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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.


Core-shell structure of curcumin-loaded PLGA droplets produced by CES.(a) Confocal fluorescence microscopic image of droplets showing the shell shape (Nile red 0.01 w% in outer liquid); (b) Confocal fluorescence microscopic image of MPs showing the core (I), the shell (II) and the core-shell shapes (III) (Nile red 0.01 w% in outer liquid and coumarin-6 0.01 w% in inner liquid). The applied voltages: V1 = 4.8 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution, Qout = 1.0 mL/h; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.5 mL/h; The vertical distances: h = 0.2 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.
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pone.0132609.g006: Core-shell structure of curcumin-loaded PLGA droplets produced by CES.(a) Confocal fluorescence microscopic image of droplets showing the shell shape (Nile red 0.01 w% in outer liquid); (b) Confocal fluorescence microscopic image of MPs showing the core (I), the shell (II) and the core-shell shapes (III) (Nile red 0.01 w% in outer liquid and coumarin-6 0.01 w% in inner liquid). The applied voltages: V1 = 4.8 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution, Qout = 1.0 mL/h; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.5 mL/h; The vertical distances: h = 0.2 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.

Mentions: Confocal laser scanning microscopy (CLSM) and scanning electron microscopy (SEM) have been commonly used to show the core-shell structure of the multilayered MPs. In this work, the morphology of curcumin-loaded PLGA droplets collected in the PVA solution are first observed by CLSM imaging. When the outer PLGA solution is added by Nile red (0.01 w%), a circular shape of the shell can be clearly observed by the CLSM imaging, as shown in Fig 6(a). When the inner curcumin solution is further stained by coumarin-6 (0.01 w%), the core-shell structure with PLGA as the shell and curcumin solution as the core can be imaged by different channels of CLSM system, as indicated in Fig 6(b). The confocal fluorescence images show that the curcumin-loaded PLGA droplets have a satisfactory morphology and a core-shell structure.


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)

Core-shell structure of curcumin-loaded PLGA droplets produced by CES.(a) Confocal fluorescence microscopic image of droplets showing the shell shape (Nile red 0.01 w% in outer liquid); (b) Confocal fluorescence microscopic image of MPs showing the core (I), the shell (II) and the core-shell shapes (III) (Nile red 0.01 w% in outer liquid and coumarin-6 0.01 w% in inner liquid). The applied voltages: V1 = 4.8 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution, Qout = 1.0 mL/h; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.5 mL/h; The vertical distances: h = 0.2 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.
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pone.0132609.g006: Core-shell structure of curcumin-loaded PLGA droplets produced by CES.(a) Confocal fluorescence microscopic image of droplets showing the shell shape (Nile red 0.01 w% in outer liquid); (b) Confocal fluorescence microscopic image of MPs showing the core (I), the shell (II) and the core-shell shapes (III) (Nile red 0.01 w% in outer liquid and coumarin-6 0.01 w% in inner liquid). The applied voltages: V1 = 4.8 kV, V2 = 1.5 kV, V3 = -5 kV; The outer liquid: 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution, Qout = 1.0 mL/h; The inner liquid: 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution, Qin = 0.5 mL/h; The vertical distances: h = 0.2 mm, H1 = 2 mm, H2 = 20 mm, H3 = 80 mm.
Mentions: Confocal laser scanning microscopy (CLSM) and scanning electron microscopy (SEM) have been commonly used to show the core-shell structure of the multilayered MPs. In this work, the morphology of curcumin-loaded PLGA droplets collected in the PVA solution are first observed by CLSM imaging. When the outer PLGA solution is added by Nile red (0.01 w%), a circular shape of the shell can be clearly observed by the CLSM imaging, as shown in Fig 6(a). When the inner curcumin solution is further stained by coumarin-6 (0.01 w%), the core-shell structure with PLGA as the shell and curcumin solution as the core can be imaged by different channels of CLSM system, as indicated in Fig 6(b). The confocal fluorescence images show that the curcumin-loaded PLGA droplets have a satisfactory morphology and a core-shell structure.

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.