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Optimization and in-vivo evaluation of isradipine nanoparticles using Box-Behnken design surface response methodology

机译:使用Box-Behnken设计表面响应方法对伊拉地平纳米粒子进行优化和体内评估

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The isradipine is the potent anti hypertensive drug, which is matrix in polymeric nanoparticle by using solvent evaporation method. In this work, 3-factor, 3-level Box-Behnken design was used to optimize the process parameters like polymer concentration (A), sonication frequency (B) and sonication time (C). Three dependent variable’s particle size, entrapment efficiency and practical yield were measured as responses. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The optimization model of particle size of 343.14 nm, entrapment efficiency of about 83.74% and practical yield of 85.39% with A, B and C levels of 750 mg, 37.5 min and 40 kHz respectively. The observed responses were in close agreement with the predicted values of the optimized process. The prepared nanoparticle was characterized by Fourier transform infrared spectroscopy, morphological studies and in-vitro drug release studies. The prepared nanoparticle was showed good sustained release of drug upto 24 h. The anti-hypertensive study was performed on animal model. The PMMA (Poly-Methyl-Metha- Acrylate) isradipine nano particle shows fall in blood pressure was delayed and reach 152±2 mmHg at 1 h. The action was sustained until prolong period. Based on pharmacokinetic and pharmacodynamics parameter, the isradipine nanoparticles shows better bioavailability compare with solution form. Graphical abstract Display Omitted Highlights ? Isradipine is a potent hypertensive drug. ? Isradipine nanoparticle preparation was optimized by 3-level factorial design. ? 3-factor, 3-level Box-Behnken design. ? Independent variables like polymer concentration, sonication frequency and sonication time. ? Dependent variables like particle size, entrapment efficiency and practical yield.
机译:伊拉地平是一种有效的抗高血压药,通过溶剂蒸发法在聚合物纳米颗粒中形成基质。在这项工作中,使用三因素,三级Box-Behnken设计来优化工艺参数,例如聚合物浓度(A),超声处理频率(B)和超声处理时间(C)。测量了三个因变量的粒径,截留效率和实际收率作为响应。数学方程和响应面图用于关联因变量和自变量。 A,B和C含量分别为750 mg,37.5 min和40 kHz时,粒径为343.14 nm,包封率约为83.74%和实际产率为85.39%的优化模型。观察到的响应与优化过程的预测值非常一致。通过傅立叶变换红外光谱,形态学研究和体外药物释放研究来表征所制备的纳米颗粒。制备的纳米颗粒在24小时内显示出良好的药物持续释放。在动物模型上进行了抗高血压研究。 PMMA(聚甲基丙烯酸甲酯)丙烯酸异拉平纳米颗粒显示血压下降延迟并在1 h达到152±2 mmHg。该行动一直持续到很长时间。根据药代动力学和药效学参数,异拉地平纳米颗粒与溶液形式相比具有更好的生物利用度。图形摘要显示省略的突出显示?伊拉地平是一种有效的高血压药物。 ?通过三级因子设计优化了伊拉地平纳米颗粒的制备。 ? 3因子3级Box-Behnken设计。 ?独立变量,例如聚合物浓度,超声处理频率和超声处理时间。 ?因变量,例如粒度,截留效率和实际收率。

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