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用于经皮共递送氢化可的松/羟基酪醇的自组装聚合物纳米粒:使用 NC/Nga 小鼠模型的离体和体内研究。

Self-assembled polymeric nanoparticles for percutaneous co-delivery of hydrocortisone/hydroxytyrosol: an ex vivo and in vivo study using an NC/Nga mouse model.

机构信息

Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz 50300, Kuala Lumpur, Malaysia.

出版信息

Int J Pharm. 2013 Feb 28;444(1-2):109-19. doi: 10.1016/j.ijpharm.2013.01.024. Epub 2013 Jan 18.

DOI:10.1016/j.ijpharm.2013.01.024
PMID:23337632
Abstract

In this study, hydroxytyrosol (HT; a potent antioxidant) was co-administered with hydrocortisone (HC) to mitigate the systemic adverse effects of the latter and to provide additional anti-inflammatory and antioxidant benefits in the treatment of atopic dermatitis (AD). The co-loaded nanoparticles (NPs) prepared had shown different particle sizes, zeta potentials, loading efficiencies, and morphology, when the pH of the chitosan solution was increased from 3.0 to 7.0. Ex vivo permeation data showed that the co-loaded NPs formulation significantly reduced the corresponding flux (17.04μg/cm(2)/h) and permeation coefficient (3.4×10(-3)cm/h) of HC across full-thickness NC/Nga mouse skin. In addition, the NPs formulation showed higher epidermal (1560±31μg/g of skin) and dermal (880±28μg/g of skin) accumulation of HC than did a commercial HC formulation. Moreover, an in vivo study using an NC/Nga mouse model revealed that compared to the other treatment groups, the group treated with the NPs formulation efficiently controlled transepidermal water loss (13±2g/m(2)/h), intensity of erythema (207±12), and dermatitis index (mild). In conclusion, NPs co-loaded with HC/HT is proposed as a promising system for the percutaneous co-delivery of anti-inflammatory and antioxidative agents in the treatment of AD.

摘要

在这项研究中,羟基酪醇(HT;一种有效的抗氧化剂)与氢化可的松(HC)联合给药,以减轻后者的全身不良反应,并在治疗特应性皮炎(AD)方面提供额外的抗炎和抗氧化作用。当壳聚糖溶液的 pH 值从 3.0 增加到 7.0 时,所制备的共载纳米颗粒(NPs)显示出不同的粒径、Zeta 电位、载药效率和形态。体外渗透数据表明,共载 NPs 制剂显著降低了 HC 穿过全厚 NC/Nga 小鼠皮肤的相应通量(17.04μg/cm(2)/h)和渗透系数(3.4×10(-3)cm/h)。此外,NPs 制剂显示出比商业 HC 制剂更高的 HC 在表皮(1560±31μg/g 皮肤)和真皮(880±28μg/g 皮肤)中的积累。此外,使用 NC/Nga 小鼠模型的体内研究表明,与其他治疗组相比,用 NPs 制剂治疗的组有效地控制了经表皮水分流失(13±2g/m(2)/h)、红斑强度(207±12)和皮炎指数(轻度)。总之,共载 HC/HT 的 NPs 被提议作为一种有前途的系统,用于经皮共递抗炎和抗氧化剂治疗 AD。

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