Nanoparticles Obtained from Zein for Encapsulation of Mesalazine

We encapsulated MSZ in zein nanoparticles (NP-ZN) using a desolvation method followed by drying in a mini spray dryer. These nanoparticles exhibited a size of 266.6 ± 52 nm, IPD of 0.14 ± 1.1 and zeta potential of −36.4 ± 1.5 mV, suggesting colloidal stability. Quantification using HPLC showed a dru...

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Main Authors: Izabela Borges C. Lima, Lina Clara G. A. I. Moreno, Ana Victória Peres, Ana Cristina Gramoza Santana, Adonias Carvalho, Mariana H. Chaves, Lorena Lima, Rayran Walter Sousa, Dalton Dittz, Hercília M. L. Rolim, Lívio César Cunha Nunes
Format: Article
Language:English
Published: MDPI AG 2022-12-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/14/12/2830
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author Izabela Borges C. Lima
Lina Clara G. A. I. Moreno
Ana Victória Peres
Ana Cristina Gramoza Santana
Adonias Carvalho
Mariana H. Chaves
Lorena Lima
Rayran Walter Sousa
Dalton Dittz
Hercília M. L. Rolim
Lívio César Cunha Nunes
author_facet Izabela Borges C. Lima
Lina Clara G. A. I. Moreno
Ana Victória Peres
Ana Cristina Gramoza Santana
Adonias Carvalho
Mariana H. Chaves
Lorena Lima
Rayran Walter Sousa
Dalton Dittz
Hercília M. L. Rolim
Lívio César Cunha Nunes
author_sort Izabela Borges C. Lima
collection DOAJ
description We encapsulated MSZ in zein nanoparticles (NP-ZN) using a desolvation method followed by drying in a mini spray dryer. These nanoparticles exhibited a size of 266.6 ± 52 nm, IPD of 0.14 ± 1.1 and zeta potential of −36.4 ± 1.5 mV, suggesting colloidal stability. Quantification using HPLC showed a drug-loaded of 43.8 µg/mg. SEM demonstrated a spherical morphology with a size variation from 220 to 400 nm. A FTIR analysis did not show drug spectra in the NPs in relation to the physical mixture, which suggests drug encapsulation without changing its chemical structure. A TGA analysis showed thermal stability up to 300 °C. In vitro release studies demonstrated gastroresistance and a sustained drug release at pH 7.4 (97.67 ± 0.32%) in 120 h. The kinetic model used for the release of MSZ from the NP-ZN in a pH 1.2 medium was the Fickian diffusion, in a pH 6.8 medium it was the Peppas–Sahlin model with the polymeric relaxation mechanism and in a pH 7.4 medium it was the Korsmeyer–Peppas model with the Fickian release mechanism, or “Case I”. An in vitro cytotoxicity study in the CT26.WT cell line showed no basal cytotoxicity up to 500 μg/mL. The NP-ZN showed to be a promising vector for the sustained release of MSZ in the colon by oral route.
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spelling doaj.art-5520f8d93f2844179b5a9a162940a0ba2023-11-24T17:22:45ZengMDPI AGPharmaceutics1999-49232022-12-011412283010.3390/pharmaceutics14122830Nanoparticles Obtained from Zein for Encapsulation of MesalazineIzabela Borges C. Lima0Lina Clara G. A. I. Moreno1Ana Victória Peres2Ana Cristina Gramoza Santana3Adonias Carvalho4Mariana H. Chaves5Lorena Lima6Rayran Walter Sousa7Dalton Dittz8Hercília M. L. Rolim9Lívio César Cunha Nunes10Laboratory of Technological Innovation, Entrepreneurship, Medicines and Related (LITE), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilPharmaceutical Nanosystems Laboratory (NANOSFAR), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilLaboratory of Technological Innovation, Entrepreneurship, Medicines and Related (LITE), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilLaboratory of Technological Innovation, Entrepreneurship, Medicines and Related (LITE), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilNatural Products Laboratory (LPN), Department of Chemistry, Federal University of Piauí, Teresina 64049-550, PI, BrazilNatural Products Laboratory (LPN), Department of Chemistry, Federal University of Piauí, Teresina 64049-550, PI, BrazilLaboratory of Technological Innovation, Entrepreneurship, Medicines and Related (LITE), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilLaboratory of Experimental Cancerology (LabCâncer), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilLaboratory of Experimental Cancerology (LabCâncer), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilPharmaceutical Nanosystems Laboratory (NANOSFAR), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilLaboratory of Technological Innovation, Entrepreneurship, Medicines and Related (LITE), Nucleus of Pharmaceutical Technology, Federal University of Piauí, Teresina 64049-550, PI, BrazilWe encapsulated MSZ in zein nanoparticles (NP-ZN) using a desolvation method followed by drying in a mini spray dryer. These nanoparticles exhibited a size of 266.6 ± 52 nm, IPD of 0.14 ± 1.1 and zeta potential of −36.4 ± 1.5 mV, suggesting colloidal stability. Quantification using HPLC showed a drug-loaded of 43.8 µg/mg. SEM demonstrated a spherical morphology with a size variation from 220 to 400 nm. A FTIR analysis did not show drug spectra in the NPs in relation to the physical mixture, which suggests drug encapsulation without changing its chemical structure. A TGA analysis showed thermal stability up to 300 °C. In vitro release studies demonstrated gastroresistance and a sustained drug release at pH 7.4 (97.67 ± 0.32%) in 120 h. The kinetic model used for the release of MSZ from the NP-ZN in a pH 1.2 medium was the Fickian diffusion, in a pH 6.8 medium it was the Peppas–Sahlin model with the polymeric relaxation mechanism and in a pH 7.4 medium it was the Korsmeyer–Peppas model with the Fickian release mechanism, or “Case I”. An in vitro cytotoxicity study in the CT26.WT cell line showed no basal cytotoxicity up to 500 μg/mL. The NP-ZN showed to be a promising vector for the sustained release of MSZ in the colon by oral route.https://www.mdpi.com/1999-4923/14/12/2830natural polymerzein5-ASAnanoparticlescolon
spellingShingle Izabela Borges C. Lima
Lina Clara G. A. I. Moreno
Ana Victória Peres
Ana Cristina Gramoza Santana
Adonias Carvalho
Mariana H. Chaves
Lorena Lima
Rayran Walter Sousa
Dalton Dittz
Hercília M. L. Rolim
Lívio César Cunha Nunes
Nanoparticles Obtained from Zein for Encapsulation of Mesalazine
Pharmaceutics
natural polymer
zein
5-ASA
nanoparticles
colon
title Nanoparticles Obtained from Zein for Encapsulation of Mesalazine
title_full Nanoparticles Obtained from Zein for Encapsulation of Mesalazine
title_fullStr Nanoparticles Obtained from Zein for Encapsulation of Mesalazine
title_full_unstemmed Nanoparticles Obtained from Zein for Encapsulation of Mesalazine
title_short Nanoparticles Obtained from Zein for Encapsulation of Mesalazine
title_sort nanoparticles obtained from zein for encapsulation of mesalazine
topic natural polymer
zein
5-ASA
nanoparticles
colon
url https://www.mdpi.com/1999-4923/14/12/2830
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