负载鲁立康唑的Niosol局部凝胶:因子设计、体外表征和抗真菌研究

IF 0.8 4区 医学 Q3 EDUCATION, SCIENTIFIC DISCIPLINES Indian Journal of Pharmaceutical Education and Research Pub Date : 2023-08-23 DOI:10.5530/ijper.57.3s.60
N. Shah, R. Prajapati, D. Gohil, C. Aundhia, Piyushkumar Sadhu, S. Kardani
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引用次数: 0

摘要

目的/背景:本研究旨在利用乳小体的潜在优势,改善难溶性露立康唑的外用给药。材料与方法:以聚合物卡波波尔934为原料,成功制备了用于治疗真菌感染的抗真菌药物Luliconazole。采用32全因子统计设计对乳质体配方进行优化,考察胆固醇浓度和span 60两个配方因素对乳质体配方中药物释放率和药物包封率两个因变量的影响。结果:优化处方的平均囊泡大小为150.6±11.1 nm, Zeta电位为-23.5±5.08 nm,释药效率为92.41±2.44%,包封效率为92.36±2.85%。扫描电镜研究表明,优化后的配方为球形、多孔且表面粗糙。差示扫描量热法研究表明,该药物可溶解或转化为无定形在乳质体囊泡。乳质体凝胶的黏度和涂抹性良好,便于外用。体外实验表明,优化后的乳质体凝胶释药率(97.31±3.18%)显著高于市售产品(82.20±1.95%)。抗真菌研究表明,niosomal gel与传统的市售制剂相比具有相当的抗真菌效果。结论:由此可见,负载乳质体的露立康唑外用凝胶可能有助于减少常规外用产品的使用频率,从而提高患者的依从性。
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Luliconazole Loaded Niosomal Topical Gel: Factorial Design, in vitro Characterization and Antifungal Study
Aim/Background: This research work intended to make use of prospective advantages of niosomes for the improvement in topical delivery of poorly soluble luliconazole. Materials and Methods: Luliconazole, an anti-fungal agent used in the treatment of fungal infection, was successfully formulated as niosomal topical gel by using a polymer carbopol 934. The 3 2 full factorial statistical design was employed as a means for the optimization of niosomal formulation to check the impact of two formulation factors namely, concentration of cholesterol and span 60 on two dependent variables % drug release and % drug entrapment efficiency in formulated niosomal formulations. Results: The mean vesicular size, Zeta potential, drug release and entrapment efficiency of optimized formulation was found 150.6 ± 11.1 nm, -23.5 ± 5.08, 92.41 ± 2.44% and 92.36 ± 2.85%, respectively. The scanning electron microscopy study reveals that the optimized formulation was spherical, porous and rough in surface. The thermogram of differential scanning calorimetry study states that the drug may be solubilise or converted to amorphous form in niosomal vesicles. The viscosity and spreadability of niosomal gel were observed satisfactorily for the easy topical application. The ex vivo study of optimized niosomal gel showed significant higher drug release (97.31 ± 3.18%) in comparison with marketed product (82.20 ± 1.95%). The antifungal study showed considerable antifungal effectiveness of niosomal gel against the conventional marketed preparation. Conclusion: Henceforth, it can be concluded that the niosomes loaded topical gel of luliconazole may be useful for reducing the application frequency of conventional topical product and thereby improves the patient compliance.
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来源期刊
CiteScore
1.40
自引率
0.00%
发文量
227
审稿时长
>12 weeks
期刊介绍: The official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967. IJPER, a quarterly publication devoted to publish reviews and research articles in pharmacy and the related disciplines of Pharmaceutical education. It mainly covers the articles of special interest, covering the areas of Pharmaceutical research, teaching and learning, laboratory innovations, education technology, curriculum design, examination reforms, training and other related issues. It encourages debates and discussions on the issues of vital importance to Pharmaceutical education and research. The goal of the journal is to provide the quality publications and publish most important research and review articles in the field of drug development and pharmaceutical education. It is circulated and referred by more than 6000 teachers, 40,000 students and over 1000 professionals working in Pharmaceutical industries, Regulatory departments, hospitals etc.
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