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Synthesis and evaluation of luliconazole loaded biodegradable nanogels prepared by pH-responsive Poly (acrylic acid) grafted Sodium Carboxymethyl Cellulose using amine based cross linker for topical targeting: In vitro and Ex vivo assessment
Polymer-Plastics Technology and Materials ( IF 2.7 ) Pub Date : 2020-05-06 , DOI: 10.1080/25740881.2020.1759633
Rahul L. Rajput 1 , Jitendra S. Narkhede 1 , Arun Mujumdar 2 , Jitendra B. Naik 1
Affiliation  

Fungal infection in immuno compromised patients causes skin syndromes and problems. At Present, innovative alternatives are required to cure skin disorders and infections. Luliconazole is a novel, broad spectrum, imidazole antifungal agent. The purpose of this study was to develop biodegradable, pH responsive, chemically cross-linked and Poly (acrylic acid) grafted sodium carboxymethyl cellulose nanogels. Nanogels had been synthesized to evaluate its applicability as an effective carrier of luliconazole for topical (skin) targeting. Chemically cross-linked sodium carboxymethyl cellulose-grafted-Poly acrylic acid (NaCMC-g-PAA) was synthesized from acrylic acid and sodium carboxymethyl cellulose using N, N’-methylene bisacrylamide (cross-linker) and potassium persulfate (initiator) using free radical polymerization. Variation of reaction parameters such as pH, cross linker, initiator and temperature has been used to optimize the best one. The developed nanogels reveal significant pH sensitive drug releasing behavior. NaCMC-g-PAA nanogels has been characterized using various physicochemical characterization techniques. Nanogels characteristics were evaluated through the In vitro drug release, Ex vivo permeation study, Nuclear magnetic resonance spectroscopy, Fourier Transform Infrared Spectroscopy, Field Emission Scanning Electron Microscope, Stability Study and antifungal activity. All batches were characterized for particle size analysis and ranged from 78.82 nm to 190 nm. The viscosity of developed nanogels was found to be 5941 cps. It was observed that the developed drug-loaded NaCMC-g-PAA nanogels were more effective in killing the fungus. Consequently, Nanogels incorporated with luliconazole could be a new approach with improved antifungal activity and increased topical delivery for a drug with poor aqueous solubility rather than coarse drug-containing cream.



中文翻译:

pH响应的聚丙烯酸丙烯酸接枝羧甲基纤维素钠制备的负载卢立康唑的可生物降解纳米凝胶的合成和评估,使用胺基交联剂进行局部靶向:体外和离体评估

免疫受损患者的真菌感染会导致皮肤综合症和问题。目前,需要创新的替代品来治疗皮肤疾病和感染。卢立康唑是一种新型的,广谱的咪唑类抗真菌剂。这项研究的目的是开发可生物降解,pH响应,化学交联和聚(丙烯酸)接枝的羧甲基纤维素钠纳米凝胶。已经合成了纳米凝胶以评估其作为卢立康唑用于局部(皮肤)靶向的有效载体的适用性。使用N,N'-亚甲基双丙烯酰胺(交联剂)和过硫酸钾(引发剂),由丙烯酸和羧甲基纤维素钠由丙烯酸和羧甲基纤维素钠合成化学交联的羧甲基纤维素钠接枝聚丙烯酸(NaCMC-g-PAA)。自由基聚合。反应参数的变化(例如pH值,交联剂,引发剂和温度)已用于优化最佳反应参数。已开发的纳米凝胶显示出显着的pH敏感药物释放行为。NaCMC-g-PAA纳米凝胶已使用多种物理化学表征技术进行了表征。纳米凝胶的特性通过体外药物释放,离体渗透研究,核磁共振波谱,傅立叶变换红外光谱,场发射扫描电子显微镜,稳定性研究和抗真菌活性。对所有批次进行表征以进行粒度分析,范围为78.82 nm至190 nm。发现已开发的纳米凝胶的粘度为5941 cps。观察到,开发的载有药物的NaCMC-g-PAA纳米凝胶在杀死真菌方面更有效。因此,掺入卢立康唑的纳米凝胶可能是一种新的方法,具有改善的抗真菌活性并增加了水溶性较差的药物(而不是含有粗糙药物的乳膏)的局部递送。

更新日期:2020-05-06
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