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Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers
Loading small molecular weight hydrophilic drugs into polymeric carriers is a challenging task. Metformin hydrochloride (MET) is a highly soluble oral antidiabetic drug of small size and high cationic charge. Hydrophobic ion pairing (HIP) is an approach for reversible modulation of solubility and hy...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8986808/ https://www.ncbi.nlm.nih.gov/pubmed/35388027 http://dx.doi.org/10.1038/s41598-022-09384-6 |
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author | Abd-El Hafeez, Sara I. Eleraky, Nermin E. Hafez, Ehsan Abouelmagd, Sara A. |
author_facet | Abd-El Hafeez, Sara I. Eleraky, Nermin E. Hafez, Ehsan Abouelmagd, Sara A. |
author_sort | Abd-El Hafeez, Sara I. |
collection | PubMed |
description | Loading small molecular weight hydrophilic drugs into polymeric carriers is a challenging task. Metformin hydrochloride (MET) is a highly soluble oral antidiabetic drug of small size and high cationic charge. Hydrophobic ion pairing (HIP) is an approach for reversible modulation of solubility and hydrophilicity of water-soluble drugs via complexation with oppositely charged molecules. Herein, we prepared MET ion pairs and carefully studied and characterized MET interaction with different ligands, with the aim of increasing MET lipophilicity and loading efficiency. HIP was successful using three hydrophilic anionic ligands; sodium dodecyl sulphate (SDS) Carbopol (CB) and tannic acid (TA). Electrostatic interaction and hydrogen bonding drove the complexation per spectroscopic and thermal studies. Complexation efficiency depended on ligand type and charge ratio. While complexes had varying interaction strengths, the excessive stability of TA/MET resulted in unfavorable poor MET dissociation. Notably, HIP imparted a 450 and tenfold lipophilicity increase for SDS/MET and CB/MET, respectively. The latter showed favorable controlled, yet complete release of MET at pH 6.8 and was loaded into alginate beads. Complex bulkiness and decreased lipophilicity resulted in a dramatic 88% increase of MET loading, demonstrating the success of HIP as a simple, efficient and applicable approach for modulating drug’s properties. |
format | Online Article Text |
id | pubmed-8986808 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Nature Publishing Group UK |
record_format | MEDLINE/PubMed |
spelling | pubmed-89868082022-04-08 Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers Abd-El Hafeez, Sara I. Eleraky, Nermin E. Hafez, Ehsan Abouelmagd, Sara A. Sci Rep Article Loading small molecular weight hydrophilic drugs into polymeric carriers is a challenging task. Metformin hydrochloride (MET) is a highly soluble oral antidiabetic drug of small size and high cationic charge. Hydrophobic ion pairing (HIP) is an approach for reversible modulation of solubility and hydrophilicity of water-soluble drugs via complexation with oppositely charged molecules. Herein, we prepared MET ion pairs and carefully studied and characterized MET interaction with different ligands, with the aim of increasing MET lipophilicity and loading efficiency. HIP was successful using three hydrophilic anionic ligands; sodium dodecyl sulphate (SDS) Carbopol (CB) and tannic acid (TA). Electrostatic interaction and hydrogen bonding drove the complexation per spectroscopic and thermal studies. Complexation efficiency depended on ligand type and charge ratio. While complexes had varying interaction strengths, the excessive stability of TA/MET resulted in unfavorable poor MET dissociation. Notably, HIP imparted a 450 and tenfold lipophilicity increase for SDS/MET and CB/MET, respectively. The latter showed favorable controlled, yet complete release of MET at pH 6.8 and was loaded into alginate beads. Complex bulkiness and decreased lipophilicity resulted in a dramatic 88% increase of MET loading, demonstrating the success of HIP as a simple, efficient and applicable approach for modulating drug’s properties. Nature Publishing Group UK 2022-04-06 /pmc/articles/PMC8986808/ /pubmed/35388027 http://dx.doi.org/10.1038/s41598-022-09384-6 Text en © The Author(s) 2022 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) . |
spellingShingle | Article Abd-El Hafeez, Sara I. Eleraky, Nermin E. Hafez, Ehsan Abouelmagd, Sara A. Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
title | Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
title_full | Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
title_fullStr | Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
title_full_unstemmed | Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
title_short | Design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
title_sort | design and optimization of metformin hydrophobic ion pairs for efficient encapsulation in polymeric drug carriers |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8986808/ https://www.ncbi.nlm.nih.gov/pubmed/35388027 http://dx.doi.org/10.1038/s41598-022-09384-6 |
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