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

• Published in: Journal of microencapsulation Vol. 34; no. 6; pp. 582 - 591
• Main Authors: Chevalier, Merari T., García, Mónica C., Gonzalez, Daniela, Gomes-Filho, Sandro M., Bassères, Daniela S., Farina, Hernan, Alvarez, Vera A.
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 18.08.2017
• Subjects: Antineoplastic Agents - administration & dosage; Biopolymers; Cell Line, Tumor; Drug Delivery Systems; Humans; microparticles; Pancreatic Neoplasms - drug therapy; polylactic acid; Polylysine - chemistry; Polymers - chemistry; ε-polylysine; ε-polylysine; microparticles; polylactic acid; Biopolymers
• ISSN: 0265-2048; 1464-5246
• DOI: 10.1080/02652048.2017.1370028

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 (T d 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.