Multifunctional theranostic Pluronic mixed micelles improve targeted photoactivity of Verteporfin in cancer cells

Pellosi, Diogo Silva; Calori, Italo Rodrigo; Paula, Leonardo Barcelos de; Hioka, Noboru; Quaglia, Fabiana; Tedesco, Antônio Cláudio

doi:10.1016/j.msec.2016.09.064

Cited by 52 publications

(29 citation statements)

References 41 publications

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“…The processing technique also controls the structure. Drug-loaded micelles of one or more type of poloxamer have shown promising results in the delivery of anticancer and benzoporphyrin derivatives for photodynamic therapy [ 113 , 150 , 151 ]. Mixed micelles and nanoparticles (the latter sometimes with structures of a diameter >50 nm) typically combine poloxamers of opposing hydrophilic-lipophilic balance (HLB) numbers in order to achieve increased solubilization (in the PPO core) and steric stabilization (PEO corona).…”

Section: Discussionmentioning

confidence: 99%

Formulation of Poloxamers for Drug Delivery

Bodratti

Alexandridis

2018

JFB

425

267

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Poloxamers, also known as Pluronics®, are block copolymers of poly(ethylene oxide) (PEO) and poly(propylene oxide) (PPO), which have an amphiphilic character and useful association and adsorption properties emanating from this. Poloxamers find use in many applications that require solubilization or stabilization of compounds and also have notable physiological properties, including low toxicity. Accordingly, poloxamers serve well as excipients for pharmaceuticals. Current challenges facing nanomedicine revolve around the transport of typically water-insoluble drugs throughout the body, followed by targeted delivery. Judicious design of drug delivery systems leads to improved bioavailability, patient compliance and therapeutic outcomes. The rich phase behavior (micelles, hydrogels, lyotropic liquid crystals, etc.) of poloxamers makes them amenable to multiple types of processing and various product forms. In this review, we first present the general solution behavior of poloxamers, focusing on their self-assembly properties. This is followed by a discussion of how the self-assembly properties of poloxamers can be leveraged to encapsulate drugs using an array of processing techniques including direct solubilization, solvent displacement methods, emulsification and preparation of kinetically-frozen nanoparticles. Finally, we conclude with a summary and perspective.

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Section: Discussionmentioning

confidence: 99%

Formulation of Poloxamers for Drug Delivery

Bodratti

Alexandridis

2018

JFB

425

267

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“…VP was granted FDA approval in 2000 10 , 11 . Since then, the potential of VP for the treatment of cancers, such as prostatic cancer and breast cancer, has been investigated 12 . In recent years, VP has been reported to exhibit broad biological properties independent of light stimulation.…”

Section: Introductionmentioning

confidence: 99%

Verteporfin Inhibits Cell Proliferation and Induces Apoptosis in Human Leukemia NB4 Cells without Light Activation

et al. 2017

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Background and Aims: Verteporfin (VP), clinically used in photodynamic therapy for neovascular macular degeneration, has recently been proven a suppressor of yes-associated protein (YAP) and has shown potential in anticancer treatment. However, its anti-human leukemia effects in NB4 cells remain unclear. In this study, we investigated the effects of VP on proliferation and apoptosis in human leukemia NB4 cells.Methods: NB4 cells were treated with VP for 24 h. The effects of VP on cell proliferation were determined using a Cell-Counting Kit-8 assay (CCK-8) assay and colony forming assay. Apoptosis and cell cycle were evaluated by flow cytometry (FCM). The protein levels were detected by western blot.Results: We found that VP inhibited the proliferation of NB4 cells in a concentration and time-dependent manner. FCM analysis showed that VP induced apoptosis in a concentration dependent manner and that VP treatment led to cell cycle arrest at G0/G1 phase. Moreover, VP significantly decreased the protein expression of YAP, p-YAP, Survivin, c-Myc, cyclinD1, p-ERK, and p-AKT. In addition, VP increased the protein expression of cleaved caspase3, cleaved PARP, Bax, and p-p38 MAPK.Conclusions: VP inhibited the proliferation and induced apoptosis in NB4 cells.

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“…Verteporfin was approved for the treatment of agerelated macular degeneration 23 . The potential of verteporfin for the treatment of cancers, such as prostatic cancer, breast cancer, and pancreatic ductal adenocarcinoma has been investigated 24 . Verteporfin also has been reported to inhibit autophagy at an early stage by suppressing autophagosome formation 25 .…”

Section: Discussionmentioning

confidence: 99%

Protoporphyrin IX and verteporfin prevent SARS-CoV-2 infectionin vitroand in a mouse model expressing human ACE2

Guo

et al. 2020

Preprint

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The infection of SARS-CoV-2 has spread to more than 200 countries and regions and the numbers of infected people and deaths worldwide are expected to continue to rise.Current treatment of COVID-19 is limited and mostly supportive. At present, there is no specific therapeutics against SARS-CoV-2. In this study, we discovered that protoporphyrin IX and verteporfin, two FDA-approved drugs for treatment of human diseases, had significant antiviral effect against SARS-CoV-2, with EC50 values for the reduction of viral RNA at nanomolar concentrations. Both drugs completely inhibited the cytopathic effect (CPE) produced by SARS-CoV-2 infection at lower drug concentrations than that of remdesivir. The selection indices of protoporphyrin IX and verteporfin are 952.74 and 368.93, respectively, suggesting wide safety margins. Both drugs were able to prevent SARS-CoV-2 infection as well as suppress established SARS-CoV-2 infection. The compounds share a porphyrin ring structure. Molecular docking indicates that the compounds may interact with viral receptor ACE2 and could block the cell-cell fusion mediated by ACE2 and viral S protein. Our finding suggests that protoporphyrin IX and verteporfin might be potential antivirals against SARS-CoV-2 infection and also sheds new light on the development of a novel class of small compounds against SARS-CoV-2.

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Multifunctional theranostic Pluronic mixed micelles improve targeted photoactivity of Verteporfin in cancer cells

Cited by 52 publications

References 41 publications

Formulation of Poloxamers for Drug Delivery

Formulation of Poloxamers for Drug Delivery

Verteporfin Inhibits Cell Proliferation and Induces Apoptosis in Human Leukemia NB4 Cells without Light Activation

Protoporphyrin IX and verteporfin prevent SARS-CoV-2 infectionin vitroand in a mouse model expressing human ACE2

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