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

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.