药组在血浆中的药物浓度最高(13.52±2.58)μg.mL-1,相对分布率25.24%。结论:所制HCPT微球具有明显的缓释性及肺靶向性。     

中心组合设计法优化3′,5′-二辛酰基-氟苷药质体制备工艺

目的采用中心组合设计法优化3′,5′-二辛酰基-5-氟脲嘧啶脱氧核苷药质体的制备工艺.方法以薄膜-超声分散法制备药质体,以平均粒径、包封率、载药量和综合指标为因变量,对药物与磷脂的比例、F-68浓度和三硬脂酸甘油酯浓度3个自变量的各个水平进行二项式拟合,效应面法选取较佳工艺条件并进行预测分析.结果平均粒径、包封率、载药量和综合指标拟合所得多元二次方程的复相关系数分别为0.9393,0.7739,0.9801和0.8369.优化条件制备的药质体的平均粒径、包封率和载药量分别为76nm,97.49%和29.37%.结论中心组合设计有应用简便、预测性好等优点,制备的药质体符合设计要求.     

Nanoparticles in plant extracts: influence of drugs on the formation of nanoparticles and precipitates in black tea infusions.

The influence of the neuroleptics fluphenazine and promethazine on the formation of nanoparticles in aqueous tea infusions was investigated using photon correlation spectroscopy. Formation of nanoparticles and of precipitates was observed in decaffeinated tea and caffeine-containing tea. The amount of drug in the nanoparticle fraction was determined at different starting concentrations using high-performance liquid chromatography. In the case of fluphenazine, between 8 and 30% are assigned to the nanoparticles fraction, in the case of promethazine between 30 and 56%. The concentration of free active principle is reduced by about 99% for fluphenazine or by about 90% for promethazine. A loss of pharmacological activity of the neuroleptics is probable. The addition of promethazine to infusions of caffeine containing tea resulted in the formation of nanoparticles with a small size distribution; their mean size was comparable to the diameter of nanoparticles in pure tea infusions. In the case of fluphenazine the mean particle size grew with increasing concentration. Adding promethazine to infusions of decaffeinated tea resulted in the formation of nanoparticles with a broad size distribution. Two different size classes were formed after addition of fluphenazine. Caffeine and neuroleptics both take part in the formation of nanoparticles in caffeine containing tea. The particles were visualized using scanning electron microscopy. Molecular modelling calculations were performed to investigate probable geometries between neuroleptics and thearubigins.