Medical University of Gdańsk, Division of Physical Chemistry, Hallera 107, 80-416 Gdańsk, Poland.
Mater Sci Eng C Mater Biol Appl. 2013 Oct;33(7):3942-50. doi: 10.1016/j.msec.2013.05.041. Epub 2013 May 25.
This study investigated the use of a novel particle-type formulation, composed of a sol-gel derived bioactive silica-poly(dimethylsiloxane) composite containing calcium and phosphate, as a slow release delivery system for an anticancer drug (doxorubicin hydrochloride, DOX). DOX in the solution form was in situ incorporated into the composite network during the sol-gel process. The DOX loaded-formulation was immersed in a simulated body fluid (SBF) having ion concentrations and a pH value nearly equal to those of human blood plasma. The effect of different drug loads and particle sizes - on the release profiles in such biomimetic conditions was studied. The bioactivity was examined in vitro with respect to the ability of hydroxyapatite layer to form on the surface of residual DOX-loaded formulation as a result of contact with SBF. The infrared absorption spectra, scanning electron microscopy, nitrogen gas adsorption/desorption, and X-ray powder diffraction studies were conducted before and after contact of the formulation with SBF. The results show that all the DOX-loaded formulations are characterized by mesoporosity with the uniform pore-size-distribution. The release profiles of DOX consisted of two sequential zero order-controlled stages with distinctly different release rates. After 20 days of DOX release, a semicrystalline carbonated hydroxyapatite with a highly developed porous structure was formed, indicative of their bioactive character. Furthermore, these new covered-particle-type formulations released DOX over 1 month at a constant rate.
本研究探讨了一种新型的颗粒型制剂的应用，该制剂由含有钙和磷的溶胶-凝胶衍生的生物活性硅-聚二甲基硅氧烷复合材料组成，作为一种抗癌药物（盐酸多柔比星，DOX）的缓释递送系统。DOX 以溶液形式在溶胶-凝胶过程中原位掺入复合网络中。将载有 DOX 的制剂浸入模拟体液（SBF）中，其离子浓度和 pH 值与人体血浆非常接近。研究了不同药物负载和粒径 - 在这种仿生条件下对释放曲线的影响。通过接触 SBF 后表面形成羟基磷灰石层的能力，从体外研究了生物活性。在与 SBF 接触前后进行了红外吸收光谱、扫描电子显微镜、氮气吸附/解吸和 X 射线粉末衍射研究。结果表明，所有载有 DOX 的制剂均具有中孔结构，且孔径分布均匀。DOX 的释放曲线由两个连续的零级控制阶段组成，释放速率明显不同。在 DOX 释放 20 天后，形成了具有高度发达的多孔结构的半晶碳酸羟基磷灰石，表明其具有生物活性。此外，这些新型覆盖颗粒型制剂以恒定的速率持续释放 DOX 1 个月以上。
