阿达帕林-Tyrospheres局部凝胶制剂的开发，表征及其临床疗效评估,Molecular Pharmaceutics

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阿达帕林-Tyrospheres局部凝胶制剂的开发，表征及其临床疗效评估
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-07-11 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00318
Tannaz Ramezanli _{1,

2} , Bozena B. Michniak-Kohn _{1,

2}

Affiliation

在这项研究中，我们旨在开发载有阿达帕林的聚合物纳米颗粒的半固体制剂，以提高痤疮治疗的功效并改善皮肤耐受性。自组装成纳米球的两亲性和生物相容性共聚物（称为TyroSpheres）用于封装阿达帕林并提高其溶解度。施加水溶性粘性剂以制备载有阿达帕林的TyroSpheres（aapalene-TyroSphere）的凝胶制剂。研究了阿达帕林-TyroSphere凝胶制剂的粒径，形态，均质性和流变特性。进一步研究了具有优选物理和结构特性的制剂，用于体外皮肤刺激和体内犀牛小鼠模型中的粉刺活性。根据体外皮肤刺激性研究，将阿达帕林包埋在TyroSphere中可显着降低促炎细胞因子（IL-1α和IL-8）的分泌，从而证实阿达帕林的TyroSphere制剂比市售凝胶（Differin）刺激性小。与Differin处理相比，Adapalene的TyroSphere凝胶制剂可通过显着减小犀牛小鼠开放囊的大小来改善该制剂的粉刺作用。使用TyroSpheres，我们能够开发出替代的阿达帕林局部用药配方，其潜在的刺激性和功效比市售产品低。

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Development and Characterization of a Topical Gel Formulation of Adapalene-TyroSpheres and Assessment of Its Clinical Efficacy

In this study we aimed to develop a semi-solid formulation of polymeric nanoparticles loaded with adapalene to enhance the efficacy and improve the skin tolerability in acne therapy. An amphiphilic and biocompatible copolymer that self-assembles to nanospheres (known as TyroSpheres) was used to encapsulate adapalene and increase its solubility. A water-soluble viscous agent was applied to prepare a gel formulation of adapalene-loaded TyroSpheres (aapalene-TyroSphere). Particle size, morphology, homogeneity, and rheological characteristics of the adapalene-TyroSphere gel formulations were studied. The formulation with the preferred physical and structural properties was further investigated for in vitro skin irritation and in vivo comedolytic activity in a rhino mouse model. Based on the in vitro skin irritation study encapsulation of adapalene in TyroSphere significantly decreased secretion of pro-inflammatory cytokines (IL-1α and IL-8), confirming that the TyroSphere formulation of adapalene is less irritant than the commercial gel (Differin). TyroSphere gel formulation of adapalene improved the comedolytic properties of the formulation by significantly reducing the size of open utricles in rhino mice compared to Differin treatment. Using TyroSpheres, we were able to develop an alternative topical formulation of adapalene, which is potentially less irritant and more potent than the commercial product.

更新日期：2018-07-11

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