当前位置: X-MOL 学术Mol. Pharmaceutics › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Comparative Evaluation for Controlled Release of Amoxicillin from RSM-CCD-Optimized Nanocomposites Based on Sodium Alginate and Chitosan-Containing Inclusion Complexes
Molecular Pharmaceutics ( IF 4.9 ) Pub Date : 2021-09-05 , DOI: 10.1021/acs.molpharmaceut.1c00340
Khushbu 1 , Rajeev Jindal 1
Affiliation  

Amoxicillin (AMX) is a semisynthetic antibiotic, an analogue of ampicillin, with a wide spectrum of bacterial activity against many microorganisms but possesses some limits. To increase the drug effectiveness, supramolecule nanocomposites composed of β-cyclodextrin (β-CD) and chitosan/sodium alginate/GO were chosen in the present study as a sustained release formulation. Nanocomposites of chitosan (CH), sodium alginate (ALG), and graphene oxide (GO) were synthesized at 50 °C. The inclusion complexes (ICs) were processed via the physical mixture (PM), kneading (KM), microwave (MW) method, or coprecipitation (CP) and directly loaded into the nanocomposite. To confirm the formation of true ICs, the ICs were analyzed by DSC, SEM, 1H NMR, 2D NMR ROESY, and XRD. A drug release study was performed to find out which method is best for the controlled release of drugs in different environments of pH 2, 7, and 7.4 at 37 °C. From the observed drug release data, it was found that PM and KM showed a burst release of drugs and the microwave method was the most suitable method to prepare exact ICs of AMX and β-CD for sustained release of drugs. Kinetics of drug release was analyzed by various kinetic models, and it was observed that the Korsmeyer–Peppas and Peppas–Sahlin models were best fit for drug release in all cases. A Phase solubility study was carried out to find the stoichiometry of IC formation and the complexation constant. The drug release was controlled and pH-dependent, confirming that nanocomposites are pH-sensitive. From drug release analysis, it was acknowledged that β-CD is capable of causing sustained drug release.

中文翻译:

基于海藻酸钠和壳聚糖包合物的 RSM-CCD 优化纳米复合材料中阿莫西林控制释放的比较评价

阿莫西林 (AMX) 是一种半合成抗生素,是氨苄青霉素的类似物,对许多微生物具有广谱的细菌活性,但具有一定的局限性。为了提高药物有效性,本研究选择了由β-环糊精(β-CD)和壳聚糖/海藻酸钠/GO组成的超分子纳米复合材料作为缓释制剂。壳聚糖 (CH)、海藻酸钠 (ALG) 和氧化石墨烯 (GO) 的纳米复合材料在 50 °C 下合成。包合物 (IC) 通过物理混合物 (PM)、捏合 (KM)、微波 (MW) 或共沉淀 (CP) 方法进行处理,并直接加载到纳米复合材料中。为了确认真正 IC 的形成,通过 DSC、SEM、1对 IC 进行了分析H NMR、2D NMR ROESY 和 XRD。进行了药物释放研究,以确定在 37 °C 下,在 pH 2、7 和 7.4 的不同环境中,哪种方法最适合药物的控释。从观察到的药物释放数据发现,PM和KM表现出药物的爆发释放,微波法是制备药物缓释AMX和β-CD精确IC的最合适方法。通过各种动力学模型分析药物释放动力学,观察到 Korsmeyer-Peppas 和 Peppas-Sahlin 模型在所有情况下都最适合药物释放。进行了相溶解度研究以找到 IC 形成的化学计量和络合常数。药物释放受控且依赖于 pH 值,证实了纳米复合材料对 pH 值敏感。从药物释放分析,
更新日期:2021-10-04
down
wechat
bug