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液晶纳米载体对毛囊皮脂腺的靶向作用:包封米诺地尔的体外和体内效应

Targeting of the Pilosebaceous Follicle by Liquid Crystal Nanocarriers: In Vitro and In Vivo Effects of the Entrapped Minoxidil.

作者信息

Fresta Massimo, Mancuso Antonia, Cristiano Maria Chiara, Urbanek Konrad, Cilurzo Felisa, Cosco Donato, Iannone Michelangelo, Paolino Donatella

机构信息

Department of Health Sciences, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", viale Europa, 88100 Germaneto (CZ), Italy.

Department of Experimental and Clinical Medicine, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", viale Europa, 88100 Germaneto (CZ), Italy.

出版信息

Pharmaceutics. 2020 Nov 22;12(11):1127. doi: 10.3390/pharmaceutics12111127.

Abstract

The topical administration of active compounds represents an advantageous strategy to reach the various skin components as well as its appendages. Pilosebaceous follicles are skin appendages originating in the deeper skin layers. They are very difficult to target, and hence higher active dosages are generally required to achieve effective biological responses, thus favoring the rise of side effects. The aim of this work was to design a supramolecular colloidal carrier, i.e., a liquid crystal nanocarrier, for the selective delivery of active compounds into the pilosebaceous follicle. This nanocarrier showed mean sizes of ~80 nm, a good stability, a negative surface charge, and great safety properties. In vitro studies highlighted its ability to contain and release different substances and to successfully permeate the skin. Minoxidil was encapsulated in the nanocarriers and the in vivo biological effect was compared with a conventional dosage form. Minoxidil-loaded liquid crystal nanocarrier was able to selectively reach the pilosebaceous follicle, thus allowing an increased biological effectiveness of the delivered active in terms of biological response, duration of the biological effects, and reduction of collaterals. Our investigation showed that liquid crystal nanocarriers represent a promising device for the treatment of different pilosebaceous follicular impairments/diseases.

摘要

活性化合物的局部给药是一种能够作用于皮肤各层及其附属器的有效策略。毛囊皮脂腺是起源于皮肤深层的皮肤附属器。它们很难被靶向作用,因此通常需要较高的活性剂量才能实现有效的生物学反应,从而增加了副作用出现的几率。这项工作的目的是设计一种超分子胶体载体,即液晶纳米载体,用于将活性化合物选择性地递送至毛囊皮脂腺。这种纳米载体的平均尺寸约为80纳米,具有良好的稳定性、负表面电荷和出色的安全性。体外研究突出了其容纳和释放不同物质以及成功渗透皮肤的能力。将米诺地尔封装在纳米载体中,并将其体内生物学效应与传统剂型进行比较。负载米诺地尔的液晶纳米载体能够选择性地到达毛囊皮脂腺,从而在生物学反应、生物学效应持续时间和减少副作用方面提高所递送活性成分的生物学有效性。我们的研究表明,液晶纳米载体是治疗不同毛囊皮脂腺损伤/疾病的一种有前景的手段。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f2/7700400/ebaee18e1ad7/pharmaceutics-12-01127-g001.jpg

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