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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Formulation and evaluation of stomach-specific amoxicillin-loaded carbopol-934P mucoadhesive microspheres for anti-Helicobacter pylori therapy
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Formulation and evaluation of stomach-specific amoxicillin-loaded carbopol-934P mucoadhesive microspheres for anti-Helicobacter pylori therapy

机译：胃特异性阿莫西林负载的carbopol-934P粘膜粘附微球的配制和评估，用于抗幽门螺杆菌治疗

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摘要

The purpose of this research was to formulate and systemically evaluate in vitro and in vivo performances of mucoadhesive amoxicillin microspheres for the potential use in the treatment of gastric and duodenal ulcers, which were associated with Helicobacter pylori. Amoxicillin mucoadhesive microspheres containing carbopol-934P as mucoadhesive polymer and ethyl cellulose as carrier polymer were prepared by an emulsion-solvent evaporation technique. Results of preliminary trials indicate that quantity of emulsifying agent, time for stirring, drug-to-polymers ratio and speed of rotation affected the characteristics of microspheres. Microspheres were discrete, spherical, free flowing and showed a good percentage of drug entrapment efficiency. An in vitro mucoadhesive test showed that amoxicillin mucoadhesive microspheres adhered more strongly to the gastric mucous layer and could retain in the gastrointestinal tract for an extended period of time. A 32 full factorial design was employed to study the effect of independent variables, drug-to-polymer-to-polymer ratio (amoxicillin-ethyl cellulose-carbopol-934P) (X1) and stirring speed (X2) on dependent variables, i.e. percentage mucoadhesion, drug entrapment efficiency, particle size and t_(80) The best batch exhibited a high drug entrapment efficiency of 56%;;mucoadhesion percentage after 1 h was 80% and the particle size was 109 μm. A sustained drug release was obtained for more than 12 h. The drug-to-polymer-to-polymer ratio had a more significant effect on the dependent variables. The morphological characteristics of the mucoadhesive microspheres were studied under a scanning electron microscope. In vitro release test showed that amoxicillin released slightly faster in pH 1.2 hydrochloric acid than in pH 7.8 phosphate buffer. In vivo H. pylori clearance tests were also carried out by administering amoxicillin powder and mucoadhesive microspheres to H. pylori infectious Wistar rats under fed conditions at single dose or multiple dose(s) in oral administration. The results showed that amoxicillin mucoadhesive microspheres had a better clearance effect than amoxicillin powder, in conclusion, the prolonged gastrointestinal residence time and enhanced amoxicillin stability resulting from the mucoadhesive microspheres of amoxicillin might make a contribution to H. pylori complete eradication.
机译：这项研究的目的是制定和系统评估粘膜粘附性阿莫西林微球的体外和体内性能，以潜在地治疗与幽门螺杆菌相关的胃溃疡和十二指肠溃疡。通过乳液-溶剂蒸发技术制备了含有卡波普-934P作为粘膜粘附性聚合物和乙基纤维素作为载体聚合物的阿莫西林粘膜粘附性微球。初步试验结果表明，乳化剂的量，搅拌时间，药物与聚合物的比例和旋转速度都会影响微球的特性。微球是离散的，球形的，自由流动的，并显示出良好的药物截留效率百分比。体外粘膜粘附试验表明，阿莫西林粘膜粘附微球更牢固地粘附于胃粘膜层，并可以在胃肠道中保留较长时间。采用32个全因子设计来研究自变量，药物与聚合物与聚合物的比率（阿莫西林-乙基纤维素-carbopol-934P）（X1）和搅拌速度（X2）对因变量（即百分比）的影响粘膜粘附力，药物包封率，粒径和t_（80）最佳批次显示出56％的高药物捕获率; 1 h后的粘膜粘附率为80％，粒径为109μm。持续释放药物超过12小时。药物对聚合物对聚合物的比率对因变量具有更显着的影响。在扫描电子显微镜下研究了粘膜粘附性微球的形态特征。体外释放试验表明，阿莫西林在pH 1.2盐酸溶液中的释放比在pH 7.8磷酸盐缓冲液中的释放稍快。体内幽门螺杆菌清除试验还通过在喂食条件下以单剂量或多剂量口服给予阿莫西林粉末和粘膜粘附微球给幽门螺杆菌感染性Wistar大鼠来进行。结果表明，阿莫西林粘膜粘附微球的清除效果好于阿莫西林粉，因此，阿莫西林粘膜粘附微球导致的胃肠道滞留时间延长和阿莫西林稳定性增强，可能有助于彻底根除幽门螺杆菌。

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