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

Context Metformin is an important oral anti-hyperglycemic used in diabetes. Polylactic-co-glycolic acid (PLGA) has been widely used due to its reliability in controlling the release of drugs. Objective This study evaluates the in vitro-in vivo availability of metformin hydrochloride-loaded polylacti...

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Autores principales: Aline de Sousa Barbosa Freitas Pereira, Maria Laura de Souza Lima, Arnobio Antonio da Silva-Junior, Emanuell dos Santos Silva, Raimundo Fernandes de Araújo Júnior, Agnes Andrade Martins, Jovelina Samara Ferreira Alves, Artur de Santana Oliveira, Leandro De Santis Ferreira, Emily Cintia Tossi de Araújo Costa, Gerlane Coelho Bernardo Guerra, Caroline Addison Carvalho Xavier de Medeiros, Gerly A. C. Brito, Renata Ferreira de Carvalho Leitao, Aurigena Antunes de Araújo
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Publicado: Taylor & Francis Group 2021
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spelling oai:doaj.org-article:7d4d72e176694e5aa3a792b23b8a3c962021-11-26T11:19:47ZIn vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model1388-02091744-511610.1080/13880209.2021.2002369https://doaj.org/article/7d4d72e176694e5aa3a792b23b8a3c962021-01-01T00:00:00Zhttp://dx.doi.org/10.1080/13880209.2021.2002369https://doaj.org/toc/1388-0209https://doaj.org/toc/1744-5116Context Metformin is an important oral anti-hyperglycemic used in diabetes. Polylactic-co-glycolic acid (PLGA) has been widely used due to its reliability in controlling the release of drugs. Objective This study evaluates the in vitro-in vivo availability of metformin hydrochloride-loaded polylactic-co-glycolic acid. Material and methods In vitro metformin release (Met-free or PLGA + Met-12.5 mg/mL per 360 min) was evaluated using static Franz vertical diffusion cells. The in vivo study was performed with two control groups (validation bioanalytical method) and two experimental groups of diabetic male Wistar rats treated with PLGA + Met 10 mg/kg or Met 100 mg/kg by oral gavage. Diabetes was induced by streptozotocin (40 mg/kg) through the penile vein. Blood samples were collected 0.5, 1, 4, 7, 10, 12, 18, 24, 36, 48 and 72 h and analysed by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Results PLGA + Met 10 mg/kg was released in the in vitro assay suggesting a parabolic diffusion kinetic model (K −0.0619−0.5h) with a 100% release profile in 10 h by controlled diffusion. The in vivo assay showed the apparent volume of distribution Vz/F (PLGA + Met 10 mg/kg, 40971.8 mL/kg vs. Met 100 mg/kg, 2174.58 mL/kg) and mean residence time MRTinf (PLGA + Met 10 mg/kg, 37.66 h vs. Met 100 mg/kg, 3.34 h). Discussion and Conclusions The formulation modifies pharmacokinetics parameters such as apparent distribution volume and mean residence time. The PLGA + Met 10 mg/kg had a slower elimination rate compared to Met 100 mg/kg in diabetic rats in a periodontal disease experimental model.Aline de Sousa Barbosa Freitas PereiraMaria Laura de Souza LimaArnobio Antonio da Silva-JuniorEmanuell dos Santos SilvaRaimundo Fernandes de Araújo JúniorAgnes Andrade MartinsJovelina Samara Ferreira AlvesArtur de Santana OliveiraLeandro De Santis FerreiraEmily Cintia Tossi de Araújo CostaGerlane Coelho Bernardo GuerraCaroline Addison Carvalho Xavier de MedeirosGerly A. C. BritoRenata Ferreira de Carvalho LeitaoAurigena Antunes de AraújoTaylor & Francis Grouparticlepolylactic-co-glycolic acidbioavailabilitydiabetesTherapeutics. PharmacologyRM1-950ENPharmaceutical Biology, Vol 59, Iss 1, Pp 1576-1584 (2021)
institution DOAJ
collection DOAJ
language EN
topic polylactic-co-glycolic acid
bioavailability
diabetes
Therapeutics. Pharmacology
RM1-950
spellingShingle polylactic-co-glycolic acid
bioavailability
diabetes
Therapeutics. Pharmacology
RM1-950
Aline de Sousa Barbosa Freitas Pereira
Maria Laura de Souza Lima
Arnobio Antonio da Silva-Junior
Emanuell dos Santos Silva
Raimundo Fernandes de Araújo Júnior
Agnes Andrade Martins
Jovelina Samara Ferreira Alves
Artur de Santana Oliveira
Leandro De Santis Ferreira
Emily Cintia Tossi de Araújo Costa
Gerlane Coelho Bernardo Guerra
Caroline Addison Carvalho Xavier de Medeiros
Gerly A. C. Brito
Renata Ferreira de Carvalho Leitao
Aurigena Antunes de Araújo
In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model
description Context Metformin is an important oral anti-hyperglycemic used in diabetes. Polylactic-co-glycolic acid (PLGA) has been widely used due to its reliability in controlling the release of drugs. Objective This study evaluates the in vitro-in vivo availability of metformin hydrochloride-loaded polylactic-co-glycolic acid. Material and methods In vitro metformin release (Met-free or PLGA + Met-12.5 mg/mL per 360 min) was evaluated using static Franz vertical diffusion cells. The in vivo study was performed with two control groups (validation bioanalytical method) and two experimental groups of diabetic male Wistar rats treated with PLGA + Met 10 mg/kg or Met 100 mg/kg by oral gavage. Diabetes was induced by streptozotocin (40 mg/kg) through the penile vein. Blood samples were collected 0.5, 1, 4, 7, 10, 12, 18, 24, 36, 48 and 72 h and analysed by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Results PLGA + Met 10 mg/kg was released in the in vitro assay suggesting a parabolic diffusion kinetic model (K −0.0619−0.5h) with a 100% release profile in 10 h by controlled diffusion. The in vivo assay showed the apparent volume of distribution Vz/F (PLGA + Met 10 mg/kg, 40971.8 mL/kg vs. Met 100 mg/kg, 2174.58 mL/kg) and mean residence time MRTinf (PLGA + Met 10 mg/kg, 37.66 h vs. Met 100 mg/kg, 3.34 h). Discussion and Conclusions The formulation modifies pharmacokinetics parameters such as apparent distribution volume and mean residence time. The PLGA + Met 10 mg/kg had a slower elimination rate compared to Met 100 mg/kg in diabetic rats in a periodontal disease experimental model.
format article
author Aline de Sousa Barbosa Freitas Pereira
Maria Laura de Souza Lima
Arnobio Antonio da Silva-Junior
Emanuell dos Santos Silva
Raimundo Fernandes de Araújo Júnior
Agnes Andrade Martins
Jovelina Samara Ferreira Alves
Artur de Santana Oliveira
Leandro De Santis Ferreira
Emily Cintia Tossi de Araújo Costa
Gerlane Coelho Bernardo Guerra
Caroline Addison Carvalho Xavier de Medeiros
Gerly A. C. Brito
Renata Ferreira de Carvalho Leitao
Aurigena Antunes de Araújo
author_facet Aline de Sousa Barbosa Freitas Pereira
Maria Laura de Souza Lima
Arnobio Antonio da Silva-Junior
Emanuell dos Santos Silva
Raimundo Fernandes de Araújo Júnior
Agnes Andrade Martins
Jovelina Samara Ferreira Alves
Artur de Santana Oliveira
Leandro De Santis Ferreira
Emily Cintia Tossi de Araújo Costa
Gerlane Coelho Bernardo Guerra
Caroline Addison Carvalho Xavier de Medeiros
Gerly A. C. Brito
Renata Ferreira de Carvalho Leitao
Aurigena Antunes de Araújo
author_sort Aline de Sousa Barbosa Freitas Pereira
title In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model
title_short In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model
title_full In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model
title_fullStr In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model
title_full_unstemmed In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model
title_sort in vitro-in vivo availability of metformin hydrochloride-plga nanoparticles in diabetic rats in a periodontal disease experimental model
publisher Taylor & Francis Group
publishDate 2021
url https://doaj.org/article/7d4d72e176694e5aa3a792b23b8a3c96
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