The Potential of Atractylodin-Loaded PLGA Nanoparticles as Chemotherapeutic for Cholangiocarcinoma

载苍术素的 PLGA 纳米粒子作为胆管癌化疗药物的潜力

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作者:Nada Muhamad, Tullayakorn Plengsuriyakarn, Chuda Chittasupho, Kesara Na-Bangchang

Conclusion

ALNPs were successfully prepared by solvent displacement method using PLGA MW 12,000 (ALNPs-1) with suitable pharmaceutical properties and cytotoxic activity against CCA. However, nano-formulation with improved pharmaceutical properties (higher %EE and %LE) and cytotoxic activity (improved selectivity to CCA) should be further developed for potential used as drug delivery systems for the treatment of CCA.<br />.

Methods

The ALNPs were prepared using PLGA MW 12,000 and 48,000 by solvent displacement methods. Particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency (%EE) and loading efficiency (%LE) as well as drug releasing profile of ALNPs were characterized. The selected ALNPs formulation was then investigated cytotoxic activity against CCA cell lines, CL-6 and HuCC-T1.

Results

The ALNPs preparation was achieved using PLGA MW 12,000 (ALNPs-1) with mean (±SD) values of particle diameter, PDI and zeta potential of 158.13±0.21 nm, 0.076±0.003, and (-) 23.80± (-) 0.75 mV, respectively. The transmission electron microscopy (TEM) showed spherical morphology of NPs. The %EE and %LE were 50.16±1.77% and 2.22±0.08%, respectively. The release of atractylodin from ALNPs-1 in PBS was up to 88% in 72 h. The potency of ALNPs-1 cytotoxic activity including selectivity against CCA cell line, CL-6, were about twice of the unformulated atractylodin after 24 h of exposure (IC50: 29.28 vs 56.36 µg/mL, selectivity index 2.99 vs 1.50).

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