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使用不同载体优化醋氯芬酸前体脂质体,第1部分:研制与表征

Optimization of Aceclofenac Proniosomes by Using Different Carriers, Part 1: Development and Characterization.

作者信息

Sammour Rana M F, Taher Muhammad, Chatterjee Bappaditya, Shahiwala Aliasgar, Mahmood Syed

机构信息

Pharmaceutical Technology Department, Kulliyyah of Pharmacy, International Islamic University Malaysia, Kuantan 25200, Pahang, Malaysia.

Pharmaceutics Department, Dubai Pharmacy College for Girls, Dubai, UAE.

出版信息

Pharmaceutics. 2019 Jul 18;11(7):350. doi: 10.3390/pharmaceutics11070350.

Abstract

In the contemporary medical model world, the proniosomal system has been serving as a new drug delivery system that is considered to significantly enhance the bioavailability of drugs with low water solubility. The application of this system can improve the bioavailability of aceclofenac that is used for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. The present study is intended to develop an optimized proniosomal aceclofenac formula by the use of different carriers. Aceclofenac proniosomes have been prepared by slurry method, and different carriers such as maltodextrin, mannitol, and glucose were tried. Prepared proniosomes characterized by differential scanning calorimetry (DSC) analysis and Fourier transform infrared (FTIR) analysis revealed the compatibility of the drug chosen with the ingredient added, powder X-ray diffractometry (XRD) confirmed the amorphous phase of the prepared proniosomes, and finally, the surfactant layer was observed by scanning electron microscopy (SEM). Aceclofenac physical state transformations were confirmed with all formulas but maltodextrin proniosomes exhibited solubility more than other formulations. HPLC method has been used to analyze the niosomes derived from proniosomes in terms of their entrapment capability and drug content. The obtained results revealed that aceclofenac proniosomes can be successfully prepared by using different carriers.

摘要

在当代医学模式的背景下,前体脂质体系统一直作为一种新型药物递送系统,被认为能显著提高低水溶性药物的生物利用度。该系统的应用可提高用于缓解骨关节炎、类风湿性关节炎和强直性脊柱炎疼痛与炎症的醋氯芬酸的生物利用度。本研究旨在通过使用不同载体开发一种优化的醋氯芬酸前体脂质体配方。已采用乳化法制备了醋氯芬酸前体脂质体,并尝试了不同的载体,如麦芽糊精、甘露醇和葡萄糖。通过差示扫描量热法(DSC)分析和傅里叶变换红外光谱(FTIR)分析对制备的前体脂质体进行表征,结果显示所选药物与添加成分具有相容性,粉末X射线衍射(XRD)证实了所制备前体脂质体的非晶相,最后通过扫描电子显微镜(SEM)观察了表面活性剂层。所有配方均证实了醋氯芬酸的物理状态转变,但麦芽糊精前体脂质体的溶解度高于其他配方。已使用高效液相色谱(HPLC)法分析从前体脂质体衍生的脂质体的包封能力和药物含量。所得结果表明,使用不同载体可成功制备醋氯芬酸前体脂质体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba38/6680652/cd278f137a26/pharmaceutics-11-00350-g001a.jpg

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