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Triple protection delivery system for retinal: Preparation, skin penetration and controlled release at the hair follicles.

机译:视网膜三重保护递送系统:毛囊的制备,皮肤渗透和控释。

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To continuously supply skin with vitamin A, nanoparticles which can penetrate into the skin via hair follicles and slowly release un-degraded retinal, were designed and fabricated. The nanoparticles were prepared by covalently linking retinal to succinylchitosan and then allowing the obtained retinilidenesuccinylchitosan (RSC) to self-assemble into nanoparticles in water. Loading of the antioxidants, butylated hydroxytoluene (BHT) and vitamin E (vitE), individually into the RSC particles was also carried out to further improve the stability of the grafted retinilidene moieties in the particles. At the same loading level, vitE was more effective than BHT in protecting the retinilidene moieties from being degraded by a combination of light, heat and oxygen exposure. The vitE-loaded RSC particles possessed three potential protection barriers for the retinilidene moieties, that is (i) a chemical barrier via the imine bond, (ii) a physical barrier from the chitosan matrix around the retinilidene core, and (iii) an antioxidative barrier of the vitE which was confined within the grafted vitamin A derivatives. Covalently labeling the RSC particles with the fluorophore rhodamine B was carried out and used with confocal fluorescent microscopic analysis to reveal the ex-vivo penetration of the particles into the epidermis and dermis of porcine ear skin via hair follicles, followed by the clear release and diffusion of retinal from the particles within the tissue.
机译:为了连续地向皮肤提供维生素A,设计和制造了可以通过毛囊渗入皮肤并缓慢释放未降解的视网膜的纳米颗粒。通过将视网膜与琥珀酰壳聚糖共价连接,然后使所得的视黄酮琥珀酰壳聚糖(RSC)在水中自组装成纳米颗粒,来制备纳米颗粒。还分别将抗氧化剂,丁基化羟基甲苯(BHT)和维生素E(vitE)装载到RSC颗粒中,以进一步提高颗粒中接枝的视黄叉部分的稳定性。在相同的负载水平下,vitE比BHT更有效地保护视黄叉部分不因光,热和氧气的暴露而降解。负载vitE的RSC颗粒具有对视黄醛部分的三个潜在保护屏障,即(i)通过亚胺键的化学屏障,(ii)来自视黄醛核心周围的壳聚糖基质的物理屏障,和(iii)抗氧化性vitE的屏障被限制在接枝的维生素A衍生物中。进行了用荧光染料若丹明B共价标记RSC颗粒,并用于共聚焦荧光显微镜分析,揭示了颗粒通过毛囊离体渗透到猪耳皮肤的表皮和真皮中,然后清晰地释放和扩散视网膜从组织内的颗粒中分离出来。

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