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首页> 外文期刊>Acta biomaterialia >The effect of polyethylene glycol structure on paclitaxel drug release and mechanical properties of PLGA thin films.
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The effect of polyethylene glycol structure on paclitaxel drug release and mechanical properties of PLGA thin films.

机译：聚乙二醇结构对紫杉醇药物释放和PLGA薄膜力学性能的影响。

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摘要

Thin films of poly(lactic acid-co-glycolic acid) (PLGA) incorporating paclitaxel typically have slow release rates of paclitaxel of the order of 1 mug day(-1) cm(-2). For implementation as medical devices a range of zero order release rates (i.e. 1-15 mug day(-1) cm(-2)) is desirable for different tissues and pathologies. Eight and 35 kDa molecular weight polyethylene glycol (PEG) was incorporated at 15%, 25% and 50% weight ratios into PLGA containing 10 wt.% paclitaxel. The mechanical properties were assessed for potential use as medical implants and the rates of release of paclitaxel were quantified as per cent release and the more clinically useful rate of release in mug day(-1) cm(-2). Paclitaxel quantitation was correlated with the release of PEG from PLGA, to further understand its role in paclitaxel/PLGA release modulation. PEG release was found to correlate with paclitaxel release and the level of crystallinity of the PEG in the PLGA film, as measured by Raman spectrometry. This supports the concept of using a phase separating, partitioning compound to increase the release rates of hydrophobic drugs such as paclitaxel from PLGA films, where paclitaxel is normally homogeneously distributed/dissolved. Two formulations are promising for medical device thin films, when optimized for tensile strength, elongation, and drug release. For slow rates of paclitaxel release an average of 3.8 mug day(-1) cm(-2) using 15% 35k PEG for >30 days was achieved, while a high rate of drug release of 12 mug day(-1) cm(-2) was maintained using 25% 8 kDa PEG for up to 12 days.
机译：掺入紫杉醇的聚乳酸-乙醇酸共聚物（PLGA）薄膜通常具有大约1马克天（-1）cm（-2）的紫杉醇缓慢释放速率。为了实现作为医疗设备，对于不同的组织和病理学，期望零级释放速率的范围（即1-15马克杯天（-1）cm（-2））。将8和35kDa分子量的聚乙二醇（PEG）以15％，25％和50％的重量比掺入含有10重量％紫杉醇的PLGA中。评估了其机械性能，可作为医疗植入物的潜在用途，并将紫杉醇的释放速率量化为释放的百分比，以及更有效的临床使用率（杯天（-1）cm（-2））。紫杉醇定量与PLGA中PEG的释放相关，以进一步了解其在紫杉醇/ PLGA释放调节中的作用。通过拉曼光谱法测定，发现PEG释放与紫杉醇释放和PLGA膜中PEG的结晶度相关。这支持了使用相分离，分配化合物来提高疏水性药物（例如紫杉醇）从PLGA膜中释放的概念，其中紫杉醇通常均匀分布/溶解。当针对拉伸强度，伸长率和药物释放进行优化时，两种配方有望用于医疗器械薄膜。对于紫杉醇的缓慢释放，使用15％35k PEG进行> 30天的平均3.8马克天（-1）cm（-2）的平均释放，而12马克天（-1）cm（ -2）使用25％8 kDa PEG维持长达12天。

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