ArticleAntiviral research2012
Development and evaluation of a thermosensitive vaginal gel containing raltegravir+efavirenz loaded nanoparticles for HIV prophylaxis.
Article in Antiviral research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed.
- Antiviral role of nanomaterials: a material scientist's perspective.RSC advances · 2022Review
- Niclosamide-loaded nanoparticles disrupt Candida biofilms and protect mice from mucosal candidiasis.PLoS biology · 2022Article
- Craft of Co-encapsulation in Nanomedicine: A Struggle To Achieve Synergy through Reciprocity.ACS pharmacology & translational science · 2022Review
- Application of Sol-Gels for Treatment of Gynaecological Conditions-Physiological Perspectives and Emerging Concepts in Intravaginal Drug Delivery.Gels (Basel, Switzerland) · 2022Review
- Virus-Mimicking Polymer Nanoparticles Targeting CD169ACS applied materials & interfaces · 2022Article
- Recent Advances in the Excipients Used in Modified Release Vaginal Formulations.Materials (Basel, Switzerland) · 2022Review
- Antifungal activity of alexidine dihydrochloride in a novel diabetic mouse model of dermatophytosis.Frontiers in cellular and infection microbiology · 2022Article
- Enzyme Responsive Vaginal Microbicide Gels Containing Maraviroc and Tenofovir Microspheres Designed for Acid Phosphatase-Triggered Release for Pre-Exposure Prophylaxis of HIV-1: A Comparative Analysis of a Bigel and Thermosensitive Gel.Gels (Basel, Switzerland) · 2021Article
- A new engineering process of biodegradable polymeric solid implants for ultra-long-acting drug delivery.International journal of pharmaceutics: X · 2021Article
- Novel Antiretroviral Therapeutic Strategies for HIV.Molecules (Basel, Switzerland) · 2021Review
- Biodegradable polymeric solid implants for ultra-long-acting delivery of single or multiple antiretroviral drugs.International journal of pharmaceutics · 2021Article
- Recent Advances in Polymer-Based Vaginal Drug Delivery Systems.Pharmaceutics · 2021Review
- Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora.HIV/AIDS (Auckland, N.Z.) · 2021Article
- In vitro Study on Synergistic Interactions Between Free and Encapsulated Q-Griffithsin and Antiretrovirals Against HIV-1 Infection.International journal of nanomedicine · 2021Article
- Emergence of Nanotechnology to Fight HIV Sexual Transmission: The Trip of G2-S16 Polyanionic Carbosilane Dendrimer to Possible Pre-Clinical Trials.International journal of molecular sciences · 2020Review
- Next generation miRNA inhibition using short anti-seed PNAs encapsulated in PLGA nanoparticles.Journal of controlled release : official journal of the Controlled Release Society · 2020Article
- Anti-αScience advances · 2020Article
- Advancements in prophylactic and therapeutic nanovaccines.Acta biomaterialia · 2020Review
- Sustained Intracellular Raltegravir Depots Generated with Prodrugs Designed for Nanoparticle Delivery.ACS biomaterials science & engineering · 2019Article
- Tetrahydrocurcumin-loaded vaginal nanomicrobicide for prophylaxis of HIV/AIDS: in silico study, formulation development, and in vitro evaluation.Drug delivery and translational research · 2019Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The objective of this investigation was to develop a thermosensitive vaginal gel containing raltegravir+efavirenz loaded PLGA nanoparticles (RAL+EFV-NPs) for pre-exposure prophylaxis of HIV. RAL+EFV-NPs were fabricated using a modified emulsion-solvent evaporation method and characterized for size and zeta potential. The average size and surface charge of RAL+EFV-NP were 81.8±6.4 nm and -23.18±7.18 mV respectively. The average encapsulation efficiency of raltegravir and efavirenz was 55.5% and 98.2% respectively. Thermosensitive vaginal gel containing RAL+EFV-NPs was successfully prepared using a combination of Pluronic F127 (20% w/v) and Pluronic F68 (1% w/v). Incorporation RAL+EFV-NPs in the gel did not result in nanoparticle aggregation and RAL+EFV-NPs containing gel showed thermogelation at 32.5°C. The RAL+EFV-NPs were evaluated for inhibition of HIV-1(NL4-3) using TZM-bl indicator cells. The EC(90) of RAL+EFV-NPs was lower than raltegravir+efavirenz (RAL+EFV) solution but did not reach significance. Compared to control HeLa cells without any treatment, RAL+EFV-NPs or blank gel were not cytotoxic for 14 days in vitro. The intracellular levels of efavirenz in RAL+EFV-NPs treated HeLa cells were above the EC(90) for 14 days whereas raltegravir intracellular concentrations were eliminated within 6 days. Transwell experiments of NPs-in-gel demonstrated rapid transfer of fluorescent nanoparticles from the gel and uptake in HeLa cells within 30 min. These data demonstrate the potential of antiretroviral NP-embedded vagina gels for long-term vaginal pre-exposure prophylaxis of heterosexual HIV-1 transmission.
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Registered trials
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