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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.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.

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.


Comparison of the curcumin release profiles versus time at different conditions.(a) Picture of four samples and schematics of corresponding structures of free curcumin, ES and CES MPs; (b) Drug release profile in 40 days of free curcumin and MPs prepared by ES and CES; (c) The enlarged figure of the release profile in first 12 hours.
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pone.0132609.g008: Comparison of the curcumin release profiles versus time at different conditions.(a) Picture of four samples and schematics of corresponding structures of free curcumin, ES and CES MPs; (b) Drug release profile in 40 days of free curcumin and MPs prepared by ES and CES; (c) The enlarged figure of the release profile in first 12 hours.

Mentions: The curcumin-loaded PLGA MPs are fabricated by the CES process. The drug release profiles of these MPs are tested and compared with those of free curcumin and curcumin-PLGA matrix produced by single axial electrospray (ES), as shown in Fig 8. For two CES-produced MP formulations (as denoted by “1:1 CES MPs” and “1.5:1 CES MPs” in Fig 8), the inner liquid flow rate is the same (i.e., Qin = 1.0 mL/h) and the outer liquid flow rate is different (i.e., Qout = 1.0 mL/h and 1.5 mL/h, respectively). The outer liquid is 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution, and the inner liquid is 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution. The applied voltages are V1 = 4.8 kV, V2 = 1.5 kV, V3 = -8 kV and the vertical distances are h = 0.2 mm, H1 = 2.5 mm, H2 = 20 mm, H3 = 80 mm, respectively. The ES MPs are fabricated in an ES device, which is similar to the CES one but utilizes a single needle with an inner diameter of 1.01 mm and an outer diameter of 1.48 mm instead of the coaxial needle. The ES liquid is prepared by mixing 1:1 v/v the inner curcumin and the outer PLGA solutions in the CES case. The liquid flow rate is set as 2.0 mL/h and the applied positive voltages are adjusted as V1 = 5.5 kV, V2 = 1.5 kV, V3 = -8 kV to achieve a stable cone-jet mode and a mean droplet diameter of about 4 μm. The fabrication process and the post-processing for obtaining the ES MPs are similar to those in the CES experiments.


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)

Comparison of the curcumin release profiles versus time at different conditions.(a) Picture of four samples and schematics of corresponding structures of free curcumin, ES and CES MPs; (b) Drug release profile in 40 days of free curcumin and MPs prepared by ES and CES; (c) The enlarged figure of the release profile in first 12 hours.
© Copyright Policy
Related In: Results  -  Collection

License
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getmorefigures.php?uid=PMC4514801&req=5

pone.0132609.g008: Comparison of the curcumin release profiles versus time at different conditions.(a) Picture of four samples and schematics of corresponding structures of free curcumin, ES and CES MPs; (b) Drug release profile in 40 days of free curcumin and MPs prepared by ES and CES; (c) The enlarged figure of the release profile in first 12 hours.
Mentions: The curcumin-loaded PLGA MPs are fabricated by the CES process. The drug release profiles of these MPs are tested and compared with those of free curcumin and curcumin-PLGA matrix produced by single axial electrospray (ES), as shown in Fig 8. For two CES-produced MP formulations (as denoted by “1:1 CES MPs” and “1.5:1 CES MPs” in Fig 8), the inner liquid flow rate is the same (i.e., Qin = 1.0 mL/h) and the outer liquid flow rate is different (i.e., Qout = 1.0 mL/h and 1.5 mL/h, respectively). The outer liquid is 10.0 w% PLGA (Mw = 10,000) in ethyl acetate solution, and the inner liquid is 4.0 w% curcumin and 1.0 w% PLGA (Mw = 50,000) in acetone solution. The applied voltages are V1 = 4.8 kV, V2 = 1.5 kV, V3 = -8 kV and the vertical distances are h = 0.2 mm, H1 = 2.5 mm, H2 = 20 mm, H3 = 80 mm, respectively. The ES MPs are fabricated in an ES device, which is similar to the CES one but utilizes a single needle with an inner diameter of 1.01 mm and an outer diameter of 1.48 mm instead of the coaxial needle. The ES liquid is prepared by mixing 1:1 v/v the inner curcumin and the outer PLGA solutions in the CES case. The liquid flow rate is set as 2.0 mL/h and the applied positive voltages are adjusted as V1 = 5.5 kV, V2 = 1.5 kV, V3 = -8 kV to achieve a stable cone-jet mode and a mean droplet diameter of about 4 μm. The fabrication process and the post-processing for obtaining the ES MPs are similar to those in the CES experiments.

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.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.

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.