Preparation, characterization and in vitro evaluation of ε-polylysine-loaded polymer blend microparticles for potential pancreatic cancer therapy

J Microencapsul. 2017 Sep;34(6):582-591. doi: 10.1080/02652048.2017.1370028. Epub 2017 Sep 3.

Abstract

Peptide active ingredients show great promise regarding the treatment of various health-endangering diseases. It is reported that L-lysine inhibits the proliferation of several tumour lines in vitro and in vivo. However, proteins and peptide drugs possess certain disadvantages such as in vivo instability and short biological half-life. On the grounds that drug delivery systems can overcome a wide spectrum of bioactive compounds issues, a biopolymeric blend-based microparticulated system capable of delivering ε-polylysine (PLL) was developed. PLL-loaded poly((L)Lactic acid)/poly(D,L-Lactide)-co-poly(ethylene glycol)-based microparticles (PLL-PB-MPs) were prepared and fully characterised exhibiting a narrow size distribution (1.2 ± 0.12 µm), high loading efficiency (81%) and improved thermal stability (Td from 250 °C to 291 °C). The cytotoxicity and antiproliferative effect of PLL-PB-MPs in pancreatic adenocarcinoma cell lines BxPC3 and MIA PaCa-2 were confirmed. Due to their physicochemical and biopharmaceutical properties, PB-MPs constitute a promising carrier to deliver bioactive peptides.

Keywords: Biopolymers; microparticles; polylactic acid; ε-polylysine.

MeSH terms

  • Antineoplastic Agents / administration & dosage*
  • Cell Line, Tumor
  • Drug Delivery Systems*
  • Humans
  • Pancreatic Neoplasms / drug therapy*
  • Polylysine / chemistry*
  • Polymers / chemistry

Substances

  • Antineoplastic Agents
  • Polymers
  • Polylysine