Centrifugally spun ultrafine starch/PEO fibres as release formulation for poorly water-soluble drugs

Micro & nano letters

article

Xianglong Li¹  Yishen Lu¹  Teng Hou¹  Jing Zhou¹  Bin Yang¹ 

[1] National Engineering Laboratory for Textile Fiber Materials and Processing Technology, College of Materials and Textiles, Zhejiang Sci-Tech University

关键词: drug delivery systems;    nanofabrication;    nanomedicine;    membranes;    biomedical materials;    ibu-loaded fibrous membranes;    ket-loaded fibrous membranes;    fibre-based delivery systems;    water-soluble drugs;    drug formulations;    in-vitro drug release tests;    drug-loaded ultrafine starch-PEO fibres;   

DOI  :  10.1049/mnl.2018.5267

学科分类：计算机科学（综合）

来源: Wiley

【 摘 要 】

The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1b-d), containing a Schiff base or a sulfonamido moiety, showed reasonable activity and were less potent than cephalexin with respect to E. coli and Staph. aureus. The new cephalosporins (series 2) showed remarkable activities on E. coli (62.5-15.6µg/ml) and staph. aureus (31.2-62.5µg/ml) when compared with cephalexin (250 and 125 µg/ml) respectively. Moreover, compounds 1 and 3 showed very promising activity against MRSA (250 and 500µg/ml) respectively. The incorporation of a sulfonamido moiety to the cephalosporin molecule was successfully achieved. This is a very interesting finding which may open a new approach in the synthesis of newer cephalosporins.

【 授权许可】

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