Spanlastics gel-A novel drug carrier for transdermal delivery of glimepiride.

IF 3.6 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Elsaied H Elsaied, Hamdy M Dawaba, El Sherbini A Ibrahim, Mohsen I Afouna
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引用次数: 3

Abstract

Glimepiride (3rd-generation sulfonylurea) is used for treatment of type 2 diabetes, but its oral administration has been associated with severe gastric disturbances such as nausea, vomiting, heartburn, anorexia, haemolytic anaemia. Accordingly, the transdermal route may represent a potentially suitable alternative. This work investigates the usefulness of a novel drug carrier system for transdermal application. The system investigated were called spanlastics gels and constituted span 60 with edge activator (tween 60 or tween 80). Spanlastics gel has been introduced as a stable form alternative to the liquid formulations of spanlastics. Spanlastics gels were prepared by coacervation phase separation method. Entrapment efficiency and size of spanlastics vesicles produced from the hydration of spanlastics gels were characterised. In vitro release and skin permeation of glimepiride from various spanlastics gel formulations were investigated across mixed cellulose membrane and excised rabbit skin. The obtained results indicated that the maximum entrapment efficiency was 65.36% when the tween 60 content was 30%. The drug release and permeation were increase as the concentration of edge activator increased. Spanlastics gel prepared with Tween 80 at concentration 50% showed higher permeability and flux value (248.69 µg/cm2and 8.31 µg/cm2.h, respectively) through rabbit skin.

一种新型格列美脲经皮给药载体。
格列美脲(第三代磺脲类药物)用于治疗2型糖尿病,但口服格列美脲会导致恶心、呕吐、胃灼热、厌食、溶血性贫血等严重的胃紊乱。因此,透皮途径可能是一种潜在的合适的替代方法。本研究探讨了一种新型药物载体系统在经皮应用中的有效性。所研究的体系被称为弹性体凝胶,由边缘活化剂(60或80之间)构成跨度60。介绍了一种可替代液体配方的稳定形式的塑料凝胶。采用聚守恒相分离法制备了塑料凝胶。研究了由塑料凝胶水化作用产生的塑料小泡的包封效率和大小。研究了不同塑料凝胶制剂格列美脲在混合纤维素膜和兔皮肤上的体外释放和皮肤渗透。结果表明,当tween 60含量为30%时,捕集效率最高为65.36%。随着边缘激活剂浓度的增加,药物的释放和渗透均增加。以50%浓度的吐温80制备的塑料凝胶通过兔皮肤的渗透率和通量值分别为248.69µg/cm2和8.31µg/cm2。
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来源期刊
Journal of Liposome Research
Journal of Liposome Research 生物-生化与分子生物学
CiteScore
10.50
自引率
2.30%
发文量
24
审稿时长
3 months
期刊介绍: The Journal of Liposome Research aims to publish original, high-quality, peer-reviewed research on the topic of liposomes and related systems, lipid-based delivery systems, lipid biology, and both synthetic and physical lipid chemistry. Reviews and commentaries or editorials are generally solicited and are editorially reviewed. The Journal also publishes abstracts and conference proceedings including those from the International Liposome Society. The scope of the Journal includes: Formulation and characterisation of systems Formulation engineering of systems Synthetic and physical lipid chemistry Lipid Biology Biomembranes Vaccines Emerging technologies and systems related to liposomes and vesicle type systems Developmental methodologies and new analytical techniques pertaining to the general area Pharmacokinetics, pharmacodynamics and biodistribution of systems Clinical applications. The Journal also publishes Special Issues focusing on particular topics and themes within the general scope of the Journal.
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