Conjugation, Prodrug, and Co-Administration Strategies in Support of Nanotechnologies to Improve the Therapeutic Efficacy of Phytochemicals in the Central Nervous System

Rassu, Giovanna; Sorrenti, Milena; Catenacci, Laura; Pavan, Barbara; Ferraro, Luca; Gavini, Elisabetta; Bonferoni, Maria Cristina; Giunchedi, Paolo; Dalpiaz, Alessandro

doi:10.3390/pharmaceutics15061578

Cited by 7 publications

(1 citation statement)

References 217 publications

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“…Therefore, numerous attempts are currently being made to improve the bioavailability of polyphenols. The development of formulations and delivery systems, such as prodrugs or conjugates using nanotechnologies to target the appropriate molecules, has been attempted [182]. For instance, resveratrol-loaded PLGA nanoparticles were observed to enhance resveratrol penetration into the BBB and induce neuroprotection within the brain in experimental models of PD [183].…”

Section: Attempt To Increase the Bioavailability Of Polyphenolsmentioning

confidence: 99%

Polyphenols in Inner Ear Neurobiology, Health and Disease: From Bench to Clinics

Osakabe,

Modafferi,

Ontario

et al. 2023

Medicina

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There is substantial experimental and clinical interest in providing effective ways to both prevent and slow the onset of hearing loss. Auditory hair cells, which occur along the basilar membrane of the cochlea, often lose functionality due to age-related biological alterations, as well as from exposure to high decibel sounds affecting a diminished/damaged auditory sensitivity. Hearing loss is also seen to take place due to neuronal degeneration before or following hair cell destruction/loss. A strategy is necessary to protect hair cells and XIII cranial/auditory nerve cells prior to injury and throughout aging. Within this context, it was proposed that cochlea neural stem cells may be protected from such aging and environmental/noise insults via the ingestion of protective dietary supplements. Of particular importance is that these studies typically display a hormetic-like biphasic dose–response pattern that prevents the occurrence of auditory cell damage induced by various model chemical toxins, such as cisplatin. Likewise, the hormetic dose–response also enhances the occurrence of cochlear neural cell viability, proliferation, and differentiation. These findings are particularly important since they confirmed a strong dose dependency of the significant beneficial effects (which is biphasic), whilst having a low-dose beneficial response, whereas extensive exposures may become ineffective and/or potentially harmful. According to hormesis, phytochemicals including polyphenols exhibit biphasic dose–response effects activating low-dose antioxidant signaling pathways, resulting in the upregulation of vitagenes, a group of genes involved in preserving cellular homeostasis during stressful conditions. Modulation of the vitagene network through polyphenols increases cellular resilience mechanisms, thus impacting neurological disorder pathophysiology. Here, we aimed to explore polyphenols targeting the NF-E2-related factor 2 (Nrf2) pathway to neuroprotective and therapeutic strategies that can potentially reduce oxidative stress and inflammation, thus preventing auditory hair cell and XIII cranial/auditory nerve cell degeneration. Furthermore, we explored techniques to enhance their bioavailability and efficacy.

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Section: Attempt To Increase the Bioavailability Of Polyphenolsmentioning

confidence: 99%

Polyphenols in Inner Ear Neurobiology, Health and Disease: From Bench to Clinics

Osakabe,

Modafferi,

Ontario

et al. 2023

Medicina

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Exploring Piperine: Unleashing the multifaceted potential of a phytochemical in cancer therapy

Tripathi,

Gupta,

Pandey

2024

Mol Biol Rep

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Polyethylene Glycol–Based Polymer-Drug Conjugates: Novel Design and Synthesis Strategies for Enhanced Therapeutic Efficacy and Targeted Drug Delivery

Verma,

Pandey,

Jha

et al. 2024

Appl Biochem Biotechnol

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Due to their potential to enhance therapeutic results and enable targeted drug administration, polymer-drug conjugates that use polyethylene glycol (PEG) as both the polymer and the linker for drug conjugation have attracted much research. This study seeks to investigate recent developments in the design and synthesis of PEG-based polymer-drug conjugates, emphasising fresh ideas that fill in existing knowledge gaps and satisfy the increasing need for more potent drug delivery methods. Through an extensive review of the existing literature, this study identifies key challenges and proposes innovative strategies for future investigations. The paper presents a comprehensive framework for designing and synthesising PEG-based polymer-drug conjugates, including rational molecular design, linker selection, conjugation methods, and characterisation techniques. To further emphasise the importance and adaptability of PEG-based polymer-drug conjugates, prospective applications are highlighted, including cancer treatment, infectious disorders, and chronic ailments.

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Conjugation, Prodrug, and Co-Administration Strategies in Support of Nanotechnologies to Improve the Therapeutic Efficacy of Phytochemicals in the Central Nervous System

Cited by 7 publications

References 217 publications

Polyphenols in Inner Ear Neurobiology, Health and Disease: From Bench to Clinics

Polyphenols in Inner Ear Neurobiology, Health and Disease: From Bench to Clinics

Exploring Piperine: Unleashing the multifaceted potential of a phytochemical in cancer therapy

Polyethylene Glycol–Based Polymer-Drug Conjugates: Novel Design and Synthesis Strategies for Enhanced Therapeutic Efficacy and Targeted Drug Delivery

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