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Optimized ciprofloxacin release from citric acid crosslinked starch-PVA hydrogel film: modelling with mixture design
Journal of Polymer Research ( IF 2.6 ) Pub Date : 2021-01-05 , DOI: 10.1007/s10965-020-02397-7
Jennifer David , Biswanath Mahanty

Projecting optimal composition for hydrogel blends, while designing sustained release formulation of hydrophilic drug, is of paramount importance. In present study, composite hydrogel incorporating ciprofloxacin (0.2% w/w) was prepared by sequential addition of polyvinyl alcohol (PVA) (20–95% w/w), starch (0–75% w/w), citric acid (5–80% w/w) as cross-linker in a heat-induced gelatinization process. A constrained simplex mixture design was adopted to rationalize the proportion of ingredients in hydrogel composition while modelling the time required for 50% drug release from the hydrogel under in-vitro conditions. Prepared hydrogels were also characterized for swelling ratio, tensile strength, and antimicrobial disc-diffusion assay. Decreasing proportion of starch relative to PVA results in a transparent hydrogel, with a high degree of equilibrium swelling (up to 104%). Drug release from all hydrogel blend arguably followed Korsmeyer-Peppas release kinetics with quasi-Fickian to non-Fickian release behaviour. The time required for 50% drug release and the hydrogel dissolution was proportional, indicating disintegration-controlled release rate. Reduced cubic-model based on the forward selection offered good agreement with experimental data (R2, 0.98 and adjusted R2 of 0.91). Optimal blend projection by the model with a mass ratio of 0.38:0.21:0.41 for PVA: Starch: citric acid was verified to be reasonably correct.



中文翻译:

从柠檬酸交联淀粉-PVA水凝胶膜中优化环丙沙星的释放:采用混合物设计建模

在设计亲水性药物的缓释制剂时,预测水凝胶混合物的最佳组成至关重要。在本研究中,通过依次添加聚乙烯醇(PVA)(20–95%w / w),淀粉(0–75%w / w),柠檬酸(0.25%w / w)制备了包含环丙沙星(0.2%w / w)的复合水凝胶。 5–80%w / w)作为热诱导糊化过程中的交联剂。采用受约束的单纯形混合物设计来合理化水凝胶组合物中成分的比例,同时模拟体外水凝胶中50%药物释放所需的时间条件。还对制得的水凝胶进行了溶胀率,抗张强度和抗微生物椎间盘扩散测定的表征。淀粉相对于PVA的比例降低会导致形成透明的水凝胶,并具有高度的平衡溶胀度(高达104%)。从所有水凝胶混合物中释放的药物可以说是遵循Korsmeyer-Peppas释放动力学,具有准Fickian到非Fickian的释放行为。50%药物释放和水凝胶溶解所需的时间成比例,表明崩解控制释放速率。基于正向选择降低立方模型提供了良好的协议与实验数据(R 2,0.98和调整后的R2 20.91)。通过模型对PVA:淀粉:柠檬酸的质量比为0.38:0.21:0.41的最佳混合预测被证明是合理正确的。

更新日期:2021-01-05
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