Comparative analysis of risedronate and its regioisomers synthesized via microwave-assisted method: bone affinity, cytotoxicity, permeability, and therapeutic potential.

Monika Zielińska, Amanda Pacholak, Bartosz Orwat, Mariusz Sandomierski, Ireneusz Kownacki, Ewa Kaczorek, Adam Voelkel

Abstract readComparative Study

In one paragraph

Article in Pharmacological reports : PR, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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7 authors.

Monika ZielińskaInstitute of Chemical Technology and Engineering, Poznan University of Technology, Berdychowo 4, 60-965, Poznań, Poland. monika.zielinska@put.poznan.pl.ORCID http://orcid.org/0000-0002-8850-6270

Amanda PacholakInstitute of Chemical Technology and Engineering, Poznan University of Technology, Berdychowo 4, 60-965, Poznań, Poland.

Bartosz OrwatDepartment of Molecular Physics, Lodz University of Technology, Lodz, Poland.

Mariusz SandomierskiInstitute of Chemical Technology and Engineering, Poznan University of Technology, Berdychowo 4, 60-965, Poznań, Poland.

Ireneusz KownackiCenter for Advanced Technologies, Adam Mickiewicz University, Poznan, Poland.

Ewa KaczorekInstitute of Chemical Technology and Engineering, Poznan University of Technology, Berdychowo 4, 60-965, Poznań, Poland.

Adam VoelkelInstitute of Chemical Technology and Engineering, Poznan University of Technology, Berdychowo 4, 60-965, Poznań, Poland.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundBisphosphonates (BPs) are widely used for treating bone diseases such as osteoporosis due to their strong affinity for hydroxyapatite (HA) in bones. Minor structural variations among BPs can significantly affect their therapeutic potential. This study aimed to synthesize risedronate (RSD) and its two regioisomers (2-RSD, 4-RSD) and investigate the impact of these variations on bone affinity, permeability, and cytotoxicity.

methodsRSD and its regioisomers were synthesized using a microwave-assisted method. Bone affinity was assessed through sorption studies on HA and two polymer-ceramic materials mimicking bone properties. Compound permeability was predicted using the Parallel Artificial Membrane Permeability Assay (PAMPA). Cytotoxicity was evaluated by analyzing the response of bacterial cells to BPs using metabolic activity assays.

results2-RSD demonstrated a higher bone affinity and similar permeability than commercially available RSD. 2-RSD also showed reduced cytotoxicity in bacterial cell assays, indicating enhanced biocompatibility. These findings suggest that minor structural changes can lead to significant differences in therapeutic efficacy.

conclusionsThe study highlights the potential of the 2-RSD as a more effective treatment for bone diseases. Structural variations in BPs can greatly influence their biological properties, paving the way for the development of improved therapeutic agents.

Indexed as

Bone and BonesBone Density Conservation AgentsRisedronic AcidDurapatiteHumansMicrowavesPermeabilityStereoisomerismBone Density Conservation AgentsDurapatiteRisedronic AcidBisphosphonatesCytotoxicityHydroxyapatiteMicrowave synthesisPampaPolymer composites

Identifiers

PMID39928090

DOI10.3390/colloids2030035

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