阿托伐酮智能脂质系统:设计,统计优化和体外评估

IF 4.6 Q1 CHEMISTRY, APPLIED Food Hydrocolloids for Health Pub Date : 2023-07-22 DOI:10.1016/j.fhfh.2023.100144
Hardik Rana, Drashti Patel, Vaishali Thakkar, Tejal Gandhi
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引用次数: 0

摘要

本研究旨在设计、开发和表征一种生物利用度不足的阿托伐醌(ATQ)的智能脂质系统。水溶性和溶解性差是生物利用度不足的主要制约因素。溶解度研究表明,Labrasol-ALF (L-ALF)、Tween 80和Trancutol®P (TP)分别被筛选为油脂、表面活性剂和助表面活性剂。通过拟三元图确定各成分的适宜用量,选择l-ALF: Tween 80: TP的比例为1:3:1。利用降落伞效应评价了沉淀抑制剂的效果。选择Soluplus®(SP)作为5%的沉淀抑制剂。采用石川图和定性风险评估筛选关键材料属性(cma)和关键工艺参数(CPPs)。采用d-最优配合比设计进行配方优化。将油量、表面活性剂和助表面活性剂作为自变量,而将球粒径、多分散性指数(PDI)和溶解度作为因变量。对设计批进行体外溶出度、PDI、zeta电位、微球大小等评价。利用叠加图确定最优区域。优化后的制剂在1 h内释药率为97.91%。zeta电位(-27.43 mV)和PDI(0.468)值表明该制剂具有较好的稳定性。探讨了降落伞效应对沉淀抑制剂选择的影响。SP能增加ATQ的溶解度,减少药物的沉淀。l-ALF、Tween、80和TP的添加量对SNEDDS的制备有显著影响。该配方新颖、有效、对患者友好、面向行业。
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Atovaquone smart lipid system: Design, statistical optimization, and in-vitro evaluation

The research was undertaken to design, develop and characterize the smart lipid system of an inadequate bioavailable Atovaquone (ATQ). The poor aqueous solubility and dissolution are the major constrain of inadequate bioavailability. The solubility study reveals that Labrasol-ALF (L-ALF), Tween 80, and Trancutol®P (TP) were screened as oil, surfactant, and co-surfactant, respectively. The pseudo ternary diagram was constructed to locate the appropriate amount of each ingredient, and a 1:3:1 ratio of l-ALF: Tween 80: TP was chosen. The effect of precipitation inhibitor was assessed using the parachute effect. Soluplus® (SP) was chosen as a precipitation inhibitor at 5%. Ishikawa diagram and qualitative risk assessment were performed to screen the critical material attributes (CMAs) and critical process parameters (CPPs). d-optimal mixture design was explored for the optimization of the formulation. The amount of oil, surfactant, and co-surfactant was screened as independent variables, whereas globule size, poly-dispersibility index (PDI), and solubility were designated dependent variables. The design batches were evaluated for the in-vitro dissolution rate, PDI, zeta potential, globule size, etc. The optimal region was located using an overlay plot. The optimized formulation has shown a 97.91% drug release within 1 h. The value of zeta potential (-27.43 mV) and PDI (0.468) indicates the stability of the formulation. The parachute effect had explored for the selection of precipitation inhibitors. SP was able to increase the solubility of ATQ and reduce the precipitation of the drug. The amount of l-ALF, Tween, 80and TP was significant for the formulation of SNEDDS. The formulation was novel, effective, patient-friendly, and industry oriented.

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CiteScore
4.50
自引率
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审稿时长
61 days
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