聚(醚-酐)凝胶性能的优化及用于包载难溶性药物的研究

Studies on the Property Opetimization of Poly(ether-anhydride) Gels and the Application for Delivery of Hydrophobic Drugs

在制备聚醚酐凝胶的基础上,用两种不同的可光交联疏水性单体与聚醚酐大分子单体在紫外光引发下制备三维交联凝胶,使得凝胶的溶胀性能和亲-疏水性能发生变化,从而影响凝胶与难溶性药物的相容性;选用吲哚美辛为模型药物,通过后包合法将其包载于凝胶网络中,X射线衍射(XRD)检测结果表明,药物能以分子或无定形态分散于其中,优化后的凝胶可得到更高的载药量和包封率,能有效地提高疏水性药物的溶出度,且药物体外释放速率与单纯聚醚酐凝胶相比,被有效延缓,更适于临床应用.

On the basis of the preparation of poly （ether-anhydride） gels, two synthesized photocrosslinkable hydrophobic monomers were added respectively to copolymerize with poly （ether-anhydride） macromers under UV irradiation to form crosslinked gel networks. Accordingly, swelling capacity and hydrophilicity/hydrophobicity of gels were modified and the compatibility between hydrophobic drugs and gels was regulated. The hydrophobic drug indomathecin was post-loaded in the gel networks as a model drug, which was proved to be distributed in an amorphous or molecular state by employing X-ray diffraction. It was tested that the drug loading and encapsulation efficacy in the modified gels were increased, and the dissolution rate from the gels was effectively improved. Compared to the pure poly （ether-anhydride） gels, in vitro drug release behavior from the modified gels was delayed and more suitable for clinical application.