| 摘要 |
<p>The invention relates to a passive solid tumor-targeted anticancer prodrug and a preparation method thereof, belonging to the field of antitumor drugs. The preparation method comprises the following steps: reacting small molecular pectin with Mw of 5,000 - 45,000 with doxorubicin to obtain a pectin-doxorubicin conjugate with Mw of 100,000 - 1,000,000, preparing the conjugate into a suspension, and treating the suspension in an ultra-high pressure nano homogenizer to obtain the passive solid tumor-targeted anticancer prodrug with particle size of 100nm - 200nm and melting point of 220 - 245°C, wherein the pectin and doxorubicin are linked by an amide bond, and the pectin is linked by an ester bond formed by condensing carboxyl groups and hydroxyl groups of pectin molecules. Cell inhibition rate of the anticancer prodrug for humanized lung cancer cells NCI-H446 and A549 is equivalent to that of doxorubicin hydrochloride. In the efficacy research of melanoma B16 pulmonary metastasis model mice, the life span of tumor-bearing mice is 42.3±12.4 days, which is remarkably higher than that of the doxorubicin hydrochloride group (23.1±10.2 days).</p> |
