Development and evaluation of Nanostructured Lipid Carrier (NLC) based topical delivery of an anti-inflammatory drug

Atul Anand Phatak , Praveen Digambar Chaudhari
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引用次数: 32

Abstract

Aims

The work is aimed to formulate aqueous nanodispersion of aceclofenac Nanostructured Lipid Carriers (NLC) by using modified hot sonication method and to prepare NLC based gel for topical delivery of aceclofenac.

Methods

The lipids incorporated in the study were Compritol 888 ATO and Miglyol and the emulsifier/stabilizer used was Polysorbate 80. The formulations were optimized by using 3 factor, 3 levels, Box–Behenken design. The independent variables were combination of lipids (% w/w), concentration of emulsifier (% w/v), lipid drug ratio and the response variables were particle size, percentage entrapment and drug release after 12 h. The formulations were also characterized for particle size, entrapment efficiency, drug loading and depression in melting point.

Results

The DSC, FTIR analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by SEM which showed spherical shape of the formulations. Further the formulations were evaluated for in vitro drug permeability study, rheological properties, skin irritation, pharmacodynamic and stability studies.

Conclusion

The pharmacodynamic characteristics of aceclofenac NLC gel with reference to the conventional gel were compared by using Carrageenan induced rat paw edema method. The study showed the promising and stable alternative form for the aceclofenac for topical application.

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基于纳米结构脂质载体(NLC)的抗炎药物局部递送的开发和评价
目的采用改进的热超声方法制备乙酰氯芬酸纳米结构脂质载体(NLC)的水相分散体,并制备以NLC为基础的醋酸氯芬酸外用凝胶。方法本研究采用的脂类为Compritol 888 ATO和Miglyol,乳化剂/稳定剂为聚山梨酯80。采用3因素3水平Box-Behenken设计对配方进行优化。自变量为脂质组合(% w/w)、乳化剂浓度(% w/v)、脂质药物比,响应变量为粒径、包封率和12 h后药物释放量,并对其粒径、包封效率、载药量和熔点降低进行表征。结果DSC、FTIR分析表征了药物和脂质修饰的状态。通过扫描电镜对配方的形状和表面形貌进行了测定,结果表明配方为球形。进一步对制剂进行了体外药物渗透性研究、流变学特性、皮肤刺激、药效学和稳定性研究。结论采用卡拉胶诱导大鼠足部水肿法,比较了乙酰氯芬酸NLC凝胶与常规凝胶的药效学特性。研究结果表明,乙酰氯芬酸外用的替代剂型具有良好的应用前景和稳定性。
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