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德孚医药出版社最新文章精选 (Part 3)
德孚医药出版社专门从事开放获取同行评议期刊的出版业务,这些期刊广泛地涉及科学、技术特别是医药领域。德孚旗下共有 130 多种开放获取期刊，许多优秀医药论文已经在我们的中文网站上发表。我们特意摘选了一些论文，与大家一起分享：
共轭的树枝状聚合物及超声波介导的透皮双氯芬酸药物输送系统
The purpose of the present study was to develop
a novel transdermal drug-delivery system comprising a polyamidoamine dendrimer
coupled with sonophoresis to enhance the permeation of diclofenac (DF) through
the skin. The novel transdermal drug-delivery system was developed by using a
statistical Plackett–Burman design.
Hairless male Wistar rat skin was used for the DF-permeation study. Coupling
media concentration, ultrasound-application time, duty cycle, distance from
probe to skin, and a third-generation polyamidoamine-dendrimer concentration
were selected as independent variables, while in vitro drug release was
selected as a dependent variable. Independent variables were found to be
statistically significant (P <0.05).
DF gel without dendrimer and ultrasound treatment to skin (passive delivery,
run 13) showed 56.69 µg/cm2 cumulative drug permeated through the
skin, while the DF-dendrimer gel without sonophoresis treatment (run 14) showed
257.3 µg/cm2 cumulative drug permeated through the skin after 24
hours. However, when the same gel was applied to sonophoresis-treated skin,
drastic permeation enhancement was observed.
In the case of run 3, the cumulative drug that permeated through the skin was
935.21 µg/cm2. It was concluded that dendrimer-coupled
sonophoresis-mediated transdermal drug delivery system has the potential to
enhance the permeation of DF through the skin.
利妥昔单抗（Rituximab, RTX）是一种针对人CD20 抗原的人-鼠嵌合型单克隆抗体，其出现大大提高了淋巴瘤的治疗效果。然而，并非所有的患者对利妥昔单抗的治疗都有较好的反应，且随着治疗的深入，越来越多的患者逐步表现出对其治疗的耐药，这大大限制了利妥昔单抗的临床应用。
目前的研究表明，利妥昔单抗主要通过以下四种机制来杀伤肿瘤细胞——补体依赖的细胞毒作用(CDC), 抗体依赖的细胞介导的细胞毒作用(ADCC),Caspase 依赖的凋亡以及溶酶体介导的程序性死亡(PCD)。然而，迄今为止尚没有一种靶向 CD20 的单克隆抗体或者抗体衍生物能够同时激活这四种机制。本研究应用纳米医学技术，将两种不同类型的 CD20 抗体（I 型抗体利妥昔单抗，II 型抗体托西莫单抗）用聚乙烯亚胺（PEI）载体进行交联，成功制备出一种新型的针对人CD20 抗原的纳米抗体梳 PPRT。
与游离的单克隆抗体相比，PPRT 纳米抗体梳对淋巴瘤细胞表面 CD20 抗原拥有相当的结合能力和更低的解离能力。随后的研究结果表明，该纳米抗体梳能够通过“细胞内交联”和“跨细胞交联”同时激活上述与 CD20 抗体相关的杀伤肿瘤细胞的所有四条通路。体内研究结果表明，PPRT 纳米抗体梳具有比游离 CD20 抗体更慢的清除率和更长的半衰期，在体内外研究中显示出极强的淋巴瘤杀伤效果。