当前位置: X-MOL 学术React. Funct. Polym. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Controlled release of testosterone by polymer-polymer interaction enriched organogel as a novel transdermal drug delivery system: Effect of limonene/PG and carbon-chain length on drug permeability
Reactive & Functional Polymers ( IF 5.1 ) Pub Date : 2019-12-28 , DOI: 10.1016/j.reactfunctpolym.2019.104461
Preeyarad Charoensumran , Hiroharu Ajiro

The aim of this research is to develop a transdermal drug delivery system (TDDS) for testosterone by novel physical chain entanglement organogels in propylene glycol. The organogels have been widely studied for TDDS, due to their good interactive properties with skin. The physical gel with amphiphilic polymers was studied and evaluated in this study, in order to fabricate the controllable release and sufficient permeability through the skin barrier of transdermal testosterone. The novel sugar amine-derived gel, that is poly(vinyl benzyl-N-methyl-D-glucamine) gel (poly(VbNMDG) gel), was obtained by the subsequent polymerization of the neutral form (VbNMDG) and cationic form (VbNMDG-H) with an organic base as a promotor. The gel showed electrostatic interactions as indicated by FTIR, and responsive behavior under alkali conditions. The network structure is generated from multi-interaction of linear polymer chain, confirmed by in situ polymerization. This was evidenced by the rheological measurement, which confirmed a gradual change from sol to gel-like behavior. Regarding the drug release, we set the target release time at 24 h, which is an effective treatment condition for hypogonadism. For the permeation, it was studied by using abdominal rat skin as a membrane. The d-limonene/PG synergistic activity enhanced the permeability, resulting in the highest coefficient (KD/L) at 8.80 ± 1.95 cm/h at 10% Limonene/PG. Furthermore, we evaluated the carbon chain length effect by copolymerizing of benzalkonium chloride. The dodecyl (C-12) group showed significant penetration enhancement, indicated by the coefficient which was 13.76 ± 5.45 cm/h.



中文翻译:

通过富含聚合物-聚合物相互作用的有机凝胶控制睾丸激素的释放,作为一种新型的透皮药物递送系统:柠檬烯/ PG和碳链长度对药物渗透性的影响

这项研究的目的是通过在丙二醇中的新型物理链缠结有机凝胶,开发一种用于睾丸激素的透皮给药系统(TDDS)。由于有机凝胶与皮肤的良好相互作用,因此已被广泛用于TDDS研究。为了通过透皮睾丸激素通过皮肤屏障制造可控的释放和足够的渗透性,对具有两亲性聚合物的物理凝胶进行了研究和评估。新颖的糖胺衍生凝胶,即聚(乙烯基苄基-N)-甲基-D-葡糖胺)凝胶(聚(VbNMDG)凝胶)是通过随后将中性形式(VbNMDG)和阳离子形式(VbNMDG-H)与有机碱作为促进剂聚合而获得的。凝胶显示出如FTIR所示的静电相互作用,以及在碱性条件下的响应行为。网络结构是由线性聚合物链的多重相互作用产生的,并通过原位聚合得到证实。流变学测量证明了这一点,该流变学测量证实了从溶胶到凝胶状行为的逐渐变化。关于药物释放,我们将目标释放时间设定为24小时,这是性腺功能减退的有效治疗条件。对于渗透,通过使用腹部大鼠皮肤作为膜来研究。该d-柠檬烯/ PG的协同活性增强了渗透性,在10%柠檬烯/ PG的情况下,在8.80±1.95 cm / h时具有最高的系数(KD / L)。此外,我们通过苯扎氯铵的共聚评估了碳链长度的影响。十二烷基(C-12)基团显示出显着的渗透增强,其系数为13.76±5.45 cm / h。

更新日期:2019-12-28
down
wechat
bug