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Physicochemical studies of carrier systems for peptide drug delivery.

机译：肽药物递送载体系统的理化研究。

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摘要

Polystyrene and dextran microspheres were investigated as model carriers for small molecular weight peptide drug delivery systems.;Polystyrene was characterized by particle sizing, atomic force microscopy (AFM), surface area measurements, and surface charge density. AFM topographical images of polystyrene depicted a highly irregular surface with crater-like depressions (d ;The adsorption and desorption characteristics of lysine vasopressin, a model nonapeptide, at polystyrene surfaces were studied as functions of pH, ionic strength, dilution volume, and surface tension. Adsorption occurred by hydrophobic and electrostatic interactions and was greatest in the region of the isoelectric point. Although no single parameter provided complete desorption, partial desorption occurred at pH values away from the isoelectric point, at low ionic strengths, and at low surface tensions. AFM images of polystyrene in the presence of lysine vasopressin showed surface irregularities which were quite different from those of the polystyrene surface itself.;Initial feasibility studies of dextran delivery systems utilized procaine hydrochloride as an inexpensive substitute for lysine vasopressin due to the higher loading capacity of dextrans compared to that of polystyrene. Procaine was sorbed or entrapped within the internal dextran matrices. Content uniformity improved as the procaine solution volume approached the liquid saturation level of the dextran particles. Drug release occurred rapidly and completely following immersion in aqueous media. Polymer coating of the procaine-loaded dextrans with hydroxypropyl methylcellulose phthalate (HPMCP) by coacervation did not provide adequate enteric properties. The coating process was evaluated by scanning electron microscopy and by "calcium-labeled" HPMCP with energy dispersive spectroscopy (EDS). EDS probing at various locations on several dextran particles gave calcium peaks indicating the presence of the coating. Based on release studies from coated dextrans, the coating was not sufficiently thick to provide enteric properties.
机译：研究了聚苯乙烯和右旋糖酐微球作为小分子量肽药物递送系统的模型载体。聚苯乙烯的特征在于粒径，原子力显微镜（AFM），表面积测量和表面电荷密度。聚苯乙烯的AFM地形图描绘了一个高度不规则的表面，具有凹坑状的凹陷（d;研究了赖氨酸加压素（一种非肽模型）在聚苯乙烯表面的吸附和解吸特性，其与pH，离子强度，稀释体积和表面张力的关系吸附是通过疏水和静电相互作用发生的，并且在等电点范围内最大，尽管没有单个参数提供完全的解吸，但是在远离等电点的pH值，低离子强度和低表面张力下发生了部分解吸。赖氨酸加压素存在下的聚苯乙烯的AFM图像显示表面不规则性与聚苯乙烯表面本身的不规则性有很大差异。；右旋糖酐递送系统的初步可行性研究使用盐酸普鲁卡因作为赖氨酸加压素的廉价替代品，因为它具有较高的负载能力。 dextrans与polysty的比较勒内。普鲁卡因被吸收或截留在内部葡聚糖基质中。当普鲁卡因溶液的体积接近右旋糖酐颗粒的液体饱和水平时，含量均匀性得到改善。浸入水性介质后，药物释放迅速而完全。通过凝聚作用用羟丙基甲基纤维素邻苯二甲酸酯（HPMCP）对普鲁卡因负载的右旋糖酐进行聚合物包衣不能提供足够的肠溶性。通过扫描电子显微镜和通过具有能量色散光谱法（EDS）的“钙标记的” HPMCP评估涂覆过程。在几种葡聚糖颗粒的不同位置进行EDS探测，发现钙峰表明了涂层的存在。基于包衣的右旋糖酐的释放研究，包衣的厚度不足以提供肠溶特性。

著录项

  • 作者

    Grandolfi, George Paul.;

  • 作者单位

    The Ohio State University.;

  • 授予单位 The Ohio State University.;
  • 学科 Pharmaceutical sciences.;Pharmacy sciences.
  • 学位 Ph.D.
  • 年度 1991
  • 页码 183 p.
  • 总页数 183
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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