Thermosensitive Pluronic® F127-Based in situ gel formulation containing nanoparticles for the sustained delivery of paclitaxel

S. Unal, M. Tekeli, O. Doğan, Y. Aktaş
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引用次数: 1

Abstract

Bone metastasis is one of the most encountered complications among cancer patients and majority of cancer types has led to bone metastasis. Paclitaxel (PCX) is an anticancer agent commonly used in cancer treatment. However, its clinical use is restricted owing to poor water solubility. PCL NPs were investigated to cope with solubility problem of PCX. The size, polydispersity index and zeta potential of PCL were 383.8±2.4 nm, 0.253±0.122 and +51.3±6.1 mV, respectively. The PCX encapsulation efficiency was 77.2±2.1%. Subsequently, in situ gellling system was prepared by using different Pluronic F-127 concentration in order to determine the optimum ratio. İn situ gel formulation containing 20% Pluronic F-127 was selected as the optimum formulation and subjected to characterization tests. The viscosity of in situ gelling system with CS/PCX-PCL NPs at room temperature (25 °C±0.1) and at body temperature (37 °C±0.1) were found 137.00 ±3.05 cP and 890.30 ±89.61 cP at 100 rpm, respectively. According to the release results, in situ gel provided prolonged release profile compared to PCL NPs alone. Consequently, in situ gel containing CS/PCX-PCL NP elucidated in detail is a promising approach for locally applicable injectable systems.
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热敏Pluronic®f127为基础的原位凝胶配方含有纳米颗粒持续递送紫杉醇
骨转移是癌症患者最常见的并发症之一,大多数癌症类型都会导致骨转移。紫杉醇(Paclitaxel, PCX)是一种常用的抗癌药物。但其水溶性较差,限制了其临床应用。研究了PCL NPs对PCX溶解度的影响。PCL的尺寸为383.8±2.4 nm,多分散性指数为0.253±0.122,zeta电位为+51.3±6.1 mV。PCX包封率为77.2±2.1%。随后,用不同Pluronic F-127浓度制备原位成胶体系,以确定最佳配比。İn选择含20% Pluronic F-127的原位凝胶配方为最佳配方,并进行表征试验。CS/PCX-PCL NPs原位胶凝体系在室温(25℃±0.1)和体温(37℃±0.1)下的粘度分别为137.00±3.05 cP和890.30±89.61 cP (100 rpm)。根据释放结果,与单独的PCL NPs相比,原位凝胶提供了较长的释放曲线。因此,详细阐明了含有CS/PCX-PCL NP的原位凝胶是一种有前途的局部适用注射系统的方法。
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