The aim of this paper is to investigate and optimize the preparation of scutellarin(SCU)-loaded HP-β-CD/chitosan(CS) nanoparticles(CD/CS-SCU-NPs). CD/CS-SCU-NPs were prepared by ionic cross-linking method and the pro...The aim of this paper is to investigate and optimize the preparation of scutellarin(SCU)-loaded HP-β-CD/chitosan(CS) nanoparticles(CD/CS-SCU-NPs). CD/CS-SCU-NPs were prepared by ionic cross-linking method and the process and formulation variables were optimized using response surface methodology(RSM) with a three-level, three factor Box–Behnken design(BBD).The independent variables were the added amounts of CS, sodium tripolyphosphate(TPP)and Pluronic F-68 during the preparation. Dependent variables(responses) were particle size and entrapment efficiency. Mathematical equations and respond surface plots were used to correlate independent and dependent variables.The preparation process and formulation variables were optimized to achieve minimum particle size and maximum entrapment efficiency by calculating the overall desirability value(OD). The optimized NP formulation was characterized for particle size, PDI, zeta potential, entrapment efficiency and in vitro drug release.According to the results, an optimized CD/CS-SCU-NP formulation was prepared. Results for particle size, PDI, zeta potential and entrapment efficiency were found to be around 200 nm,0.5, 25 mV, and 70% respectively. For in vitro study, the release of SCU from the NPs exhibited a biphasic release and was in accordance with Higuchi equation. The optimized preparation was simple with the probability for industrialization. The combination use of RSM, BBD and overall desirability values could provide a promising application for incorporating CD into CS nanoparticles as drug delivery carrier and help develop lab-scale procedures.展开更多
Eugenol, both in its pure form (EG) and included in essential clove oil (CO) was successfully solubilized in aqueous solution by forming inclusion complexes with β-cyclodextrins (β-CDs) and its modified hydroxy-prop...Eugenol, both in its pure form (EG) and included in essential clove oil (CO) was successfully solubilized in aqueous solution by forming inclusion complexes with β-cyclodextrins (β-CDs) and its modified hydroxy-propyl-β-CDs (HP-β-CDs). To investigate the molecular association between β-CDs/HP-β-CDs with pure EG and essential CO, phase solubility studies were undertaken. Essential CO formed insoluble complexes with β-CDs, but not with HP-β-CDs. The work clearly demonstrates complexes formation follow an order higher than 1:1 when high essential CO and β-CDs concentrations were used, however it was 1:1 in the case of essential CO-HP-β-CDs complexes. When pure EG was studied the results indicated that EG could form 1:1 inclusion complexes with β-CDs and HP-β-CDs. Based on the studies, the Kc values for pure EG were 4555 ± 225 M-1 and 10,633 ± 614 M-1 for β-CDs and HP-β-CDs, respectively, and 2005 ± 199 M-1 for essential CO-HP-β-CDs. These finding indicate that CDs are suitable for encapsulating EG.展开更多
基金supported by the Academic Research Fund,Faculty of Science,National University of Singapore,R148-000-180-112
文摘The aim of this paper is to investigate and optimize the preparation of scutellarin(SCU)-loaded HP-β-CD/chitosan(CS) nanoparticles(CD/CS-SCU-NPs). CD/CS-SCU-NPs were prepared by ionic cross-linking method and the process and formulation variables were optimized using response surface methodology(RSM) with a three-level, three factor Box–Behnken design(BBD).The independent variables were the added amounts of CS, sodium tripolyphosphate(TPP)and Pluronic F-68 during the preparation. Dependent variables(responses) were particle size and entrapment efficiency. Mathematical equations and respond surface plots were used to correlate independent and dependent variables.The preparation process and formulation variables were optimized to achieve minimum particle size and maximum entrapment efficiency by calculating the overall desirability value(OD). The optimized NP formulation was characterized for particle size, PDI, zeta potential, entrapment efficiency and in vitro drug release.According to the results, an optimized CD/CS-SCU-NP formulation was prepared. Results for particle size, PDI, zeta potential and entrapment efficiency were found to be around 200 nm,0.5, 25 mV, and 70% respectively. For in vitro study, the release of SCU from the NPs exhibited a biphasic release and was in accordance with Higuchi equation. The optimized preparation was simple with the probability for industrialization. The combination use of RSM, BBD and overall desirability values could provide a promising application for incorporating CD into CS nanoparticles as drug delivery carrier and help develop lab-scale procedures.
文摘Eugenol, both in its pure form (EG) and included in essential clove oil (CO) was successfully solubilized in aqueous solution by forming inclusion complexes with β-cyclodextrins (β-CDs) and its modified hydroxy-propyl-β-CDs (HP-β-CDs). To investigate the molecular association between β-CDs/HP-β-CDs with pure EG and essential CO, phase solubility studies were undertaken. Essential CO formed insoluble complexes with β-CDs, but not with HP-β-CDs. The work clearly demonstrates complexes formation follow an order higher than 1:1 when high essential CO and β-CDs concentrations were used, however it was 1:1 in the case of essential CO-HP-β-CDs complexes. When pure EG was studied the results indicated that EG could form 1:1 inclusion complexes with β-CDs and HP-β-CDs. Based on the studies, the Kc values for pure EG were 4555 ± 225 M-1 and 10,633 ± 614 M-1 for β-CDs and HP-β-CDs, respectively, and 2005 ± 199 M-1 for essential CO-HP-β-CDs. These finding indicate that CDs are suitable for encapsulating EG.