{"doi":"10.3390/ijms21249403","title":"Emergence of Nanotechnology to Fight HIV Sexual Transmission: The Trip of G2-S16 Polyanionic Carbosilane Dendrimer to Possible Pre-Clinical Trials","abstract":"<jats:p>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.</jats:p>","journal":"International Journal of Molecular Sciences","year":2020,"id":655693,"datarank":0.41588830833596724,"base_score":2.772588722239781,"endowment":2.772588722239781,"self_citation_contribution":0.41588830833596724,"citation_network_contribution":0.0,"self_endowment_contribution":0.41588830833596724,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":15,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":441508,"name":"María Ángeles Muñoz‐Fernández","orcid":"0000-0002-0813-4500","position":1,"is_corresponding":false},{"id":1481866,"name":"Ignacio Relaño-Rodríguez","orcid":"0000-0001-6259-6258","position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Emergence of Nanotechnology to Fight HIV Sexual Transmission: The Trip of G2-S16 Polyanionic Carbosilane Dendrimer to Possible Pre-Clinical Trials","abstract":"<jats:p>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.</jats:p>","is_dataset_classified":null,"base_score":2.772588722239781,"endowment":2.772588722239781,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"33321835","pmcid":"PMC7764023","openalex_id":"https://openalex.org/W3112455680","authors":[],"funders":[{"funder_name":"Instituto de Salud Carlos III","grant_id":"RD16/0025/0019; PT17/0015/0042; PI19/01638; RD06/0006/0035; RD12/0017/0037; CIBER-BBN; RD09/0076/00103; PT13/0010/0028","title":null},{"funder_name":"PENTA FOUNDATION","grant_id":"EPIICAL Project","title":null},{"funder_name":"Instituto de Investigación Sanitaria Gregorio Marañón","grant_id":"COV20/MAM-BIS","title":null},{"funder_name":"Uniwersytet Łódzki","grant_id":"NAWA International Academic Partnership Programme","title":null},{"funder_name":"European Cooperation in Science and Technology","grant_id":"COST Action CA 17140 \"Cancer Nanomedicine from the Bench to the Bedside\"","title":null},{"funder_name":"European Cooperation in Science and Technology","grant_id":"COST Action CA 17140 &quot;Cancer Nanomedicine from the Bench to the Bedside&quot;","title":null}],"total_grants":6,"fwci":1.6954,"citation_percentile":0.83860196,"influential_citations":0,"citation_trend":[{"year":2021,"count":1},{"year":2022,"count":11},{"year":2023,"count":1},{"year":2024,"count":2}],"oa_status":"gold","license":"cc-by","oa_locations":[{"url":"https://www.mdpi.com/1422-0067/21/24/9403/pdf?version=1607611404","host_type":"journal"},{"url":"https://www.mdpi.com/1422-0067/21/24/9403/pdf?version=1607611404","host_type":"publisher"},{"url":"https://www.mdpi.com/1422-0067/21/24/9403/pdf","host_type":"publisher"},{"url":"https://doi.org/10.3390/ijms21249403","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/33321835","host_type":"repository"},{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/7764023","host_type":"repository"},{"url":"https://doaj.org/article/e38301f27bd94d52a1ac09b9f2dc768d","host_type":"repository"},{"url":"https://dx.doi.org/10.3390/ijms21249403","host_type":"repository"},{"url":"https://europepmc.org/articles/PMC7764023","host_type":"Europe_PMC"},{"url":"https://europepmc.org/articles/PMC7764023?pdf=render","host_type":"Europe_PMC"}],"fields_of_study":["Reproductive tract infections research","HIV/AIDS Research and Interventions","HIV Research and Treatment","Administration, Intravaginal","Alkanesulfonates","Animals","Anti-HIV Agents","Dendrimers","Drug Evaluation, Preclinical","Female","HIV Infections","Humans","Male","Organosilicon Compounds"],"mesh_terms":["Administration, Intravaginal","Alkanesulfonates","Animals","Drug Evaluation, Preclinical","Female","Humans","Male","HIV Infections","Organosilicon Compounds","Anti-HIV Agents","Dendrimers"],"keywords":["Microbicide","Microbicides for sexually transmitted diseases","Sexual transmission","Vaginal microbicide","Human immunodeficiency virus (HIV)","Transmission (telecommunications)","Medicine","Pharmacology","Virology","Immunology","Biology","Population","Nanotechnology","Sexually Transmitted Infection","Hiv Prophylaxis","G2-s16 Pcd"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[{"name":"nct"},{"name":"doi"}],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-11T18:36:51.445946Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}