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载有酮洛芬纳米颗粒的可生物降解成分的乳凝胶。

Biodegradable Ingredient-Based Emulgel Loaded with Ketoprofen Nanoparticles.

机构信息

Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.

Department of Pharmacy, University of Swabi, Swabi, Pakistan.

出版信息

AAPS PharmSciTech. 2018 May;19(4):1869-1881. doi: 10.1208/s12249-018-0997-0. Epub 2018 Apr 12.

DOI:10.1208/s12249-018-0997-0
PMID:29651679
Abstract

Biodegradable materials are extensively employed to design nanocarriers that mimic extracellular environment in arthritis. The aim of this study was to formulate and characterize biocompatible, biodegradable ketoprofen-loaded chitosan-chondroitin sulfate (CHS-CS) nanoparticles with natural ingredients for transdermal applications. Polymers used in the design of nanocarriers are biodegradable and produce synergistic anti-inflammatory effect for the treatment of arthritis. For transdermal application, argan oil-based emulgel is utilized to impart viscosity to the formulation. Furthermore, naturally occurring argan oil synergizes anti-inflammatory effect of formulation and promotes skin penetration. CHS and CS form nanoparticles by polyelectrolyte complex formation or complex coacervation at pH 5.0. These particles were loaded into argan oil-based emulgel. Employing this method, nanoparticles were formulated with particle size in the range of 300-500 nm. These nanocarriers entrapped ketoprofen and showed more than 76% encapsulation efficiency and 77% release of the ketoprofen at pH 7.4 within 72 h. Drug releases from CHS-CS nanoparticles by mechanism of simple diffusion. Nanoparticle-loaded argan oil emulgel significantly enhanced skin penetration of ketoprofen as compared to marketed gel (p < 0.05). Nanocarriers prepared successfully delivered drug through transdermal route using natural ingredients. Graphical abstract ᅟ.

摘要

可生物降解材料被广泛用于设计纳米载体,以模拟关节炎中外细胞环境。本研究的目的是制备并表征具有生物相容性和可生物降解性的载酮洛芬壳聚糖-硫酸软骨素(CHS-CS)纳米粒子,该纳米粒子含有天然成分,可用于经皮给药。用于设计纳米载体的聚合物是可生物降解的,并产生协同抗炎作用,用于治疗关节炎。为了经皮给药,利用阿甘油基乳凝胶赋予制剂粘性。此外,天然存在的阿甘油协同制剂的抗炎作用,并促进皮肤渗透。CHS 和 CS 在 pH 5.0 下通过聚电解质复合形成或复合凝聚形成纳米粒子。这些颗粒被加载到阿甘油基乳凝胶中。采用这种方法,可将纳米颗粒的粒径在 300-500nm 的范围内进行配方设计。这些纳米载体包封了酮洛芬,在 pH 7.4 下 72 小时内释放超过 76%的酮洛芬,载药效率超过 77%。CHS-CS 纳米颗粒中的药物通过简单扩散机制释放。与市售凝胶相比,载药阿甘油乳凝胶显著提高了酮洛芬的经皮渗透(p<0.05)。成功制备的纳米载体使用天然成分通过经皮途径递药。

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