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Coaxial Electrospray of Curcumin-Loaded Microparticles for Sustained Drug Release.

Yuan S, Lei F, Liu Z, Tong Q, Si T, Xu RX - PLoS ONE (2015)

Bottom Line: Curcumin exhibits superior anti-inflammatory, antiseptic and analgesic activities without significant side effects.To overcome this limitation, we propose to encapsulate curcumin in poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs) by an improved coaxial electrospray (CES) process.Our experimental results show that the CES process can be effectively controlled to encapsulate drugs of low aqueous solubility for high encapsulation efficiency and optimal drug release profiles.

View Article: PubMed Central - PubMed

Affiliation: Department of Precision Machinery and Precision Instrumentation, University of Science and Technology of China, Hefei, Anhui, 230027, People's Republic of China.

ABSTRACT
Curcumin exhibits superior anti-inflammatory, antiseptic and analgesic activities without significant side effects. However, clinical dissemination of this natural medicine is limited by its low solubility and poor bio-availability. To overcome this limitation, we propose to encapsulate curcumin in poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs) by an improved coaxial electrospray (CES) process. This process is able to generate a stable cone-jet mode in a wide range of operation parameters in order to produce curcumin-loaded PLGA MPs with a clear core-shell structure and a designated size of several micrometers. In order to optimize the process outcome, the effects of primary operation parameters such as the applied electric voltages and the liquid flow rates are studied systemically. In vitro drug release experiments are also carried out for the CES-produced MPs in comparison with those by a single axial electrospray process. Our experimental results show that the CES process can be effectively controlled to encapsulate drugs of low aqueous solubility for high encapsulation efficiency and optimal drug release profiles.

No MeSH data available.


The influence of outer liquid flow rate Qout on the stable cone-jet mode and the size of resultant droplets.(a) Sequence of experimental images showing the stable cone-jet structure changing with Qout; (b) The angle of the cone θ as a function of Qout; (c) The diameter of the resultant droplets Dd as a function of Qout. The applied voltages: V1 = 4 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.2 mL/h; The vertical distances: h = 0.3 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.
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pone.0132609.g005: The influence of outer liquid flow rate Qout on the stable cone-jet mode and the size of resultant droplets.(a) Sequence of experimental images showing the stable cone-jet structure changing with Qout; (b) The angle of the cone θ as a function of Qout; (c) The diameter of the resultant droplets Dd as a function of Qout. The applied voltages: V1 = 4 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.2 mL/h; The vertical distances: h = 0.3 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.

Mentions: Fig 5 presents the influence of the outer liquid flow rate Qout on the stable coaxial cone-jet structure and the size of droplets collected just after the breakup of the coaxial liquid jet. The increase of the outer liquid flow rate from 0.2 mL/h to 1.8 mL/h shows a clear tendency with an increase in the diameter of droplets (from about 1.96 μm to 9.03 μm) and a decrease in the cone angle θ (from about 35° to 24°), and the coaxial cone is elongated. As the diameter of the coaxial jet is positively correlated with the liquid flow rate [18,19], it is easily understood that the mean diameter of the droplets increases gradually as the value of Qout increases. In particular, the droplet diameter increases linearly with the outer liquid flow rate, which is in accordance with the analytical scaling law predicted in previous studies [14]. It was also pointed out that due to the higher viscosity of the inner liquid, the size of the resultant droplets was mainly governed by the break up of the inner liquid jet, and the viscous stresses acting at the liquid-liquid interface was considerable [14]. As a result, the balance of accelerating and drag forces leads to the dependence of the droplet size on the liquid flow rate. The results indicate that the CES process is an effective approach to obtain drug-loaded PLGA droplets with tunable size by simply controlling the liquid flow rates and the applied voltages in the stable cone-jet mode for a given group of materials and a fixed CES device.


Coaxial Electrospray of Curcumin-Loaded Microparticles for Sustained Drug Release.

Yuan S, Lei F, Liu Z, Tong Q, Si T, Xu RX - PLoS ONE (2015)

The influence of outer liquid flow rate Qout on the stable cone-jet mode and the size of resultant droplets.(a) Sequence of experimental images showing the stable cone-jet structure changing with Qout; (b) The angle of the cone θ as a function of Qout; (c) The diameter of the resultant droplets Dd as a function of Qout. The applied voltages: V1 = 4 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.2 mL/h; The vertical distances: h = 0.3 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4514801&req=5

pone.0132609.g005: The influence of outer liquid flow rate Qout on the stable cone-jet mode and the size of resultant droplets.(a) Sequence of experimental images showing the stable cone-jet structure changing with Qout; (b) The angle of the cone θ as a function of Qout; (c) The diameter of the resultant droplets Dd as a function of Qout. The applied voltages: V1 = 4 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.2 mL/h; The vertical distances: h = 0.3 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.
Mentions: Fig 5 presents the influence of the outer liquid flow rate Qout on the stable coaxial cone-jet structure and the size of droplets collected just after the breakup of the coaxial liquid jet. The increase of the outer liquid flow rate from 0.2 mL/h to 1.8 mL/h shows a clear tendency with an increase in the diameter of droplets (from about 1.96 μm to 9.03 μm) and a decrease in the cone angle θ (from about 35° to 24°), and the coaxial cone is elongated. As the diameter of the coaxial jet is positively correlated with the liquid flow rate [18,19], it is easily understood that the mean diameter of the droplets increases gradually as the value of Qout increases. In particular, the droplet diameter increases linearly with the outer liquid flow rate, which is in accordance with the analytical scaling law predicted in previous studies [14]. It was also pointed out that due to the higher viscosity of the inner liquid, the size of the resultant droplets was mainly governed by the break up of the inner liquid jet, and the viscous stresses acting at the liquid-liquid interface was considerable [14]. As a result, the balance of accelerating and drag forces leads to the dependence of the droplet size on the liquid flow rate. The results indicate that the CES process is an effective approach to obtain drug-loaded PLGA droplets with tunable size by simply controlling the liquid flow rates and the applied voltages in the stable cone-jet mode for a given group of materials and a fixed CES device.

Bottom Line: Curcumin exhibits superior anti-inflammatory, antiseptic and analgesic activities without significant side effects.To overcome this limitation, we propose to encapsulate curcumin in poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs) by an improved coaxial electrospray (CES) process.Our experimental results show that the CES process can be effectively controlled to encapsulate drugs of low aqueous solubility for high encapsulation efficiency and optimal drug release profiles.

View Article: PubMed Central - PubMed

Affiliation: Department of Precision Machinery and Precision Instrumentation, University of Science and Technology of China, Hefei, Anhui, 230027, People's Republic of China.

ABSTRACT
Curcumin exhibits superior anti-inflammatory, antiseptic and analgesic activities without significant side effects. However, clinical dissemination of this natural medicine is limited by its low solubility and poor bio-availability. To overcome this limitation, we propose to encapsulate curcumin in poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs) by an improved coaxial electrospray (CES) process. This process is able to generate a stable cone-jet mode in a wide range of operation parameters in order to produce curcumin-loaded PLGA MPs with a clear core-shell structure and a designated size of several micrometers. In order to optimize the process outcome, the effects of primary operation parameters such as the applied electric voltages and the liquid flow rates are studied systemically. In vitro drug release experiments are also carried out for the CES-produced MPs in comparison with those by a single axial electrospray process. Our experimental results show that the CES process can be effectively controlled to encapsulate drugs of low aqueous solubility for high encapsulation efficiency and optimal drug release profiles.

No MeSH data available.