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Particle-stabilized oil-in-water emulsions as a platform for topical lipophilic drug delivery
Colloids and Surfaces B: Biointerfaces ( IF 5.8 ) Pub Date : 2020-10-18 , DOI: 10.1016/j.colsurfb.2020.111423
Suphatra Hiranphinyophat 1 , Akihisa Otaka 2 , Yuta Asaumi 3 , Syuji Fujii 4 , Yasuhiko Iwasaki 5
Affiliation  

Low-environmental-impact emulsion systems for transdermal drug delivery in topical treatment have gained increasing interest. However, low stability and adverse systemic side effects severely decrease their efficiency. This study proposed a stable oil-in-water (O/W) emulsion loaded with bifonazole (BFZ) as a lipophilic drug stabilized by poly(2-isopropoxy-2-oxo-1,3,2-dioxaphospholane)-modified cellulose nanocrystals (CNC-g-PIPP) as vehicles for topical delivery of lipophilic drugs. We fully characterized stability, BFZ-loaded particle-stabilized emulsions (PEs) for morphology, droplet size, and its distribution. In addition, we evaluated the in vitro drug-releasing capacity and in vitro skin permeation of BFZ in a porcine skin animal model using a side-bi-side® diffusion cell. An O/W BFZ-loaded emulsion stabilized with CNC-g-PIPP particles (BFZ-loaded CP-PE) with a small mean droplet size of 2.54 ± 1.39 μm was developed and was stable for > = 15 days without a significant change in droplet size. The BFZ-loading efficiency in PEs was 83.1 %. BFZ was slowly released over an extended period, and the releasing ratio from BFZ-loaded CP-PE was only 17 % after 48 h. The BFZ-loaded CP-PE showed a ∼4.4-fold increase in BFZ permeation and penetration compared to a conventional surfactant-stabilized emulsion and BFZ control solution. Fluorescence-labeling studies showed that BFZ-loaded CP-PE could well penetrate skin layers from the stratum corneum (SC) to the dermis. In addition, histopathology studies of porcine skin treated with the PE formulation showed an intact SC with unaltered adjacent structures and no observed signs of inflammation. Therefore, the proposed CP-PE shows great potential as a transdermal drug carrier for enhancing lipophilic drug permeation.



中文翻译:

颗粒稳定的水包油型乳剂作为局部亲脂性药物递送的平台

在局部治疗中用于透皮药物递送的低环境影响乳液系统已引起越来越多的关注。但是,低稳定性和不利的全身副作用严重降低了其效率。这项研究提出了一种稳定的水包油(O / W)乳状液,其中载有联苯并唑(BFZ)作为亲脂性药物,由聚(2-异丙氧基-2-氧代-1,3,2-二氧杂磷杂环戊烷)改性的纤维素纳米晶体稳定化(CNC-g-PIPP)作为局部递送亲脂性药物的载体。我们充分表征了稳定性,负载BFZ的颗粒稳定乳液(PEs)的形态,液滴大小及其分布。此外,我们评估了在体外药物释放能力,并在体外在皮肤用侧双向侧的猪皮肤的动物模型BFZ的渗透®扩散池。研制出了用CNC-g-PIPP颗粒(BFZ装载的CP-PE)稳定的O / W BFZ装载的乳液,其平均液滴尺寸小,为2.54±1.39μm,并且在> = 15天的时间内保持稳定,且无显着变化液滴尺寸。PE中的BFZ加载效率为83.1%。BFZ在一段较长的时间内缓慢释放,而负载BFZ的CP-PE在48小时后的释放率仅为17%。与传统的表面活性剂稳定的乳液和BFZ对照溶液相比,负载BFZ的CP-PE的BFZ渗透性和渗透性增加了约4.4倍。荧光标记研究表明,负载BFZ的CP-PE可以很好地穿透皮肤层,从角质层(SC)到真皮。此外,用PE制剂处理的猪皮肤的组织病理学研究表明,完整的SC具有不变的相邻结构,没有观察到炎症迹象。因此,提出的CP-PE显示出作为增强亲脂性药物渗透的透皮药物载体的巨大潜力。

更新日期:2020-11-02
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