&lt;p&gt;G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity&lt;/p&gt;

Ceña-Díez, Rafael; Martín-Moreno, Alba; Mata, F. Javier de la; Gomez-Ramirez, Rafael; Muñóz, Eduardo; Ardoy, Manuel; Muñoz‐Fernández, María Ángeles

doi:10.2147/ijn.s188495

Cited by 15 publications

(15 citation statements)

References 31 publications

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“…Previously published reports of PCDs against HIV-1 [ 25 ], HSV-2 [ 11 , 12 ] or even HCV [ 10 ] propose PCDs as alternative agents against several viral infections [ 26 ]. The studies of the potential activity of G1-S4, G2-S16 and G2-S24P PCDs against HCMV AD−169 infection was performed by plaque reduction assays in MRC-5 cells (Fig.…”

Section: Resultsmentioning

confidence: 99%

Nanotechnology against human cytomegalovirus in vitro: polyanionic carbosilane dendrimers as antiviral agents

et al. 2021

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Background Human cytomegalovirus (HCMV) is a worldwide infection, causing different troublesome in immunosupressed patients and very related to Human Immunodeficiency Virus 1 (HIV-1) infection, mainly in developing countries, with a co-infection rate of 80% in Africa. The high cost of present treatments and the lack of routinely tests in these countries urge the necessity to develop new molecules or strategies against HCMV. The new treatments should be low-cost and capable of avoiding the emerging problem of resistant virus. Nanoparticles play an important role in several viral infections. Our main focus is to study the potential activity of polyanionic carbosilane dendrimers (PDC), which are hyperbranched molecules with several sulfonate or sulfate groups in their periphery, against different viruses. Results We studied the activity of G1-S4, G2-S16 and G2-S24P PDCs in MRC-5 cell line against HCMV infection by several plaque reduction assays. Our results show that dendrimers present good biocompatibility at the concentrations tested (1–50 µM) for 6 days in cell culture. Interestingly, both G2-S16 and G2-S24P showed a remarked inhibition at 10 µM against HCMV infection. Results on attachment and virucidal assays indicated that the inhibition was not directed to the virus or the virus-cell attachment. However, results of time of addition, showed a longer lasting activity of these dendrimers in comparison to ganciclovir, and the combination of G2-S16 or G2-S24P with ganciclovir increases the HCMV inhibition around 90 %. Conclusions Nanotechnology, in particular polyanionic carbosilane dendrimers, have proved their potential application against HCMV, being capable of inhibiting the infection by themselves or enhancing the activity of ganciclovir, the actual treatment. These compounds represent a low-cost approach to fight HCMV infections.

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Section: Resultsmentioning

confidence: 99%

Nanotechnology against human cytomegalovirus in vitro: polyanionic carbosilane dendrimers as antiviral agents

et al. 2021

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“…The development of prophylactic strategies with dual microbicide and contraceptive activity is also interesting. Platycodin D (PD), a promising contraceptive, was combined with G1-S2 or G2-S16 dendrimers to develop a prophylactic strategy with dual activity [ 64 ]. The results show that PD does not affect the antiviral activity of the dendrimers and they do not affect the spermicide activity of PD.…”

Section: Nanotechnology Approaches For Prevention Of Hiv Infectionmentioning

confidence: 99%

Nanosystems Applied to HIV Infection: Prevention and Treatments

Macchione

Bedoya

Figueroa

et al. 2020

IJMS

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Sexually-transmitted infections (STIs) are a global health concern worldwide as they cause acute diseases, infertility, and significant mortality. Among the bacterial, viral, and parasitic pathogens that can be sexually transmitted, human immunodeficiency virus (HIV) has caused one of the most important pandemic diseases, which is acquired immune deficiency syndrome (AIDS). 32.7 million people have died from AIDS-related illnesses since the start of the epidemic. Moreover, in 2019, 38 million people were living with HIV worldwide. The need to deal with this viral infection becomes more obvious, because it represents not only a problem for public health, but also a substantial economic problem. In this context, it is necessary to focus efforts on developing methods for prevention, detection and treatment of HIV infections that significantly reduce the number of newly infected people and provide a better quality of life for patients. For several decades, biomedical research has been developed allowing quick solutions through the contribution of effective tools. One of them is the use of polymers as vehicles, drug carrier agents, or as macromolecular prodrugs. Moreover, nanosystems (NSs) play an especially important role in the diagnosis, prevention, and therapy against HIV infection. The purpose of this work is to review recent research into diverse NSs as potential candidates for prevention and treatment of HIV infection. Firstly, this review highlights the advantages of using nanosized structures for these medical applications. Furthermore, we provide an overview of different types of NSs used for preventing or combating HIV infection. Then, we briefly evaluate the most recent developments associated with prevention and treatment alternatives. Additionally, the implications of using different NSs are also addressed.

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“…In this context, G2-S16 PCD in combination with Platicodin D, a spermicide compound, could prevent HIV infection and non-desired pregnancies at the same time. Our results showed that a combination of G2-S16 PCD/Platicodin D inhibit 95% HIV infection and retain 100% of sperm mobility, not showing toxicity, neither in vitro nor in vivo [ 77 ].…”

Section: How Does G2-s16 Pcd Work In Vitro?mentioning

confidence: 99%

“…In vivo G2-S16 PCD, in combination with Platycodin D, appears as a vaginal microbicide candidate with contraceptive activity. [77] 2019…”

mentioning

confidence: 99%

Emergence of Nanotechnology to Fight HIV Sexual Transmission: The Trip of G2-S16 Polyanionic Carbosilane Dendrimer to Possible Pre-Clinical Trials

Relaño-Rodríguez

Muñoz‐Fernández

2020

IJMS

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Development of new, safe, and effective microbicides to prevent human immunodeficiency virus HIV sexual transmission is needed. Unfortunately, most microbicides proved ineffective to prevent the risk of HIV-infection in clinical trials. We are working with G2-S16 polyanionic carbosilane dendrimer (PCD) as a new possible vaginal topical microbicide, based on its short reaction times, wide availability, high reproducibility, and quantitative yields of reaction. G2-S16 PCD exerts anti-HIV activity at an early stage of viral replication, by blocking gp120/CD4/CCR5 interaction, and providing a barrier against infection for long periods of time. G2-S16 PCD was stable at different pH values, as well as in the presence of seminal fluids. It maintained the anti-HIV activity against R5/X4 HIV over time, did not generate any type of drug resistance, and retained the anti-HIV effect when exposed to semen-enhanced viral infection. Importantly, G2-S16 PCD did not modify vaginal microbiota neither in vitro or in vivo. Histopathological examination did not show vaginal irritation, inflammation, lesions, or damage in the vaginal mucosa, after administration of G2-S16 PCD at different concentrations and times in female mice and rabbit animal models. Based on these promising data, G2-S16 PCD could become a good, safe, and readily available candidate to use as a topical vaginal microbicide against HIV.

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<p>G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity</p>

Cited by 15 publications

References 31 publications

Nanotechnology against human cytomegalovirus in vitro: polyanionic carbosilane dendrimers as antiviral agents

Nanotechnology against human cytomegalovirus in vitro: polyanionic carbosilane dendrimers as antiviral agents

Nanosystems Applied to HIV Infection: Prevention and Treatments

Emergence of Nanotechnology to Fight HIV Sexual Transmission: The Trip of G2-S16 Polyanionic Carbosilane Dendrimer to Possible Pre-Clinical Trials

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