scholarly journals Dapivirine Bioadhesive Vaginal Tablets Based on Natural Polymers for the Prevention of Sexual Transmission of HIV

Polymers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 483 ◽  
Author(s):  
Raúl Cazorla-Luna ◽  
Araceli Martín-Illana ◽  
Fernando Notario-Pérez ◽  
Luis-Miguel Bedoya ◽  
Paulina Bermejo ◽  
...  
Keyword(s):  
Sexual Transmission ◽  
Vaginal Fluid ◽  
Natural Polymers ◽  
Vaginal Microbicides ◽  
Realistic Option ◽  
Sub Saharan ◽  
Sexual Transmission Of Hiv ◽  
Prevention Of Sexual Transmission ◽  
Exposure Prophylaxis ◽  
Self Protection

Young sub-Saharan women are a group that is vulnerable to the sexual transmission of HIV. Pre-exposure prophylaxis through vaginal microbicides could provide them an option for self-protection. Dapivirine has been demonstrated to have topical inhibitory effects in HIV, and to provide protection against the sexual transmission of this virus. This paper reports on the studies into swelling behaviour, bioadhesion and release carried out on dapivirine tablets based on chitosan, locust bean gum and pectin, to select the most suitable formulation. The modified simulated vaginal fluid led to a high solubility of dapivirine and allowed the dapivirine release profiles to be characterized in sink conditions; this aqueous medium is an alternative to organic solvents, which are not a realistic option when evaluating systems whose behaviour varies in aqueous and organic media. Of the formulations evaluated, dapivirine/pectin tablets containing 290 mg of polymer and 30 mg of dapivirine present the most moderate swelling, making them the most comfortable dosage forms. Their high bioadhesive capacity would also allow the formulation to remain in the action zone and release the drug in a sustained manner, pointing to this formulation as the most promising candidate for future evaluations of vaginal microbicides for the prevention of HIV.

scholarly journals Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir

Pharmaceutics ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 20 ◽  
Author(s):  
Raúl Cazorla-Luna ◽  
Fernando Notario-Pérez ◽  
Araceli Martín-Illana ◽  
Roberto Ruiz-Caro ◽  
Aitana Tamayo ◽  
...  
Keyword(s):  
Sexual Transmission ◽  
Microstructural Characterization ◽  
Vaginal Fluid ◽  
Vaginal Mucosa ◽  
Vaginal Microbicides ◽  
Polyelectrolyte Complexes ◽  
Antiretroviral Drug ◽  
Sexual Transmission Of Hiv ◽  
Self Protection

Vaginal microbicides have the potential to give women at high risk of contracting HIV the option of self-protection by preventing the sexual transmission of the virus. In this paper, mucoadhesive vaginal tablets based on chitosan, alone and in combination with pectin and locust bean gum, were developed for the sustained release of tenofovir (an antiretroviral drug). The formulations were placed in simulant vaginal fluid (SVF) to swell, and Hg porosity and SEM microscopy were used for the microstructural characterization of the swelling witnesses. The results show that the association of pectin and chitosan generated polyelectrolyte complexes and produced a robust system able to maintain its structure during the swelling process, when small pores are formed. Drug release and bovine vaginal mucoadhesion studies were performed in SVF showing that tenofovir-controlled dissolution profiles and adhesion to the mucosa were conditioned by the swelling processes of the polymer/s in each formulation. Tablets based on chitosan/pectin have the most homogeneous tenofovir dissolution profiles and last up to 96 h, remaining attached to the vaginal mucosa for the same period. These formulations can therefore be considered a good option for the self-protection of women from the sexual transmission of HIV.

scholarly journals Smart Freeze-Dried Bigels for the Prevention of the Sexual Transmission of HIV by Accelerating the Vaginal Release of Tenofovir during Intercourse

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 232 ◽  
Author(s):  
Araceli Martín-Illana ◽  
Fernando Notario-Pérez ◽  
Raúl Cazorla-Luna ◽  
Roberto Ruiz-Caro ◽  
María Dolores Veiga
Keyword(s):  
Controlled Release ◽  
Seminal Fluid ◽  
Sexual Transmission ◽  
Antiretroviral Drugs ◽  
African Women ◽  
Vaginal Fluid ◽  
Freeze Dried ◽  
Route Of Transmission ◽  
Sub Saharan ◽  
Sexual Transmission Of Hiv

Sub-Saharan African women are still at risk from the human immunodeficiency virus (HIV), and sex with men is the main route of transmission. Vaginal formulations containing antiretroviral drugs are promising tools to give women the power to protect themselves. The aim of this work was to obtain freeze-dried bigels containing pectin, chitosan, or hypromellose for the vaginal controlled release of Tenofovir, which is accelerated in the presence of semen. Nine batches of bigels were formulated using different proportions of these polymers in the hydrogel (1, 2, and 3% w/w). The bigels obtained were freeze-dried and then underwent hardness and deformability, mucoadhesion, swelling, and drug release tests, the last two in simulated vaginal fluid (SVF) and SVF/simulated seminal fluid (SSF) mixture. The formulation containing 3% pectin (fd3P) has the highest values for hardness, resistance to deformation, and good mucoadhesivity. Its swelling is conditioned by the pH of the medium, which is responsive to the controlled release of Tenofovir in SVF, with the fastest release in the SVF/SSF mixture. fd3P would be an interesting smart microbicidal system to allow faster release of Tenofovir in the presence of semen, and thus increase women’s ability to protect themselves from the sexual transmission of HIV.

scholarly journals Influence of Chitosan Swelling Behaviour on Controlled Release of Tenofovir from Mucoadhesive Vaginal Systems for Prevention of Sexual Transmission of HIV

Marine Drugs ◽  
2017 ◽  
Vol 15 (2) ◽  
pp. 50 ◽  
Author(s):  
Fernando Notario-Pérez ◽  
Araceli Martín-Illana ◽  
Raúl Cazorla-Luna ◽  
Roberto Ruiz-Caro ◽  
Luis-Miguel Bedoya ◽  
...  
Keyword(s):  
Controlled Release ◽  
Sexual Transmission ◽  
Swelling Behaviour ◽  
Sexual Transmission Of Hiv ◽  
Prevention Of Sexual Transmission

scholarly journals Vaginal Formulations for Prevention of Sexual Transmission of HIV

2018 ◽  
Author(s):  
María-Dolores Veiga-Ochoa ◽  
Roberto Ruiz-Caro ◽  
Raúl Cazorla-Luna ◽  
Araceli Martín-Illana ◽  
Fernando Notario-Pérez
Keyword(s):  
Sexual Transmission ◽  
Sexual Transmission Of Hiv ◽  
Prevention Of Sexual Transmission

“Do I need to use condoms if I’m taking my meds?”

HIV ◽  
2020 ◽  
pp. 45-54
Author(s):  
Robert K. Bolan
Keyword(s):  
Viral Load ◽  
Sexual Transmission ◽  
Hiv Treatment ◽  
Load Testing ◽  
Hiv Replication ◽  
Viral Load Testing ◽  
Sexual Transmission Of Hiv ◽  
The Individual ◽  
Exposure Prophylaxis ◽  
Living With Hiv

It has been conclusively proven that sexual transmission of HIV does not occur if the individual living with HIV is adherent to antiretroviral therapy and HIV replication is consistently maintained below a plasma level of 200 copies/mL. What remains to be defined is the frequency of viral load testing to provide assurance that HIV is suppressed and how long must it remain so until suppression can be considered durable. This is required in order to provide guidance for HIV pre-exposure prophylaxis (PrEP) use by a sexual partner who is not living with HIV. Based on currently published studies and until more data are presented, it seems prudent to recommend that sexual partners of individuals living with HIV who are highly adherent to treatment use PrEP for 6 months to 1 year following initiation of HIV treatment and that viral load testing be performed quarterly for at least the first 2 years in the partner living with HIV.

scholarly journals Strategies to prevent HIV transmission to serodiscordant couples

2015 ◽  
Vol 18 (suppl 1) ◽  
pp. 169-182 ◽  
Author(s):  
Ronaldo Campos Hallal ◽  
Juan Carlos Raxach ◽  
Nêmora Tregnago Barcellos ◽  
Ivia Maksud
Keyword(s):  
Hiv Transmission ◽  
Sexual Transmission ◽  
Sexual Practices ◽  
Transmission Risk ◽  
Prevention Policy ◽  
Serodiscordant Couples ◽  
Prevention Interventions ◽  
Single Strategy ◽  
Sexual Transmission Of Hiv ◽  
Exposure Prophylaxis

ABSTRACTIntroduction:The use antiretroviral reduces the sexual transmission of HIV, expanding interventions for serodiscordant couples.Objective:This article aims to review the use of antiretroviral and other prevention interventions among serodiscordant couples and to analyze its use in Brazil.Methods:A retrospective review was performed through the MEDLINE database and bases included in the Biblioteca Virtual em Saúde.Results:The articles recovered exhibit four main strategies: (1) condom; (2) reduction of risks in sexual practices; (3) use of antiretrovirals, particularly early initiation of antiretroviral therapy (TASP) and pre-exposure prophylaxis (PrEP); (4) risk reduction in reproduction.Discussion:TASP is highly effective in reducing sexual transmission, PrEP was tested in serodiscordant couples and both reduce the sexual transmission risk in different sexual practices, enabling individualized prevention strategies.Conclusions:When used in combination, antiretrovirals and sexual practices with condoms offer greater efficacy than any single strategy. The combined use of new and old strategies allows us to build a prevention policy for all.

Acceptability of tenofovir gel as a vaginal microbicide among women in a phase I trial a mixed-methods study,

2020 ◽  
Author(s):  
Lungwani Muungo
Keyword(s):  
Clinical Trials ◽  
Phase I ◽  
Phase I Trial ◽  
Hiv Transmission ◽  
Sexual Transmission ◽  
Initial Product ◽  
Vaginal Microbicides ◽  
Tenofovir Gel ◽  
Gender Based ◽  
Sexual Transmission Of Hiv

THE GLOBAL HIV EPIDEMIC increasingly affectswomen.1 For most, the only risk factor for becominginfected is the behavior of their male sexualpartners.1 Condoms often are unacceptableand insufficiently used,2–4 gender-based powerimbalances can make them difficult to negotiate,4–7 and religious beliefs, fertility needs, fear ofimplied infidelity, and preferences for sex withouta barrier are challenges to their acceptabilityand use. Women-initiated HIV prevention methodsare urgently needed, making the developmentof vaginal microbicides that reduce the likelihoodof sexual transmission of HIV a majorpublic health priority.First-generation vaginal microbicides will mostlikely be topical gels inserted into the vagina withan applicator. A variety of microbicides is currentlyunder development, and six have enteredlate-stage clinical trials.8–12 Initial product acceptabilityhas been assessed in clinical trials,13–16 surveysof product attributes among potentialusers17,18 and their partners,19 and studies that useover-the-counter (OTC) surrogates or placebo gelwith presumed similar formulation and applicationcharacteristics as eventual products.20–23 Acceptabilityassessments in early clinical trials areespecially important because their findings can influencefurther development of the product.Here, we report on acceptability data amongwomen participating in a phase I trial of tenofovirgel, a candidate microbicide that inhibits HIV reversetranscriptase. Details of the trial are reportedelsewhere,24 as is acceptability amongmale partners of trial participants.25 This was thefirst human trial of a topical antiretroviral thatspecifically inhibits a necessary replication stepin the HIV life cycle. Interest in this approach toHIV prevention has increased in recent yearssince efficacy trials of a topical surfactant(nonoxynyl-9) and a nonspecific inhibitor of HIVbinding (cellulose sulfate) indicated that thesetwo types of compounds were not protective andpotentially increased HIV transmission in womenwho had frequent sexual exposures to HIV. Severallarger-scale, expanded safety and proof-ofconcepttrials of tenofovir gel are now underway,based in part on the safety, tolerability, and acceptabilityof this microbicide demonstrated inthe study described in this paper.

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