Fabrication, design, and in vivo investigation of mesoporous silica-based docetaxel trihydrate nanoparticles for colonic drug delivery

Subhabrota Majumdar, Mohini Mondal, Anirbandeep Bose, Ayan Kumar Kar, Rana Mazumder
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Abstract

Abstract Background Mesoporous silica-loaded docetaxel trihydrate nanoparticles are the potential to target drug delivery toward a specific region with high stability and predictable release at the target region. They have large surface areas and mesoporous structures with large pore volumes, leading to high bioavailability and therapeutic efficacy at the disease site. This study demonstrates how nanoparticles can be prepared using an emulsion technique. Results The ratios of eudragit S100 to eudragit L100 polymers, along with phosphatidylcholine, were varied according to the response surface methodology. Differential scanning colorimetry and fluorinated transmitted infrared spectroscopy studies showed that mesoporous silica particles were successful. All formulations had average particle sizes ranging from 70.65 to 143.01 nm, with a range of zeta potential from 17.6 ± 026 to 21 ± 011. In vitro drug delivery studies were achieved for all formulations with a zeta potential of 17.6 ± 026 to 21 ± 011. As per the statistical optimization by RSM that response model for percentage drug loading ( Y 1 ) was found to be 0.0002 which is p -value < 0.05. Hence, the model is significance. Accordingly percentage drug release at 6 h. ( Y 2 ) p -value was found to be 0.0001 and percentage drug release at 10 h ( Y 3 ) p -value was found to be 0.0002, respectively. So all the models are significant. After oral administration of the docetaxel, plasma levels were measured in vivo bioavailability testing of docetaxel. Docetaxel nanosuspension had a significantly higher C max amount than docetaxel microsuspension (98.03 ± 23.40 ng/ml and 213.67 ± 72.21 ng/ml, respectively, with t max 45 min). Docetaxel was more bioavailable in nanosuspension formulations, according to a bioavailability test of rats. Conclusion The results suggested that the mesoporous silica could be a great potential nanocarrier in colonic delivery with optimal drug content and controlled release docetaxel trihydrate.
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介孔硅基多西紫杉醇三水合物纳米颗粒结肠给药的制备、设计和体内研究
介孔二氧化硅负载的三水合多西紫杉醇纳米颗粒具有高稳定性和可预测释放的潜力,可以将药物输送到特定区域。它们具有大表面积和大孔体积的介孔结构,在疾病部位具有高生物利用度和治疗效果。本研究演示了如何使用乳液技术制备纳米颗粒。结果响应面法测定了乌曲油S100与乌曲油L100聚合物以及磷脂酰胆碱的比例。差示扫描比色法和氟化透射红外光谱研究表明,介孔二氧化硅颗粒是成功的。平均粒径范围为70.65 ~ 143.01 nm, zeta电位范围为17.6±026 ~ 21±011。所有制剂的zeta电位范围为17.6±026至21±011,均实现了体外给药研究。经RSM统计优化,药量百分比(Y 1)的响应模型为0.0002,p值为<0.05. 因此,模型是有意义的。因此,6 h (Y 2) p值为0.0001,10 h (Y 3) p值为0.0002。所以所有的模型都很重要。口服多西紫杉醇后,测定多西紫杉醇体内生物利用度试验的血浆水平。多西紫杉醇纳米混悬液的最大C含量显著高于多西紫杉醇微悬液(分别为98.03±23.40 ng/ml和213.67±72.21 ng/ml,最大t含量均为45 min)。根据对大鼠的生物利用度测试,多西紫杉醇在纳米混悬液中具有更高的生物利用度。结论介孔二氧化硅是一种极具潜力的结肠给药纳米载体,具有最佳的药物含量和控释效果。
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