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Fabrication, Optimization and Characterization of Paclitaxel and Spirulina Loaded Nanoparticles for Enhanced Oral Bioavailability
Current Nanoscience ( IF 1.5 ) Pub Date : 2020-09-30 , DOI: 10.2174/1573413716666200203115101
Keerthi G.S. Nair 1 , Yamuna Ravikumar 1 , Sathesh Kumar Sukumaran 1 , Ramaiyan Velmurugan 1
Affiliation  

Background: Paclitaxel and spirulina when administered as nanoparticles, are potentially useful.

Methods: Nanoformualtions of Paclitaxel and Spirulina for gastric cancer were formulated and optimized with Central composite rotatable design (CCRD) using Response surface methodology (RSM).

Results: The significant findings were the optimal formulation of polymer concentration 48 mg, surfactant concentration 45% and stirring time of 60 min gave rise to the EE of (98.12 ± 1.3)%, DL of (15.61 ± 1.9)%, mean diameter of (198 ± 4.7) nm. The release of paclitaxel and spirulina from the nanoparticle matrix at pH 6.2 was almost 45% and 80% in 5 h and 120 h, respectively. The oral bioavailability for the paclitaxel spirulina nanoparticles developed is 24.0% at 10 mg/kg paclitaxel dose, which is 10 times of that for oral pure paclitaxel. The results suggest that RSM-CCRD could efficiently be applied for the modeling of nanoparticles. The paclitaxel and spirulina release rate in the tumor cells may be higher than in normal cells. Paclitaxel spirulina nanoparticle formulation may have higher bioavailability and longer sustainable therapeutic time as compared with pure paclitaxel.

Conclusion: Paclitaxel-Spirulina co-loaded nanoparticles could be effectively useful in gastric cancer as chemotherapeutic formulation.



中文翻译:

紫杉醇和螺旋藻负载纳米颗粒的制备,优化和表征,以提高口服生物利用度

背景:紫杉醇和螺旋藻作为纳米颗粒给药时,可能会有用。

方法:采用响应表面方法(RSM),通过中央复合可旋转设计(CCRD)制定并优化了紫杉醇和螺旋藻用于胃癌的纳米形式。

结果:显着的发现是最佳配方的聚合物浓度为48 mg,表面活性剂浓度为45%,搅拌时间为60分钟,产生的EE为(98.12±1.3)%,DL为(15.61±1.9)%,平均直径(198±4.7)nm。在pH值为6.2时,紫杉醇和螺旋藻从纳米颗粒基质中释放的时间分别为5小时和120小时,分别约为45%和80%。紫杉醇螺旋藻纳米颗粒在10 mg / kg紫杉醇剂量下的口服生物利用度为24.0%,是口服纯紫杉醇的10倍。结果表明,RSM-CCRD可以有效地应用于纳米颗粒的建模。肿瘤细胞中紫杉醇和螺旋藻的释放速率可能高于正常细胞。

结论:紫杉醇-螺旋藻纳米粒共载药可作为胃癌化疗药物有效治疗胃癌。

更新日期:2020-10-05
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