酮洛芬经皮给药纳米结构脂质载体的开发与评价

Q3 Pharmacology, Toxicology and Pharmaceutics
Thulasi Sathyanarayana, P. Sudheer, E. Jacob, Merlin Mary Sabu
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引用次数: 0

摘要

目的:酮洛芬是一种非甾体抗炎药(NSAID),当通过口服途径给药时显示出明显的胃肠道副作用,并且具有低皮肤渗透特征。本研究的目的是利用纳米结构脂质载体(NLCs)作为酮洛芬透皮递送的载体系统。方法:以蜂蜡、巴西棕榈蜡、单硬脂酸甘油(固体脂质)、亚麻籽油(液体脂质)和poloxamer188(表面活性剂)为原料,采用热均质技术制备NLCs,并通过JMP进行定制设计优化。评价反应包括药物包封效率、粒径和药物释放谱。利用方差分析对实验设计进行模型拟合评价。采用粒径、zeta电位、扫描电镜(SEM)、DSC、FTIR等指标对最佳配方进行了表征,并对其含量、包封效率、体外释放、体内释放谱进行了研究。结果:药物包埋范围为34±0.03 ~ 95.06±0.01%。在24小时的研究中发现,制剂的药物释放率为80%±0.09至95%±0.06。最大可取性为0.91。最佳配方的平均粒径为425.8nm, zeta电位为-45mV。扫描电镜结果显示,颗粒轻微团聚,表面不均匀。与纯药物贴片相比,NLC优化贴片的体外皮肤渗透通量和渗透系数更高,上市凝胶(2.5%w/w)的FTIR光谱保证了化学和物理相容性。结论:酮洛芬经NLCs经皮给药是一种改善皮肤透性的有效途径。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Nanostructured Lipid Carriers for Transdermal Delivery of Ketoprofen
Purpose: Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) which when administered via an oral route displays significant gastro-intestinal side effects and has low skin permeation profile. The objective of the present work is to utilise nanostructured lipid carriers (NLCs) as carrier system for transdermal delivery of ketoprofen. Methods: NLCs were prepared via hot homogenisation technique using bees wax, carnauba wax, glycerl monostearate (solid lipids), linseed oil (liquid lipid) and poloxamer188 (surfactant) and optimized using custom design via JMP. The responses evaluated were drug entrapment efficiency, particle size and drug release profile. The experimental design was evaluated for model fit with the assistance of ANOVA. The optimum formulations were characterized for particle size, zeta potential, SEM, DSC, FTIR and also drug content, entrapment efficiency, in- vitro drug release, ex-vivo drug release profile was studied. Results: The drug entrapment in the range of 34±0.03-95.06±0.01%. The drug release from the formulations over a 24 h study was found to be 80%±0.09 to 95%±0.06. The maximum desirability was found to be 0.91. The optimum formulation showed mean particle size of 425.8nm and a zeta potential of -45mV. SEM results revealed slightly agglomerated particles with uneven surfaces. The ex-vivo skin permeation of NLC optimized patch formulation exhibited a higher flux and permeability coefficient in comparison to the pure drug patch formulation and marketed gel (2.5%w/w) FTIR spectra assured the chemical and physical compatibility. Conclusion: Transdermal delivery of ketoprofen via NLCs would be a promising approach for improving the skin permeation.
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来源期刊
Fabad Journal of Pharmaceutical Sciences
Fabad Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.80
自引率
0.00%
发文量
12
期刊介绍: The FABAD Journal of Pharmaceutical Sciences is published triannually by the Society of Pharmaceutical Sciences of Ankara (FABAD). All expressions of opinion and statements of supposed facts appearing in articles and/or advertisiments carried in this journal are published on the responsibility of the author and/or advertiser, anda re not to be regarded those of the Society of Pharmaceutical Sciences of Ankara. The manuscript submitted to the Journal has the requirement of not being published previously and has not been submitted elsewhere. Manuscripts should be prepared in accordance with the requirements specified as given in detail in the section of “Information for Authors”. The submission of the manuscript to the Journal is not a condition for acceptance; articles are accepted or rejected on merit alone. All rights reserved.
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