Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate

Bisphosphonate drugs constitute the primary treatment for bone diseases such as Paget’s disease and osteoporosis. Despite their effectiveness, they also exhibit severe drawbacks, such as rapid excretion and limited oral bioavailability. High doses are usually administered to counterbalance these dra...

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Main Authors: Fanouria-Eirini G. Alatzoglou, Maria Vassaki, Kalliopi Nirgianaki, Eleftherios Tripodianos, Petri Turhanen, Konstantinos D. Demadis, Konstantinos E. Papathanasiou
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Materials
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Online Access:https://www.mdpi.com/1996-1944/16/9/3379
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author Fanouria-Eirini G. Alatzoglou
Maria Vassaki
Kalliopi Nirgianaki
Eleftherios Tripodianos
Petri Turhanen
Konstantinos D. Demadis
Konstantinos E. Papathanasiou
author_facet Fanouria-Eirini G. Alatzoglou
Maria Vassaki
Kalliopi Nirgianaki
Eleftherios Tripodianos
Petri Turhanen
Konstantinos D. Demadis
Konstantinos E. Papathanasiou
author_sort Fanouria-Eirini G. Alatzoglou
collection DOAJ
description Bisphosphonate drugs constitute the primary treatment for bone diseases such as Paget’s disease and osteoporosis. Despite their effectiveness, they also exhibit severe drawbacks, such as rapid excretion and limited oral bioavailability. High doses are usually administered to counterbalance these drawbacks. Subsequently, side effects are triggered, such as osteonecrosis of the lower jaw and esophageal cancer. Controlled drug release systems may be viable candidates to overcome those issues. Herein, we present novel functionalized silica-based hydrogels loaded with the osteoporosis drug etidronate (1,1-hydroxyethylidene-diphosphonate) used to control the release profile of the drug. Various methodologies were evaluated to control the initial release rate and the final released concentration of the drug. These included the gel density, by systematically increasing the initial concentration of silicate used to prepare the hydrogels, the presence of metal cations (Ca<sup>2+</sup> and Cu<sup>2+</sup>), and the internal surface functionalization of the gel with silane-based grafting agents (with anionic, cationic, and neutral groups). This study also contributes to our continuous effort to develop new a priori programmable drug-loaded gels for the controlled release of osteoporosis drugs.
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spelling doaj.art-c65de9e8480c4cecadce02b993474bb02023-11-17T23:15:16ZengMDPI AGMaterials1996-19442023-04-01169337910.3390/ma16093379Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of EtidronateFanouria-Eirini G. Alatzoglou0Maria Vassaki1Kalliopi Nirgianaki2Eleftherios Tripodianos3Petri Turhanen4Konstantinos D. Demadis5Konstantinos E. Papathanasiou6Crystal Engineering, Growth and Design Laboratory, Department of Chemistry, University of Crete, 71003 Heraklion, Crete, GreeceCrystal Engineering, Growth and Design Laboratory, Department of Chemistry, University of Crete, 71003 Heraklion, Crete, GreeceCrystal Engineering, Growth and Design Laboratory, Department of Chemistry, University of Crete, 71003 Heraklion, Crete, GreeceCrystal Engineering, Growth and Design Laboratory, Department of Chemistry, University of Crete, 71003 Heraklion, Crete, GreeceBiocenter Kuopio, School of Pharmacy, University of Eastern Finland, P.O. Box 1627, 70211 Kuopio, FinlandCrystal Engineering, Growth and Design Laboratory, Department of Chemistry, University of Crete, 71003 Heraklion, Crete, GreeceDepartment of Chemistry, School of Sciences and Engineering, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UKBisphosphonate drugs constitute the primary treatment for bone diseases such as Paget’s disease and osteoporosis. Despite their effectiveness, they also exhibit severe drawbacks, such as rapid excretion and limited oral bioavailability. High doses are usually administered to counterbalance these drawbacks. Subsequently, side effects are triggered, such as osteonecrosis of the lower jaw and esophageal cancer. Controlled drug release systems may be viable candidates to overcome those issues. Herein, we present novel functionalized silica-based hydrogels loaded with the osteoporosis drug etidronate (1,1-hydroxyethylidene-diphosphonate) used to control the release profile of the drug. Various methodologies were evaluated to control the initial release rate and the final released concentration of the drug. These included the gel density, by systematically increasing the initial concentration of silicate used to prepare the hydrogels, the presence of metal cations (Ca<sup>2+</sup> and Cu<sup>2+</sup>), and the internal surface functionalization of the gel with silane-based grafting agents (with anionic, cationic, and neutral groups). This study also contributes to our continuous effort to develop new a priori programmable drug-loaded gels for the controlled release of osteoporosis drugs.https://www.mdpi.com/1996-1944/16/9/3379silica gelshydrogelsdrug releasebisphosphonatesosteoporosiscontrolled release
spellingShingle Fanouria-Eirini G. Alatzoglou
Maria Vassaki
Kalliopi Nirgianaki
Eleftherios Tripodianos
Petri Turhanen
Konstantinos D. Demadis
Konstantinos E. Papathanasiou
Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate
Materials
silica gels
hydrogels
drug release
bisphosphonates
osteoporosis
controlled release
title Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate
title_full Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate
title_fullStr Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate
title_full_unstemmed Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate
title_short Surface-Modified Silica Hydrogels for the Programmable Release of Bisphosphonate Anti-Osteoporosis Drugs: The Case of Etidronate
title_sort surface modified silica hydrogels for the programmable release of bisphosphonate anti osteoporosis drugs the case of etidronate
topic silica gels
hydrogels
drug release
bisphosphonates
osteoporosis
controlled release
url https://www.mdpi.com/1996-1944/16/9/3379
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