Anti-Inflammatory and Gastroprotective Properties of Aspirin - Entrapped Solid Lipid Microparticles.

IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics
Salome A Chime, Paul A Akpa, Cosmas C Ugwuanyi, Anthony A Attama
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引用次数: 5

Abstract

Background: Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529, 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation.

Objective: The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance oral bioavailability and inhibit gastric irritation.

Methods: This solid lipid microparticles loaded with aspirin (SLM) was formulated by a modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, Encapsulation Efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats.

Results: The results showed that aspirin entrapped SLM exhibited the highest EE of 72% and particle size range of 7.60 + 0.141µm to 20.25 + 0.070µm. Formulations had about 55% drug release at 6h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100% gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage of anti-inflammatory activities also showed that aspirin-entrapped SLM had 78% oedema inhibition at 7h, while the reference had 68% inhibition at 7h.

Conclusion: Aspirin-entrapped SLM showed good sustained-release properties, enhanced antiinflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.

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阿司匹林包裹固体脂质微粒的抗炎和胃保护特性。
背景:阿司匹林是一种非甾体抗炎药,在治疗炎症和其他健康状况方面非常有效,然而,它会引起胃刺激。最近,研究人员开发了可吸入阿司匹林的专利(US9757529, 2019),用于快速吸收和规避胃刺激。目的:制备阿斯匹林脂基制剂,提高口服生物利用度,抑制胃刺激。方法:采用改进的冷均质-溶剂蒸发法制备阿司匹林固体脂质微粒。对其体外释放度、粒径、包封效率(EE)、微粒性能和载药量等进行了体外研究。在Wistar大鼠身上进行了抗炎和溃疡特性等药效学研究。结果:阿司匹林包埋的SLM的EE最高,达72%,粒径范围为7.60 + 0.141µm ~ 20.25 + 0.070µm。在pH值为6.8的模拟肠液中,制剂在6h时的释药率约为55%。该配方具有良好的流动性,易于填充到硬明胶胶囊壳中。SLM对阿司匹林引起的溃疡有100%的胃保护作用(p < 0.05)。抗炎活性的百分比也表明,阿司匹林包埋的SLM在7h时的水肿抑制率为78%,而参考文献在7h时的抑制率为68%。结论:阿司匹林包埋SLM具有良好的缓释特性、增强的抗炎特性和对阿司匹林致溃疡的全胃保护作用,可作为阿司匹林每日一次口服。
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来源期刊
CiteScore
3.90
自引率
0.00%
发文量
0
期刊介绍: Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.
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