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首页> 外文期刊>Drug Design, Development and Therapy >Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery
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Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery

机译：大黄酸负载型聚乳酸-乙醇酸共聚物纳米粒的制备，表征及体内研究

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Abstract: A novel rhein formulation based on poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) suitable for oral administration was developed in this study. The designed nanosystems were obtained by a modified spontaneous emulsification solvent diffusion method. The morphology of rhein-loaded PLGA NPs showed a spherical shape with a smooth surface, without any particle aggregation. Mean size of the NPs was 140.5±4.3?nm, and the zeta potential was -16.9±3.1?mV. The average drug loading was 3.9%±0.7%, and encapsulation efficiency was 84.5%±6.2%. Meanwhile, NPs are characterized by the slower release (only about 70% of rhein is released within 5?hours), and the model that fitted best for rhein released from the NPs was Higuchi kinetic model with correlation coefficient r=0.9993, revealing that rhein could be controlled released from the NPs. In vivo, NPs altered the distribution of rhein, and the half-life after oral administration was prolonged remarkably more than those of suspensions (22.6?hours vs 4.3?hours). The pharmacokinetic results indicated that the NPs had sustained-release efficacy. The area under the curve0–∞ of the NPs formulation was 3.07-fold higher than that of suspensions, suggesting that the encapsulated rhein had almost been absorbed in rats over the period of 12?hours. Although rhein-loaded PLGA NP formulations are hopefully used as a chemotherapeutic or adjuvant agent for human gastric cancer (SGC-7901), their in vivo antitumor effect and mechanisms at the molecular level still need further study.
机译：摘要：本研究开发了一种新型的基于聚乳酸-乙醇酸（PLGA）纳米粒（NPs）的大黄酸制剂，适合口服。通过改进的自发乳化溶剂扩散法获得了设计的纳米系统。装有大黄酸的PLGA NP的形态为球形，表面光滑，没有任何颗粒聚集。 NP的平均大小为140.5±4.3μm，ζ电位为-16.9±3.1μmV。平均载药量为3.9％±0.7％，包封效率为84.5％±6.2％。同时，NPs的释放速度较慢（在5？小时内仅释放约70％的大黄酸），最适合从NPs释放的大黄酸的模型是Higuchi动力学模型，相关系数r = 0.9993，表明大黄酸可以控制从NP释放。在体内，NPs改变了大黄酸的分布，口服后的半衰期比混悬液的半衰期显着延长（22.6？小时vs. 4.3？小时）。药代动力学结果表明NP具有缓释功效。 NPs制剂的0–∞曲线下面积比悬浮液高3.07倍，这表明封装的大黄酸在12小时内几乎被大鼠吸收。尽管希望将大黄酸负载的PLGA NP制剂用作人胃癌的化学治疗或佐剂（SGC-7901），但它们在分子水平上的体内抗肿瘤作用和机制仍需要进一步研究。

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