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Formulation, in-vitro and in-vivo pharmacokinetic evaluation of simvastatin nanostructured lipid carrier loaded transdermal drug delivery system
Future Journal of Pharmaceutical Sciences Pub Date : 2019-12-05 , DOI: 10.1186/s43094-019-0008-7 S Brito Raj , Kothapalli Bonnoth Chandrasekhar , Kesavan Bhaskar Reddy
Future Journal of Pharmaceutical Sciences Pub Date : 2019-12-05 , DOI: 10.1186/s43094-019-0008-7 S Brito Raj , Kothapalli Bonnoth Chandrasekhar , Kesavan Bhaskar Reddy
A simvastatin nanostructured lipid carrier loaded transdermal patch was developed to enhance the bioavailability and therapeutic effect. Simvastatin NLC preparation was prepared by optimized hot homogenization technique and were characterized by particle size in nanometer, polydispersity index, zeta potential in millivolt, scanning electron microscopy, and entrapment efficiency by applying Box Behnken design utilizing multiple linear regression method. Chosen optimized NLC F7 formulation has particle size of 125.4 ± 2.66 nm, zeta potential of − 33.6 ± 2.42 mV, and PI of 0.480 ± 0.24. The NLC was loaded in transdermal patch by solvent evaporation method and evaluated for physical characteristics, drug content, skin permeation studies, and in-vivo pharmacokinetic studies in male albino Wistar rat. In-vivo pharmacokinetic studies in NLC loaded transdermal patch show an increase in AUC0-α in mg/ml when compared to marketed oral dosage form, which confirms the enhancement of bioavailability of simvastatin by NLC loaded transdermal patch. From the data, it was concluded that drug-loaded NLC transdermal patch will be a promising drug delivery system for poorly bioavailable drugs.
中文翻译:
载有辛伐他汀纳米结构脂质载体的透皮给药系统的配制,体外和体内药代动力学评估
开发了辛伐他汀纳米结构脂质载体负载的透皮贴剂,以提高生物利用度和治疗效果。辛伐他汀NLC的制备是通过优化的热均质技术制备的,其特征在于通过应用Box Behnken设计(采用多元线性回归方法),以纳米级粒径,多分散指数,毫伏级ζ电势,扫描电子显微镜和包封效率为特征。选择的经过优化的NLC F7配方的粒径为125.4±2.66 nm,ζ电势为-33.6±2.42 mV,PI为0.480±0.24。通过溶剂蒸发法将NLC装在透皮贴剂中,并对雄性白化病Wistar大鼠的物理特性,药物含量,皮肤渗透性研究和体内药代动力学研究进行评估。与市售口服剂型相比,在装有NLC的透皮贴剂中进行体内药代动力学研究表明,AUC0-α的单位为mg / ml,这证实了装有NLC的透皮贴剂可提高辛伐他汀的生物利用度。从数据得出的结论是,载有药物的NLC透皮贴剂对于生物利用度较差的药物将是一种有希望的药物递送系统。
更新日期:2019-12-05
中文翻译:
载有辛伐他汀纳米结构脂质载体的透皮给药系统的配制,体外和体内药代动力学评估
开发了辛伐他汀纳米结构脂质载体负载的透皮贴剂,以提高生物利用度和治疗效果。辛伐他汀NLC的制备是通过优化的热均质技术制备的,其特征在于通过应用Box Behnken设计(采用多元线性回归方法),以纳米级粒径,多分散指数,毫伏级ζ电势,扫描电子显微镜和包封效率为特征。选择的经过优化的NLC F7配方的粒径为125.4±2.66 nm,ζ电势为-33.6±2.42 mV,PI为0.480±0.24。通过溶剂蒸发法将NLC装在透皮贴剂中,并对雄性白化病Wistar大鼠的物理特性,药物含量,皮肤渗透性研究和体内药代动力学研究进行评估。与市售口服剂型相比,在装有NLC的透皮贴剂中进行体内药代动力学研究表明,AUC0-α的单位为mg / ml,这证实了装有NLC的透皮贴剂可提高辛伐他汀的生物利用度。从数据得出的结论是,载有药物的NLC透皮贴剂对于生物利用度较差的药物将是一种有希望的药物递送系统。