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首页> 外文期刊>Nanotechnology >Mechanisms of chitosan-coated poly(lactic-co-glycolic acid) nanoparticles for improving oral absorption of 7-ethyl-10-hydroxycamptothecin
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Mechanisms of chitosan-coated poly(lactic-co-glycolic acid) nanoparticles for improving oral absorption of 7-ethyl-10-hydroxycamptothecin

机译：壳聚糖包覆的聚乳酸-乙醇酸共聚物纳米颗粒改善口服吸收7-乙基-10-羟基喜树碱的机制

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摘要

Chitosan-modified poly(lactic-co-glycolic acid) nanoparticles (CHI/PLGA NPs) loaded with 7-ethyl-10-hydroxycamptothecin (SN-38), named CHI/PLGA/SN-38 NPs, were successfully prepared using an oil-in-water (O/W) solvent evaporation method. The physicochemical properties of the novel NPs were characterized by DLS, Zeta potential, SEM, DSC, XRD, and FTIR. The encapsulation efficiency and drug loading content were 71.83 (±2.77)% and 6.79 (±0.26)%, respectively. In vitro drug release in the simulated gastric juice was lower than that in the intestinal juice. In situ single-pass intestinal perfusion (SPIP) studies indicated a dramatic improvement of drug absorption as a result of the synergistic effect between CHI and PLGA on P-glycoprotein (Pgp) inhibition. CHI/PLGA NPs showed high cellular uptake and low efflux for drugs in Caco-2 cells. The cytotoxicity studies revealed that CHI/PLGA NPs had a transient effect on the membrane integrity, but did not have an influence on cell viability. Based on the in vitro release studies, SPIP, and intracellular drug accumulation and transport investigations, we speculate rationally that CHI/PLGA NPs were mainly internalized in the form of intact NPs, thus escaping the recognition of enterocyte Pgp and avoiding efflux into the apical part of the enterocytes. After partial release of drugs inside the enterocytes, CHI/PLGA interfered with the microenvironment of Pgp and further weakened the Pgp-mediated efflux. Then, the drug-loaded NPs exited via the exocytose effect from the basal part of the enterocytes and entered the blood circulation. These results showed that CHI/PLGA NPs would be smart oral delivery carriers for antineoplastic agents that are also Pgp substrates.
机译：使用油成功地制备了负载有7-乙基-10-羟基喜树碱（SN-38）的壳聚糖改性聚乳酸​​-乙醇酸纳米颗粒（CHI / PLGA NPs），命名为CHI / PLGA / SN-38 NPs。水（O / W）溶剂蒸发法。通过DLS，Zeta电位，SEM，DSC，XRD和FTIR表征了新型NP的理化性质。包封效率和载药量分别为71.83（±2.77）％和6.79（±0.26）％。模拟胃液中的体外药物释放低于肠液中的药物释放。原位单程肠道灌注（SPIP）研究表明，CHI和PLGA之间对P-糖蛋白（Pgp）抑制的协同作用可显着改善药物吸收。 CHI / PLGA NP对Caco-2细胞中的药物显示高细胞摄取和低外排。细胞毒性研究表明，CHI / PLGA NPs对膜的完整性有短暂的影响，但对细胞活力没有影响。根据体外释放研究，SPIP以及细胞内药物积聚和转运研究，我们合理地推测CHI / PLGA NP主要以完整NP的形式内在化，从而避免了对肠细胞Pgp的识别并避免了向心尖部外排肠细胞。在肠细胞内部分药物释放后，CHI / PLGA干扰了Pgp的微环境并进一步减弱了Pgp介导的外排。然后，载有药物的NPs通过胞吞作用从肠细胞的基础部分退出，进入血液循环。这些结果表明，CHI / PLGA NPs将成为抗肿瘤药物的智能口服载体，这些抗肿瘤药物也是Pgp的底物。

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