• a smart micellar system with an amine-containing polycarbonate shell

    جزئیات بیشتر مقاله
    • تاریخ ارائه: 1392/01/01
    • تاریخ انتشار در تی پی بین: 1392/01/01
    • تعداد بازدید: 844
    • تعداد پرسش و پاسخ ها: 0
    • شماره تماس دبیرخانه رویداد: -
     the present paper reports the design and preparation of an amphiphilic triblock co-polymer poly(ε-caprolactone) (pcl)–poly(6,14-dimethyl-1,3,9,11-tetraoxa-6,14-diaza-cyclohexadecane-2,10-dione) (padmc)–pcl and the use of micelles composed of them as carriers for ph-sensitive drug release. the triblock co-polymers were synthesized via two-step ring-opening polymerization with catalysis by novozym-435 lipase. by adjusting the feed ratio, three co-polymers with different pcl lengths and the same padmc length were produced. the block structure of the co-polymers obtained was confirmed by comparative studies on pcl–padmc–pcls and the corresponding random poly(ε-caprolactone-random-6,14-dimethyl-1,3,9,11-tetraoxa-6,14-diaza-cyclohexadecane-2,10-dione (poly(cl-r-admc)) by means of nuclear magnetic resonance and differential scanning calorimetry. cell cytotoxicity tests showed that the co-polymer displayed no apparent cytotoxicity to 293t and hela cells. transmissions electron microscopy indicates that the self-assembled micelles exhibited a well-defined spherical shape with a diameter between ∼30 and 50 nm. the critical aggregation concentration was dependent on the block composition. due to the presence of ionizable tertiary amine groups in the padmc block, acid-induced variation in the micellar morphology was evident with respect to micelle size and size distribution. the size–ph curve was characterized by a smooth sigmoid form, and had a dramatic upward shift with decreasing ph from 6.5 to 4.5, which correlated well with the buffer range of hydrophilic padmc. as a demonstration of the potential of pcl–padmc–pcl micelles to control drug delivery, acid induced drug release for prednisone acetate-loaded micelles was explored. pcl–padmc–pcl micelles show good promise as smart drug carriers, sensing the local specific ph decrease around lesion sites.

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