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Research Article

In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model

, , , ORCID Icon, ORCID Icon, , , , ORCID Icon, , , , , & ORCID Icon show all
Pages 1574-1582 | Received 02 Jul 2021, Accepted 29 Oct 2021, Published online: 22 Nov 2021

Figures & data

Table 1. MS/MS settings for compound-dependent parameters for metformin and internal standard isoniazid.

Figure 1. Experimental in vitro drug release profile from free-drug and MET-loaded nanoparticles; respective mathematical modelling adjustment of data using: B) first-order model; C) Bhaskar model; D) modified Freundlich model; and E) Parabolic model. Notes: Notes: The samples can be identified as follows: (

) Solution of pure MET; (
) MET-loaded nanoparticles. The data are expressed as the mean ± standard deviation (SD) (n = 3).

Figure 1. Experimental in vitro drug release profile from free-drug and MET-loaded nanoparticles; respective mathematical modelling adjustment of data using: B) first-order model; C) Bhaskar model; D) modified Freundlich model; and E) Parabolic model. Notes: Notes: The samples can be identified as follows: (Display full size) Solution of pure MET; (Display full size) MET-loaded nanoparticles. The data are expressed as the mean ± standard deviation (SD) (n = 3).

Figure 2. Residual plots for metformin.

Figure 2. Residual plots for metformin.

Table 2. Linear regression data.

Figure 3. Chromatograms from selectivity study. Blank plasma chromatograms in purple, blue, red and green; blank hemolyzed plasma chromatogram in pink; blank lipemic plasma chromatogram in orange; PLGA + plasma in yellow; metformin 250 ug mL−1 in black (m/z 130.1 → m/z 60.1) and isoniazide 1000 ng mL−1 in grey (m/z 138.1 → m/z 121.1).

Figure 3. Chromatograms from selectivity study. Blank plasma chromatograms in purple, blue, red and green; blank hemolyzed plasma chromatogram in pink; blank lipemic plasma chromatogram in orange; PLGA + plasma in yellow; metformin 250 ug mL−1 in black (m/z 130.1 → m/z 60.1) and isoniazide 1000 ng mL−1 in grey (m/z 138.1 → m/z 121.1).

Table 3. Concentration of standards used for the calibration curve.

Figure 4. Bioavailability of metformin in single dose administration of metformin in saline and in formulation by oral gavage. Red: Met 100 mg + kg (metformin 100 mg/kg in saline solution, n = 4). Black: PLGA + MET 10 mg/kg (metformin 10 mg/kg in formulation containing PLGA, n = 4) in black.

Figure 4. Bioavailability of metformin in single dose administration of metformin in saline and in formulation by oral gavage. Red: Met 100 mg + kg (metformin 100 mg/kg in saline solution, n = 4). Black: PLGA + MET 10 mg/kg (metformin 10 mg/kg in formulation containing PLGA, n = 4) in black.

Table 4. Matrix effect results.

Table 5. Parameters estimates of MET pharmacokinetics with noncompartmental model in rat plasma by PKanalix version 2019R2 for PLGA + MET 10 mg kg−1 (metformin 10 mg kg−1 in formulation containing PLGA, n = 4) and MET 100 mg kg−1 (metformin 100 mg Kg−1 in saline solution, n = 4).