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Preparation and Antibacterial Activity Evaluation of 18-β-glycyrrhetinic Acid Loaded PLGA Nanoparticles.

Darvishi B, Manoochehri S, Kamalinia G, Samadi N, Amini M, Mostafavi SH, Maghazei S, Atyabi F, Dinarvand R - Iran J Pharm Res (2015)

Bottom Line: Zeta potential of the developed nanoparticles was fairly negative (-11±1.5).The antimicrobial results revealed that the nanoparticles were more effective than pure GLA against P. aeuroginosa, S. aureus and S. epidermidis. This improvement in antibacterial activity of GLA loaded nanoparticles when compared to pure GLA may be related to higher nanoparticles penetration into infected cells and a higher amount of GLA delivery in its site of action.Herein, it was shown that GLA loaded PLGA nanoparticles displayed appropriate physicochemical properties as well as an improved antimicrobial effect.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

ABSTRACT
The aim of the present study was to formulate poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with 18-β-glycyrrhetinic acid (GLA) with appropriate physicochemical properties and antimicrobial activity. GLA loaded PLGA nanoparticles were prepared with different drug to polymer ratios, acetone contents and sonication times and the antibacterial activity of the developed nanoparticles was examined against different gram-negative and gram-positive bacteria. The antibacterial effect was studied using serial dilution technique to determine the minimum inhibitory concentration of nanoparticles. Results demonstrated that physicochemical properties of nanoparticles were affected by the above mentioned parameters where nanoscale size particles ranging from 175 to 212 nm were achieved. The highest encapsulation efficiency (53.2 ± 2.4%) was obtained when the ratio of drug to polymer was 1:4. Zeta potential of the developed nanoparticles was fairly negative (-11±1.5). In-vitro release profile of nanoparticles showed two phases: an initial phase of burst release for 10 h followed by a slow release pattern up to the end. The antimicrobial results revealed that the nanoparticles were more effective than pure GLA against P. aeuroginosa, S. aureus and S. epidermidis. This improvement in antibacterial activity of GLA loaded nanoparticles when compared to pure GLA may be related to higher nanoparticles penetration into infected cells and a higher amount of GLA delivery in its site of action. Herein, it was shown that GLA loaded PLGA nanoparticles displayed appropriate physicochemical properties as well as an improved antimicrobial effect.

No MeSH data available.


Particle size distribution of nanoparticles with drug to polymer ratios of [a] (1:1) and [b] (1:2) prepared by sonication/ solvent evaporation technique
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Figure 1: Particle size distribution of nanoparticles with drug to polymer ratios of [a] (1:1) and [b] (1:2) prepared by sonication/ solvent evaporation technique

Mentions: GLA loaded NPs were prepared by sonication/ solvent evaporation method. Encapsulation efficiency, drug loading, size, polydispersity index and zeta potential of GLA loaded NPs are reported in Table1. According to Table 1, NPs size was in the range of 175 to 212 nm and the prepared nanoparticles were highly uniform and monodispersed (Figures 1a and 1b). By increasing the drug to polymer ratio from 1:1 to 1:4, size was increased from 184 to 212 nm. This result may be related to an increase in viscous forces of droplets which resists against droplets break down by sonication especially in higher polymer concentrations. These resisting forces stand against the shear forces in the oil phase and determine the final size and particle size distribution in nanoparticles (26). Furthermore, Table 1 shows that by increasing the amount of polymer, higher encapsulation efficiencies were achieved. Maximum encapsulation efficiency was attained when the amount of drug to polymer ratio was 1:4. As it is observed higher polymer concentration is related to a higher encapsulation efficiency which may be explained in two different ways. First, it can be proposed that when the polymer concentration is high, the polymer molecules may precipitate on the surface of the dispersed phase droplets. As a result drug molecules diffusion through the two phases boundary is restricted and a higher encapsulation efficiency is achieved (27). Alternatively, it may be proposed that a higher polymer concentration can increase the viscosity of the system and make a barrier toward the free diffusion of drug molecules through the boundary phase of polymeric droplets (28).


Preparation and Antibacterial Activity Evaluation of 18-β-glycyrrhetinic Acid Loaded PLGA Nanoparticles.

Darvishi B, Manoochehri S, Kamalinia G, Samadi N, Amini M, Mostafavi SH, Maghazei S, Atyabi F, Dinarvand R - Iran J Pharm Res (2015)

Particle size distribution of nanoparticles with drug to polymer ratios of [a] (1:1) and [b] (1:2) prepared by sonication/ solvent evaporation technique
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4403053&req=5

Figure 1: Particle size distribution of nanoparticles with drug to polymer ratios of [a] (1:1) and [b] (1:2) prepared by sonication/ solvent evaporation technique
Mentions: GLA loaded NPs were prepared by sonication/ solvent evaporation method. Encapsulation efficiency, drug loading, size, polydispersity index and zeta potential of GLA loaded NPs are reported in Table1. According to Table 1, NPs size was in the range of 175 to 212 nm and the prepared nanoparticles were highly uniform and monodispersed (Figures 1a and 1b). By increasing the drug to polymer ratio from 1:1 to 1:4, size was increased from 184 to 212 nm. This result may be related to an increase in viscous forces of droplets which resists against droplets break down by sonication especially in higher polymer concentrations. These resisting forces stand against the shear forces in the oil phase and determine the final size and particle size distribution in nanoparticles (26). Furthermore, Table 1 shows that by increasing the amount of polymer, higher encapsulation efficiencies were achieved. Maximum encapsulation efficiency was attained when the amount of drug to polymer ratio was 1:4. As it is observed higher polymer concentration is related to a higher encapsulation efficiency which may be explained in two different ways. First, it can be proposed that when the polymer concentration is high, the polymer molecules may precipitate on the surface of the dispersed phase droplets. As a result drug molecules diffusion through the two phases boundary is restricted and a higher encapsulation efficiency is achieved (27). Alternatively, it may be proposed that a higher polymer concentration can increase the viscosity of the system and make a barrier toward the free diffusion of drug molecules through the boundary phase of polymeric droplets (28).

Bottom Line: Zeta potential of the developed nanoparticles was fairly negative (-11±1.5).The antimicrobial results revealed that the nanoparticles were more effective than pure GLA against P. aeuroginosa, S. aureus and S. epidermidis. This improvement in antibacterial activity of GLA loaded nanoparticles when compared to pure GLA may be related to higher nanoparticles penetration into infected cells and a higher amount of GLA delivery in its site of action.Herein, it was shown that GLA loaded PLGA nanoparticles displayed appropriate physicochemical properties as well as an improved antimicrobial effect.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

ABSTRACT
The aim of the present study was to formulate poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with 18-β-glycyrrhetinic acid (GLA) with appropriate physicochemical properties and antimicrobial activity. GLA loaded PLGA nanoparticles were prepared with different drug to polymer ratios, acetone contents and sonication times and the antibacterial activity of the developed nanoparticles was examined against different gram-negative and gram-positive bacteria. The antibacterial effect was studied using serial dilution technique to determine the minimum inhibitory concentration of nanoparticles. Results demonstrated that physicochemical properties of nanoparticles were affected by the above mentioned parameters where nanoscale size particles ranging from 175 to 212 nm were achieved. The highest encapsulation efficiency (53.2 ± 2.4%) was obtained when the ratio of drug to polymer was 1:4. Zeta potential of the developed nanoparticles was fairly negative (-11±1.5). In-vitro release profile of nanoparticles showed two phases: an initial phase of burst release for 10 h followed by a slow release pattern up to the end. The antimicrobial results revealed that the nanoparticles were more effective than pure GLA against P. aeuroginosa, S. aureus and S. epidermidis. This improvement in antibacterial activity of GLA loaded nanoparticles when compared to pure GLA may be related to higher nanoparticles penetration into infected cells and a higher amount of GLA delivery in its site of action. Herein, it was shown that GLA loaded PLGA nanoparticles displayed appropriate physicochemical properties as well as an improved antimicrobial effect.

No MeSH data available.