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Development of Formulation Methods and Physical Characterization of Injectable Sodium Selenite Nanoparticles for the Delivery of Sorafenib tosylate.
Current Pharmaceutical Biotechnology ( IF 2.2 ) Pub Date : 2020-06-30 , DOI: 10.2174/1389201021666191230124041
Sivakumar S Moni 1 , Mohammad F Alam 2 , Mohammed M Safhi 2 , Muhammad H Sultan 1 , Hafiz A Makeen 3 , Mohamed E Elmobark 1
Affiliation  

Background: Sorafenib is the first oral therapeutic agent to show the activity against human hepatocellular carcinoma. Sorafenib leads to severe toxicity due to the multiple-dose regimen. Reducing the overall dose of sorafenib through injectable dosage form to release sustainably is of therapeutically more important to combat drug-induced toxicity.

Objective: The purpose of this study was to formulate and evaluate the physical parameters of sorafenib- loaded Sodium Selenite Nanoparticles (SSSNP).

Methods: Two different methods: chemical crosslinking and solvent evaporation were applied for the formulation of nanoparticles using various crosslinkers such as formaldehyde, magnesium sulfate, tripolyphosphate, dextran sulfate, and aluminum hydroxide. Physical characterization was performed with zeta potential analysis, polydispersity index, particle size and scanning electron microscopic studies for morphological analysis for all the formulated nanoparticles developed using the chemical crosslinking technique based ionic interaction.

Results: Tripolyphosphate was selected as an ideal crosslinker and used for nanoparticle formulation with the solvent evaporation technique. Based on the physical characterization, SSSNP was formulated successfully with the solvent evaporation technique using tripolyphosphate as a cross-linker. The zeta potential of SSSNP was -37.5 mV, PDI was approximately 0.3 to 0.4, and the observed size (diameter) was in the range of 208 nm to 0.2 μm. Furthermore, the particles were smooth in morphology and appeared as crystals.

Conclusion: The novel injectable sorafenib loaded sodium selenite nanoparticle dosage form will serve better than conventional oral dosage form to elicit a safe therapeutic effect.



中文翻译:

用于注射甲苯磺酸索拉非尼的可注射亚硒酸钠纳米颗粒的配制方法和物理表征的开发。

背景:索拉非尼是第一种对人肝细胞癌具有活性的口服治疗剂。由于多剂量方案,索拉非尼导致严重的毒性。通过注射剂型降低索拉非尼的总剂量以持续释放在对抗药物诱导的毒性方面在治疗上更为重要。

目的:本研究的目的是制定和评估载有索拉非尼亚硒酸钠纳米颗粒(SSSNP)的物理参数。

方法:采用两种不同的方法:化学交联和溶剂蒸发,使用各种交联剂(例如甲醛,硫酸镁,三聚磷酸酯,硫酸葡聚糖和氢氧化铝)来配制纳米颗粒。使用zeta电位分析,多分散指数,粒度和扫描电子显微镜研究进行物理表征,以对所有使用基于化学交联技术的离子相互作用开发的配制纳米颗粒进行形态分析。

结果:三聚磷酸酯被选为理想的交联剂,并通过溶剂蒸发技术用于纳米粒子配方。基于物理表征,采用三聚磷酸盐作为交联剂,采用溶剂蒸发技术成功制备了SSSNP。SSSNP的ζ电位为-37.5mV,PDI约为0.3至0.4,并且观察到的尺寸(直径)在208nm至0.2μm的范围内。此外,颗粒的形态是光滑的并以晶体形式出现。

结论:新型可注射索拉非尼负载的亚硒酸钠纳米粒剂型比常规口服剂型具有更好的治疗效果。

更新日期:2020-07-10
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