Design, characterization and evaluation of cucurbitacin B-loaded core–shell-type hybrid nano-sized particles using DoE approach

• Published in: Polymer bulletin (Berlin, Germany) Vol. 78; no. 6; pp. 3327 - 3351
• Main Authors: Sengel-Turk, Ceyda Tuba, Ozmen, Nuri, Bakar-Ates, Filiz
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 01.06.2021; Springer Nature B.V
• Subjects: Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Complex Fluids and Microfluidics; Design optimization; Drug delivery systems; Efficiency; Entrapment; Factorial design; Glycolic acid; Hybrid systems; Industrial production; Lecithin; Lipids; Nanoparticles; Organic Chemistry; Original Paper; Particle size; Phospholipids; Physical Chemistry; Polydispersity; Polyethylene glycol; Polymer Sciences; Polymers; Response surface methodology; Self-assembly; Shell stability; Soft and Granular Matter; Storage stability; Surface charge; Thermodynamic properties; Variables; United States > US; Germany; full factorial design; 3; Response surface methodology; Core–shell-type lipid polymer hybrid systems; Cucurbitacin B
• ISSN: 0170-0839; 1436-2449
• DOI: 10.1007/s00289-020-03256-7

The main objective of this research was to design and optimize novel core–shell-type hybrid nano-sized systems of cucurbitacin B (CuB) based on the design of experiment (DoE) approach. The hybrid formulations consisting of polyethylene glycol (PEG)-conjugated phospholipid, lecithin and poly-lactic-co-glycolic acid (PLGA) were produced by employing self-assembly modified nanoprecipitation technique. A 3 2 factorial design was utilized to understand the effect of two input factors, namely PEG phospholipid/polymer ratio and total lipids/lecithin ratio, on entrapment efficiency and drug release percentage. The particle size and surface charge analyses, excipient interactions and thermal behavior, particle morphology, presence and thickness of lipid shell, and also storage stability studies were carried out through in vitro characterization. The entrapment efficiency of all nanoparticles of CuB ranged between 49.35 and 80.00%. The prepared lipid–polymer hybrid systems exhibited an average particle size from 94.5 to 127.2 nm with polydispersity in the range from 0.094 to 0.114, which inhibited a narrow size distribution. The nano-sized formulation at the center point of the design was selected as optimum formulation due to its excellent characteristics and the configuration determined using ANOVA and response surface methodology (RSM) approach.