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首页> 外文期刊>International Journal of Pharmaceutical Investigation >Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer
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Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer

机译：紫杉醇新型可生物降解缓释微球制剂的开发和评价，旨在治疗乳腺癌

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Objective:The objective of this study was to develop a novel 1 month depot paclitaxel (PTX) microspheres that give a sustained and complete drug release.Materials and Methods:PTX loaded microspheres were prepared by o/w emulsion solvent evaporation technique using the blends of poly(lactic-co-glycolic acid) (PLGA) 75/25, polycaprolactone 14,000 and polycaprolactone 80,000. Fourier transform infrared spectroscopy was used to investigate drug excipient compatibility. Compatible blends were used to prepare F1-F6 microspheres, the process was characterised and the optimum formulation was selected based on the release. Optimised formulation was characterised for solid state of the drug using the differential scanning calorimetry (DSC) studies, surface morphology using the scanning electron microscopy (SEM), in vivo drug release, in vitro in vivo correlation (IVIVC) and anticancer activity. Anticancer activity of release medium was determined using the cell viability assay in Michigan Cancer Foundation (MCF-7) cell line.Results:Blend of PLGA with polycaprolactone (Mwt 14,000) at a ratio of 1:1 (F5) resulted in complete release of the drug in a time frame of 30 days. F5 was considered as the optimised formulation. Incomplete release of the drug resulted from other formulations. The surface of the optimised formulation was smooth and the drug changed its solid state upon fabrication. The formulation also resulted in 1-month drug release in vivo. The released drug from F5 demonstrated anticancer activity for 1-month. Cell viability was reduced drastically with the release medium from F5 formulation. A 100% IVIVC was obtained with F5 formulation suggesting the authenticity of in vitro release, in vivo release and the use of the formulation in breast cancer.Conclusions:From our study, it was concluded that with careful selection of different polymers and their combinations, PTX 1 month depot formulation with 100% drug release and that can be used in breast cancer was developed.
机译：目的：本研究的目的是开发一种新型的1个月长效紫杉醇贮库（PTX）微球，该微球可实现持续，完全的药物释放。材料与方法：采用o / w乳剂溶剂蒸发技术，使用三氯苯酚的共混物制备载有PTX的微球。聚（乳酸-乙醇酸共聚物）（PLGA）75/25，聚己内酯14,000和聚己内酯80,000。傅里叶变换红外光谱用于研究药物赋形剂的相容性。使用相容的共混物制备F1-F6微球，对工艺进行了表征，并根据释放量选择了最佳配方。使用差示扫描量热法（DSC）研究，药物的固态状态，使用扫描电子显微镜（SEM）的表面形态，体内药物释放，体外体内相关性（IVIVC）和抗癌活性，对优化的制剂进行了表征。使用密歇根州癌症基金会（MCF-7）细胞系中的细胞生存力测定法确定释放介质的抗癌活性。结果：PLGA与聚己内酯（Mwt 14,000）的比例为1：1（F5）混合导致了PGA的完全释放该药物的使用期限为30天。 F5被认为是优化配方。其他制剂导致药物释放不完全。优化制剂的表面是光滑的，并且药物在制造时改变了其固态。该制剂还导致体内1个月的药物释放。从F5释放的药物显示了1个月的抗癌活性。用F5制剂的释放介质会大大降低细胞活力。用F5制剂获得了100％的IVIVC，表明体外释放，体内释放以及该制剂在乳腺癌中的真实性。结论：从我们的研究中得出的结论是，通过仔细选择不同的聚合物及其组合，可以得出结论：开发了可用于乳腺癌的PTX 1个月长效制剂，具有100％的药物释放能力。

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