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首页> 外文期刊>Journal of pharmaceutical sciences. >Synthesis and in vitro studies of cross-linked hydrogel nanoparticles containing amoxicillin.
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Synthesis and in vitro studies of cross-linked hydrogel nanoparticles containing amoxicillin.

机译:含有阿莫西林的交联水凝胶纳米粒子的合成和体外研究。

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In this paper, we report the synthesis and characterization of a novel cross-linked N-isopropylacrylamide-acrylic acid-hydroxyethyl methacrylate [P (NIPASM-AA-HEM)] hydrogel nanoparticles (NPs) containing amoxicillin. The aim of present study was to investigate whether these hydrogel NPs have the potential to be used in antibiotic delivery to stomach for treatment of Helicobacter pylori. Amoxicillin-loaded hydrogel NPs were prepared using cross-linked P (NIPASM-AA-HEM) as mucoadhesive polymer for the potential use of treating gastric and duodenal ulcers. Aiming at predicting the in vivo behavior of the amoxicillin-loaded NPs, the physicochemical properties in terms of entrapment efficiency (EE%), mean diameter, and morphology of NPs was evaluated. The dependence of the EE% of the drug on the organic to aqueous phase ratio was also studied. The profile of amoxicillin release from P (NIPASM-AA-HEM) NPs system was studied under various conditions. In all these experiments, amoxicillin release in the free form was studied by ultraviolet (UV) spectrophotometric analysis. Experimental results showed that at pH 7.4, drug release rises when polymer concentration in the formulation increases; in human plasma on the contrary, drug release is reduced as concentration of the polymer in the formulation rises. In vitro amoxicillin release rate was also higher in pH 1 than that in pH 7.4. About 88.5% of amoxicillin entrapped in the NPs was released in 4 h in the pH 1.0 medium, whereas in phosphate buffer at pH 7.4 no more than 45% was released after 4 h incubation at 37 degrees C. Amoxicillin concentration in rat's gastric tissue was determined. The results of in vivo studies showed that the hydrogel NPs enhance drug concentration at topical site than powder amoxicillin. Thus, amoxicillin-loaded hydrogel NPs may provide therapeutic concentration at a much lower dose that may reduce the adverse effects of amoxicillin in high doses.
机译:在本文中,我们报告了含有阿莫西林的新型交联的N-异丙基丙烯酰胺-丙烯酸-甲基丙烯酸羟乙酯[P(NIPASM-AA-HEM)]水凝胶纳米颗粒(NPs)的合成和表征。本研究的目的是研究这些水凝胶NP是否有潜力用于向胃部输送抗生素以治疗幽门螺杆菌。使用交联的P(NIPASM-AA-HEM)作为粘膜粘附聚合物制备载有阿莫西林的水凝胶NP,可用于治疗胃和十二指肠溃疡。为了预测装载阿莫西林的NP的体内行为,评估了NP的包封率(EE%),平均直径和形态方面的理化性质。还研究了药物的EE%对有机相与水相之比的依赖性。在各种条件下研究了阿莫西林从P(NIPASM-AA-HEM)NPs系统释放的情况。在所有这些实验中,通过紫外分光光度法研究了游离形式的阿莫西林释放。实验结果表明,在pH 7.4下,当制剂中的聚合物浓度增加时,药物释放会增加;相反,在人血浆中,随着制剂中聚合物浓度的增加,药物释放减少。 pH 1的体外阿莫西林释放速率也高于pH 7.4。在pH 1.0培养基中4小时内,NP中截留的阿莫西林含量约88.5%释放,而在pH 7.4的磷酸盐缓冲液中在37°C下孵育4 h后,释放的不超过45%。大鼠胃组织中阿莫西林的浓度为决心。体内研究结果表明,水凝胶NPs比粉末阿莫西林可提高局部部位的药物浓度。因此,载有阿莫西林的水凝胶NP可以低得多的剂量提供治疗浓度,可以降低高剂量阿莫西林的不利影响。

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