首页> 外文期刊>International Journal of Pharmaceutics >Self-assembly properties, aggregation behavior and prospective application for sustained drug delivery of a drug-participating catanionic system.
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Self-assembly properties, aggregation behavior and prospective application for sustained drug delivery of a drug-participating catanionic system.

机译:自组装性质,聚集行为和参与药物的阳离子系统持续药物输送的预期应用。

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In the present study, the self-assembly properties, aggregation behavior and potential application of mixed samples formed by an active drug (diclofenac sodium, DS) and conventional surfactant (didodecyldimethyl ammonium bromide, DDAB) are investigated with surface tension, transmission electron microscope (TEM), dynamic light scattering (DLS), zeta potential, conductivity, in vitro drug release and hemolytic toxicity measurements. The physicochemical parameters such as critical micelle concentration (CMC), the surface tension at CMC (γCMC), the maximum surface excess concentration (Γ max) and the minimum area per molecule headgroup at the air/water interface (A min) and degree of counterion binding (β) are obtained from the surface tension and electrical conductivity measurements. The results show that diclofenac sodium can decrease the surface tension of water and aggregate in the aqueous solution when its concentration is large enough. The CMC and γCMC of the DS/DDAB mixed systems are found to have values between that of individual DS and DDAB solutions. TEM and DLS results demonstrate the formation of spherical vesicles in a wide range of the molar ratio of the two components. The amount of charge on the vesicles and their stability can be tuned by controlling the amount of drug and surfactant. To evaluate the potential use of the as-prepared DS/DDAB catanionic vesicles in drug delivery systems, the in vitro drug release and hemolytic toxicity are carried out. The results indicate that both the drug release behavior and the hemolytic toxicity are dependent on the composition of the samples, X1 (X1=nDS(DS+DDAB), decreasing with the decrease of X1. The results of this work suggested that the drug-participating catanionic vesicles can be used as a safe and an efficient vehicle for sustained drug release.
机译:在本研究中,通过表面张力,透射电子显微镜(活性炭(双氯芬酸钠,DS)和常规表面活性剂(十二烷基二甲基溴化铵,DDAB)形成的混合样品的自组装性质,聚集行为和潜在应用TEM),动态光散射(DLS),ζ电位,电导率,体外药物释放和溶血毒性测量。物理化学参数,例如临界胶束浓度(CMC),CMC处的表面张力(γCMC),最大表面过量浓度(Γmax)和空气/水界面处每个分子头基的最小面积(A min)和从表面张力和电导率测量中获得抗衡离子结合(β)。结果表明,双氯芬酸钠浓度足够大时,可以降低水的表面张力并在水溶液中聚集。发现DS / DDAB混合系统的CMC和γCMC的值介于单个DS和DDAB解决方案的值之间。 TEM和DLS结果证明在两种组分的摩尔比的宽范围内球形囊泡的形成。囊泡上的电荷量及其稳定性可以通过控制药物和表面活性剂的量来调节。为了评估所制备的DS / DDAB阳离子小泡在药物递送系统中的潜在用途,进行了体外药物释放和溶血毒性。结果表明,药物释放行为和溶血毒性均取决于样品的组成X1(X1 = nDS / n(DS + DDAB),随X1的减少而降低。参与药物的阳离子小泡可以用作持续释放药物的安全有效载体。

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