Limits...
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.


Differential scanning calorimetry thermograms of poly (lactide-co-glycolide) (PLGA), 18-β-glycyrrhetinic acid (GLA), their physical mixture and GLA loaded PLGA nanoparticles.
© Copyright Policy
Related In: Results  -  Collection

License
getmorefigures.php?uid=PMC4403053&req=5

Figure 3: Differential scanning calorimetry thermograms of poly (lactide-co-glycolide) (PLGA), 18-β-glycyrrhetinic acid (GLA), their physical mixture and GLA loaded PLGA nanoparticles.

Mentions: DSC was used to investigate the thermal behavior of formulations. Figure 3 shows that pure PLGA exhibits an endothermic peak at 60 °C which can be related to its relaxation peak following the glass transition phase. Due to the amorphous nature of PLGA, no melting point was observed in PLGA thermograms. The pure GLA demonstrated a sharp peak at 300 °C which can be related to its melting point. The DSC thermograms of the physical mixture of GLA and PLGA showed peaks which were the result of plain superposition of each of the two substances DSC thermograms. The enthalpy reduction for the physical mixture of drug and polymer can be explained by the presence of smaller amount of drug molecules in the mixture in comparison with pure drug. The DSC curve of GLA containing NPs did not show the endothermic peak of GLA which suggests that the drug is incorporated into the nanoparticles in a disordered and amorphous shape. Any severe alteration in the thermal behavior of either the polymer or the drug may be related to drug polymer interaction (33). In the current study no formation of any new peak and no shifting of any peak in the DSC thermogram was observed.


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)

Differential scanning calorimetry thermograms of poly (lactide-co-glycolide) (PLGA), 18-β-glycyrrhetinic acid (GLA), their physical mixture and GLA loaded PLGA nanoparticles.
© Copyright Policy
Related In: Results  -  Collection

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

Figure 3: Differential scanning calorimetry thermograms of poly (lactide-co-glycolide) (PLGA), 18-β-glycyrrhetinic acid (GLA), their physical mixture and GLA loaded PLGA nanoparticles.
Mentions: DSC was used to investigate the thermal behavior of formulations. Figure 3 shows that pure PLGA exhibits an endothermic peak at 60 °C which can be related to its relaxation peak following the glass transition phase. Due to the amorphous nature of PLGA, no melting point was observed in PLGA thermograms. The pure GLA demonstrated a sharp peak at 300 °C which can be related to its melting point. The DSC thermograms of the physical mixture of GLA and PLGA showed peaks which were the result of plain superposition of each of the two substances DSC thermograms. The enthalpy reduction for the physical mixture of drug and polymer can be explained by the presence of smaller amount of drug molecules in the mixture in comparison with pure drug. The DSC curve of GLA containing NPs did not show the endothermic peak of GLA which suggests that the drug is incorporated into the nanoparticles in a disordered and amorphous shape. Any severe alteration in the thermal behavior of either the polymer or the drug may be related to drug polymer interaction (33). In the current study no formation of any new peak and no shifting of any peak in the DSC thermogram was observed.

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.