QUERCETIN-LOADED LIPOSOMES: FORMULATION
OPTIMIZATION THROUGH A D-OPTIMAL EXPERIMENTAL
DESIGN
LUCIA RUXANDRA TEFAS, DANA-MARIA MUNTEAN*, LAURIAN VLASE, ALINA SILVIA
PORFIRE, MARCELA ACHIM, IOAN TOMUȚĂ
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Iuliu Haţieganu” University of
Medicine and Pharmacy, 8 Victor Babeș, 400012, Cluj-Napoca, Romania
*corresponding author: dana@tbs.ubbcluj.ro
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Abstract:

This study aimed to investigate the influence of formulation factors on the physico-chemical properties of quercetin-loaded
liposomes and optimize the preparation conditions. An experimental design with three factors and three levels was used. The
variables were dipalmitoylphosphatidylcholine (DPPC) concentration, DPPC:Cholesterol (CHOL) molar ratio and quercetin
(QU) concentration. The responses were the mean diameter, polydispersity index (PdI) and drug encapsulation efficiency. All
samples were prepared according to the experimental design matrix consisting of 17 experiments. Results showed that DPPC
concentration and DPPC:CHOL molar ratio had a strong influence on liposome size and PdI. Higher DPPC concentrations
led to larger particles and PdI values, but a further increase of DPPC concentration produced a reduction in size and lower
PdI. Increasing the lipid ratio caused a decrease in size, but a somewhat higher PdI. QU concentration only slightly
influenced particle size and PdI. The degree of QU loading depended on the factors assessed. Increasing DPPC concentration
and lipid ratio significantly enhanced QU entrapment. However, higher QU concentrations had a negative effect on drug
entrapment. Based on this, an optimized formulation was determined, prepared and analysed. The overall results showed that
DPPC concentration and lipid ratio were the main factors influencing particle size, while entrapment efficiency was affected
predominantly by QU concentration.

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