International Journal of Nanomedicine (Jul 2020)

A Novel Nanoparticle Preparation to Enhance the Gastric Adhesion and Bioavailability of Xanthatin

  • Zhou Y,
  • Zhu X,
  • Lin S,
  • Zhu C,
  • Wu L,
  • Chen R,
  • Chen Z,
  • Li W

Journal volume & issue
Vol. Volume 15
pp. 5073 – 5082

Abstract

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Yaqian Zhou,1,* Xingyu Zhu,2,* Shangyang Lin,1 Chenqi Zhu,1 Li Wu,1 Rui Chen,1 Zhipeng Chen,1 Weidong Li1,3 1College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, People’s Republic of China; 2Department of Pharmacy and Traditional Chinese Medicine, Jiangsu College of Nursing, Huaian 223001, People’s Republic of China; 3Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, People’s Republic of China*These authors contributed equally to this workCorrespondence: Weidong LiEngineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, People’s Republic of ChinaEmail [email protected]: To prepare xanthatin (XA)-loaded polydopamine (PDA) nanoparticles (PDA-XA-NPs) and to investigate their adhesion and bioavailability.Materials and methods: PDA-XA-NPs were synthesized and characterized using transmission electron microscopy, zeta potential analysis and encapsulation efficiency analysis. Their in vitro release kinetics and inhibitory effects on gastric cancer were studied. The adhesion of PDA-XA-NPs was evaluated by in vivo imaging atlas. The pharmacokinetics of PDA-XA-NPs and XA was compared.Results: PDA-XA-NPs had a spherical shape, a particle size of about 380 nm, an encapsulation efficiency of (82.1 ± 0.02) % and a drug loading capacity of (5.5 ± 0.1)%. The release of PDA-XA-NPs in PBS was stable and slow, without being affected by pH. The adhesion capacity of PDA-XA-NPs for mucin was significantly higher than that of bulk drug. The gastric mucosal retention of PDA-XA-NPs reached 89.1% which significantly exceeded that of XA. In vivo imaging showed that PDA-XA-NPs targeting the stomach were retained for a period of time. The pharmacokinetics study showed that PDA-XA-NPs had a longer retention time and a slower drug release than those of XA. In vitro experiments confirmed that PDA-XA-NPs exerted similar inhibitory effects on gastric cancer to those of XA, which lasted for a period of time.Conclusion: High-adhesion NPs were constructed. Gastric cancer was targeted by orally administered PDA-XA-NPs, as a potentially feasible therapy. Eventually, the bioavailability of XA was increased.Keywords: xanthatin, polydopamine, nanoparticles, gastric cancer, target, pharmacokinetics

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