RT Journal Article
T1 G1-S4 or G2-S16 carbosilane dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity.
A1 Ceña-Diez, Rafael
A1 Martin-Moreno, Alba
A1 de la Mata, F Javier
A1 Gomez-Ramirez, Rafael
A1 Muñoz, Eduardo
A1 Ardoy, Manuel
A1 Muñoz-Fernandez, Mª Angeles
K1 G1-S4 dendrimer
K1 G2-S16 dendrimer
K1 HIV-1
K1 HSV-2
K1 Platycodin D
K1 topical microbicide
AB HIV-1 and herpes simplex virus type-2 (HSV-2) represent two of the most relevant sexually transmitted diseases (STDs) worldwide. Moreover, each year there are >200 million pregnancies worldwide, and more than half are unintended. Continued high rates of unintended pregnancies and spread of HIV-1 and HSV-2 require new approaches to address these problems. G1-S4 and G2-S16 dendrimers emerge as potential candidates for the development of a topical microbicide due to their safety and effectivity against HIV-1 and HSV-2 infection, both in vitro and in vivo. Our goal is to develop a dual topical microbicide to prevent the transmission of STDs and unintended pregnancies. Platycodin D (PD) was selected for its great spermicidal activity, topical application, and biocompatibility. Toxicology and inhibitory profile of G1-S4/PD and G2-S16/PD were evaluated in vitro and in vivo. Spermicidal activity was assessed by a computer-assisted sperm analysis system (CASA). G1-S4/PD and G2-S16/PD presented >95% of HIV-1 inhibition in TZM-bl cells and peripheral blood mononuclear cells. CASA assessment determined that 0.25 mM of PD with therapeutic concentrations of G1-S4 or G2-S16 was able to induce 100% immobilization of the sperm in 30 seconds. To evaluate the toxicity in vivo, a vaginal toxicity assay was performed in BALB/c mice. No significant changes or damage to the vaginal epithelium after 7 consecutive days of application were observed. Our data indicate that G1-S4/PD and G2-S16/PD combinations are promising candidates to be developed for vaginal microbicides with contraceptive activity.
PB Dove Medical Press
YR 2019
FD 2019-04-02
LK http://hdl.handle.net/10668/13896
UL http://hdl.handle.net/10668/13896
LA en
NO Ceña-Diez R, Martin-Moreno A, de la Mata FJ, Gómez-Ramirez R, Muñoz E, Ardoy M, et al. G1-S4 or G2-S16 carbosilane dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity. Int J Nanomedicine. 2019 Apr 2;14:2371-2381
NO This work was partially funded by the RD16/0025/0019 projects as part of Acción Estratégica en Salud, Plan Nacional de Investigación Científica, and Desarrollo e Innovación Tecnológica (2013–2016), and cofinanced  by Instituto de Salud Carlos III (Subdirección General de Evaluación) and Fondo Europeo de Desarrollo Regional (FEDER), RETIC PT17/0015/0042, Fondo de Investigacion Sanitaria (FIS) (grant number PI16/01863), and the EPIICAL Project. CIBER-BBN is an initiative funded by the VI National R&D&i Plan 2008–2011, Iniciativa Ingenio 2010, the Consolider Program, and CIBER Actions, and financed by the Instituto de Salud Carlos III with assistance from the European Regional Development Fund. In addition, The European Cooperation in Science and Technology (COST), CA17140 – Cancer Nanomedicine – From the Benchto the Bedside, partially funded this work.
DS RISalud
RD Sep 6, 2025