Preparation of a tumor-targeted drug-loading material, amphiphilic peptide P10, and analysis of its anti-tumor activity
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A new tumor-targeted drug-loading material, the amphiphilic peptide DGRGGGAAAA (P10) was designed and synthesized, and its self-assembly behavior, drug-loading effects and in vitro characteristics were studied. P10 was synthesized by solid-state synthesis and doxorubicin (DOX) was loaded via dialysis. P10 and DOX were mixed with a mass ratio of 6:1 to form regular round spheres. The interconnection between groups was analyzed spectroscopically and the sphere morphology was studied with SEM and a zeta particle size analyzer. Fluorescence spectroscopy was used to analyze the ability of P10 to form micelles and the efficiency of micelle entrapment, and the drug-loading ratio and drug release characteristics were detected. Finally, the in vitro antitumor activity of P10 was studied with HeLa cells as a model. The results showed that P10’s critical micelle concentration (CMC) value and its average grain diameter were approximately 0.045 mg/L and 500 nm. The micelle entrapment ratio and drug-loading ratio were 23.011 ± 2.88 and 10.125 ± 2.62%, respectively, and the in vitro drug-releasing properties of P10 were described by the Zero-order model and the Ritger-Peppas model. Compared with DOX, P10-DOX had a higher tumor cell inhibition ratio and a dose-effect relationship with concentration. When P10-DOX’s concentration was 20 μg/mL, the inhibition ratio was 44.17%. The new amphiphilic peptide designed and prepared in this study could be a tumor-targeted drug-loading material with better prospects for application.
This work was supported by the National Natural Science Foundation of China (NSFC) [grant number 31671797], Natural Science Foundation of Anhui University [grant number 2017KJA123, KJ2017A251 and KJ2018A0117], Anhui Natural Science Foundation [grant number 1808085QC85] and the Youth talent support program of Anhui Polytechnic University [grant number 2016BJRRC006].
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Conflict of interest
The authors declare that they have no conflict of interest.
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