Polyanionic carbosilane dendrimer-conjugated antiviral drugs as efficient microbicides: Recent trends and developments in HIV treatment/therapy

Sepúlveda‐Crespo, Daniel; Gómez, Rafael; Mata, F. Javier de la; Jiménez, José Luís; Muñoz‐Fernández, María Ángeles

doi:10.1016/j.nano.2015.03.008

Cited by 63 publications

(43 citation statements)

References 120 publications

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“…G2-S16 does neither alter semen motility nor affect other functions of the semen. 16,19,28 No irritation or vaginal lesions were detected in rabbits after 2 weeks of intravaginal G2-S16 application 19 or in CD1(ICR) mice after G2-S16 vaginal administration. 19 The application of one dose of 1.5%, 3%, and 4.5% of G2-S16 to hydroxyethylcellulose (HEC) gel-treated BALB/c at various consecutive time periods does not cause disruption of the epithelial cells or produce damage in the vaginal mucosa.…”

Section: Discussionmentioning

confidence: 95%

Efficacy of HIV antiviral polyanionic carbosilane dendrimer G2-S16 in the presence of semen

Ceña-Díez¹,

García-Broncano²,

Fj³

et al. 2016

IJN

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The development of a safe and effective microbicide to prevent the sexual transmission of human immunodeficiency virus (HIV)-1 is urgently needed. Unfortunately, the majority of microbicides, such as poly(L-lysine)-dendrimers, anionic polymers, or antiretrovirals, have proved inactive or even increased the risk of HIV infection in clinical trials, most probably due to the fact that these compounds failed to prevent semen-exposed HIV infection. We showed that G2-S16 dendrimer exerts anti-HIV-1 activity at an early stage of viral replication, blocking the gp120/CD4/CCR5 interaction and providing a barrier to infection for long periods, confirming its multifactorial and nonspecific ability. Previously, we demonstrated that topical administration of G2-S16 prevents HIV transmission in humanized BLT mice without irritation or vaginal lesions. Here, we demonstrated that G2-S16 is active against mock- and semen-exposed HIV-1 and could be a promising microbicide against HIV infection.

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Section: Discussionmentioning

confidence: 95%

Efficacy of HIV antiviral polyanionic carbosilane dendrimer G2-S16 in the presence of semen

Ceña-Díez¹,

García-Broncano²,

Fj³

et al. 2016

IJN

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“…The preponderance of utilizing silicon chemistry to synthesize dendrimers rests with the fact that nucleophilic molecules can readily access electrophilic silicon (Si + ) [48]. Notably, the superiority of carbosilane dendrimers is associated with the low polarity as well as the high energy of the C-Si bond, endowing it with high hydrophobicity [49]. Although carbosilane dendrimers possess such a hydrophobic internal skeleton, they can still be converted into hydrophilic compounds via surface functionalization with polar moieties.…”

Section: Carbosilane Dendrimersmentioning

confidence: 99%

Dendrimer-Based Drug Delivery Systems for Brain Targeting

2019

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Human neuroscience has made remarkable progress in understanding basic aspects of functional organization; it is a renowned fact that the blood–brain barrier (BBB) impedes the permeation and access of most drugs to central nervous system (CNS) and that many neurological diseases remain undertreated. Therefore, a number of nanocarriers have been designed over the past few decades to deliver drugs to the brain. Among these nanomaterials, dendrimers have procured an enormous attention from scholars because of their nanoscale uniform size, ease of multi-functionalization, and available internal cavities. As hyper-branched 3D macromolecules, dendrimers can be maneuvered to transport diverse therapeutic agents, incorporating small molecules, peptides, and genes; diminishing their cytotoxicity; and improving their efficacy. Herein, the present review will give exhaustive details of extensive researches in the field of dendrimer-based vehicles to deliver drugs through the BBB in a secure and effectual manner. It is also a souvenir in commemorating Donald A. Tomalia on his 80th birthday.

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“…In particular, carbosilane dendrimers have been proposed by the group of Muñoz-Fernández and tested in vivo. Results obtained using mouse models showed that different carbosilane dendrimers were safe [54,55] and one in particular (G2-S16, a ∼8 nm, second generation, silica core and 16 sulfonate end-groups dendrimer) was able to significantly reduce HIV transmission upon vaginal challenge (84% of animals protected) [56].…”

Section: Nanomedicine and Prevention Of Hiv Sexual Transmissionmentioning

confidence: 99%

The Potential of HIV-1 Nanotherapeutics: from in vitro Studies to Clinical Trials

Roy

Rodríguez

Barber

et al. 2015

Nanomedicine (Lond.)

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Since its discovery almost three decades ago, HIV-1 has grown into the most aggressive pandemic of modern time. Following the implementation of combination antiretroviral therapy, the pathological outcome of HIV infection has substantially improved. However, combination antiretroviral therapy is limited by several factors including, long-term toxicity, serious side effects and complex dosing regimens, and so on. In this regard, researchers have directed their attention toward enhancing current treatment strategies and/or developing alternative HIV-1 therapeutics. In recent years, this attention has fixated on nanomedicine-based anti-HIV therapeutics (HIV-1 nanotherapeutics). In the present study, we have reviewed several HIV-1 nanotherapeutics that have shown success at the preclinical level and/or Phase I/II clinical trials. We also discuss the possible benefits of these nanomedicine-based approaches and their future outlook.

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Polyanionic carbosilane dendrimer-conjugated antiviral drugs as efficient microbicides: Recent trends and developments in HIV treatment/therapy

Cited by 63 publications

References 120 publications

Efficacy of HIV antiviral polyanionic carbosilane dendrimer G2-S16 in the presence of semen

Efficacy of HIV antiviral polyanionic carbosilane dendrimer G2-S16 in the presence of semen

Dendrimer-Based Drug Delivery Systems for Brain Targeting

The Potential of HIV-1 Nanotherapeutics: from in vitro Studies to Clinical Trials

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