Department of Radiology, Vancouver General Hospital, University of British Columbia, JP Pavilion G873, 855 West 12th Avenue, Vancouver V5Z 1M9, British Columbia, Canada.
J Vasc Interv Radiol. 2011 Mar;22(3):361-8. doi: 10.1016/j.jvir.2010.11.032.
To examine the loading and elution behavior of doxorubicin and superabsorbent polymer microspheres (SAP-MS) as they relate to particle size and loading techniques.
SAP-MS, 30-60 μm and 50-100 μm, were subject to loading 50 mg of doxorubicin from a dry lyophilized state. Doxorubicin loading was performed after prehydration of SAP-MS (one-step method) or serially in two divided administrations (two-step method). Loading rate and elution characteristics were determined after doxorubicin analysis using a high-pressure liquid chromatography (HPLC) assay. All experiments were performed in triplicate.
All systems showed the ability to load and elute doxorubicin effectively in the specified time frame (loading 15 minutes to 2 hours and elution 1 hour to 14 days). For the two loading methods, 30-60 μm SAP-MS showed no statistically significant difference in loading rate but a statistically significant difference in cumulative elution at 14 days (19.13 mg vs 17.83 mg, one-step vs two-step; P = .02). For the two loading methods, 50-100 μm SAP-MS showed no statistically significant difference in loading rate and no statistically significant difference in cumulative elution at 14 days (14.87 mg vs 12.77 mg, one-step vs two-step; P = .20).
SAP-MS exhibit the ability to load and release doxorubicin. In comparing particle size and loading methods, higher cumulative elution rates were associated with smaller (30-60 μm) particle size and one-step loading. Higher elution from the one-step loading method may be due to release of unbound doxorubicin. Differences in the loading and elution of doxorubicin may depend on the increased surface area of smaller SAP-MS resulting in alterations of behavior of doxorubicin and its interactions with the polymer microspheres.
研究阿霉素和高吸水性聚合物微球（SAP-MS）的加载和洗脱行为与粒径和加载技术的关系。
将 30-60μm 和 50-100μm 的 SAP-MS 进行预水合（一步法）或两次分步给药（两步法），从干燥的冻干状态下负载 50mg 的阿霉素。负载后，使用高压液相色谱（HPLC）分析阿霉素，测定载药率和洗脱特性。所有实验均重复三次进行。
所有系统均能在规定的时间内有效负载和洗脱阿霉素（负载时间为 15 分钟至 2 小时，洗脱时间为 1 小时至 14 天）。对于两种加载方法，30-60μm SAP-MS 的载药率无统计学差异，但在第 14 天的累积洗脱量有统计学差异（一步法 vs 两步法，19.13mg 比 17.83mg；P=0.02）。对于两种加载方法，50-100μm SAP-MS 的载药率和第 14 天的累积洗脱量均无统计学差异（一步法 vs 两步法，14.87mg 比 12.77mg；P=0.20）。
SAP-MS 具有负载和释放阿霉素的能力。在比较粒径和加载方法时，与较小粒径（30-60μm）和一步法加载相关的累积洗脱率更高。一步法加载中更高的洗脱率可能是由于未结合的阿霉素释放所致。阿霉素的负载和洗脱差异可能取决于 SAP-MS 较小的表面积增加，从而改变阿霉素的行为及其与聚合物微球的相互作用。
