Microbicide Dosage Forms

Rohan, Lisa C.; Devlin, Bríd; Yang, Haitao

doi:10.1007/82_2013_357

Cited by 14 publications

(17 citation statements)

References 140 publications

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“…Furthermore, optimized poly(ethylene oxide)-modified polycaprolactone nanoparticles were shown to be safe and provided favorable pharmacokinetics after vaginal delivery in a mouse model. Higher and prolonged levels of dapivirine at the lower genital tract were observed as compared with the drug in suspension ( Figure 4) [46]. These results suggest that the use of nanoparticles may potentially increase the protection window of dapivirine against vaginal HIV transmission.…”

Section: Nanomedicine and Prevention Of Hiv Sexual Transmissionmentioning

confidence: 81%

“…As advances continue to be made in the field of nanomedicine, approaches to eliminating HIV-1 in patients globally may sway from mainly treating the virus via drug therapeutics to preventative measures. One possible method of prevention is the use of topical microbicides, defined as products containing one or more anti-HIV compounds and intended to be locally administered around the time of sexual intercourse (coitus-dependent microbicides) or otherwise allow sustained drug levels for prolonged periods irrespective of the time of use (coitus-independent microbicides) [46]. Microbicides have been tested in an attempt to prevent transmission of HIV-1 through vaginal and/or rectal routes.…”

Section: Nanomedicine and Prevention Of Hiv Sexual Transmissionmentioning

confidence: 99%

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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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Section: Nanomedicine and Prevention Of Hiv Sexual Transmissionmentioning

confidence: 81%

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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“…If the aim is instant protection after administration, fast-dissolving tablets can be obtained depending on the excipients used in their development 159,160. Tablets can also be manufactured to release the drug in a sustained manner, enabling controlled drug release and remaining effective for longer, in turn requiring fewer applications and favoring adherence to treatment.…”

Section: Historical Development Of Vaginal Microbicidesmentioning

confidence: 99%

Historical development of vaginal microbicides to prevent sexual transmission of HIV in women: from past failures to future hopes

Notario-Pérez¹,

Ruíz-Caro²,

Veiga-Ochoa³

2017

DDDT

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Infection with human immunodeficiency virus (HIV) remains a global public health concern and is particularly serious in low- and middle-income countries. Widespread sexual violence and poverty, among other factors, increase the risk of infection in women, while currently available prevention methods are outside the control of most. This has driven the study of vaginal microbicides to prevent sexual transmission of HIV from men to women in recent decades. The first microbicides evaluated were formulated as gels for daily use and contained different substances such as surfactants, acidifiers and monoclonal antibodies, which failed to demonstrate efficacy in clinical trials. A gel containing the reverse transcriptase inhibitor tenofovir showed protective efficacy in women. However, the lack of adherence by patients led to the search for dosage forms capable of releasing the active principle for longer periods, and hence to the emergence of the vaginal ring loaded with dapivirine, which requires a monthly application and is able to reduce the sexual transmission of HIV. The future of vaginal microbicides will feature the use of alternative dosage forms, nanosystems for drug release and probiotics, which have emerged as potential microbicides but are still in the early stages of development. Protecting women with vaginal microbicide formulations would, therefore, be a valuable tool for avoiding sexual transmission of HIV.

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“…The rationale for using topically administered products is that vaginal and rectal administration could result in better accumulation of administered drugs in the cervicovaginal tissues, colorectal tissue, and immune cells associated with these tissues, compared to the oral and systemic routes [16]. In addition, topical administration results in lower systemic drug levels compared to oral and other administration routes, and is less likely to cause systemic side effects [17, 18]. …”

Section: Introductionmentioning

confidence: 99%

Drug transporters in tissues and cells relevant to sexual transmission of HIV: Implications for drug delivery

Patel

Zhou

et al. 2015

Journal of Controlled Release

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Efflux and uptake transporters of drugs are key regulators of the pharmacokinetics of many antiretroviral drugs. A growing body of literature has revealed the expression and functionality of multiple transporters in female genital tract (FGT), colorectal tissue, and immune cells. Drug transporters could play a significant role in the efficacy of preventative strategies for HIV-1 acquisition. Pre-exposure prophylaxis (PrEP) is a promising strategy, which utilizes topically (vaginally or rectally), orally or other systemically administered antiretroviral drugs to prevent the sexual transmission of HIV to receptive partners. The drug concentration in the receptive mucosal tissues and target immune cells for HIV is critical for PrEP effectiveness. Hence, there is an emerging interest in utilizing transporter information to explain tissue disposition patterns of PrEP drugs, to interpret inter-individual variability in PrEP drug pharmacokinetics and effectiveness, and to improve tissue drug exposure through modulation of the cervicovaginal, colorectal, or immune cell transporters. In this review, the existing literature on transporter expression, functionality and regulation in the transmission-related tissues and cells is summarized. In addition, the relevance of transporter function for drug delivery and strategies that could exploit transporters for increased drug concentration at target locales is discussed. The overall goal is to facilitate an understanding of drug transporters for PrEP optimization.

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Microbicide Dosage Forms

Cited by 14 publications

References 140 publications

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

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

Historical development of vaginal microbicides to prevent sexual transmission of HIV in women: from past failures to future hopes

Drug transporters in tissues and cells relevant to sexual transmission of HIV: Implications for drug delivery

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