title: Nanomedicine in the development of anti-HIV microbicides.
abstract: Prevention plays an invaluable role in the fight against HIV/AIDS. The use of microbicides is considered an interesting potential approach for topical pre-exposure prophylaxis of HIV sexual transmission. The prospects of having an effective product available are expected to be fulfilled in the near future as driven by recent and forthcoming results of clinical trials. Different dosage forms and delivery strategies have been proposed and tested for multiple microbicide drug candidates presently at different stages of the development pipeline. One particularly interesting approach comprises the application of nanomedicine principles to the development of novel anti-HIV microbicides, but its implications to efficacy and safety are not yet fully understood. Nanotechnology-based systems, either presenting inherent anti-HIV activity or acting as drug nanocarriers, may significantly influence features such as drug solubility, stability of active payloads, drug release, interactions between active moieties and virus/cells, intracellular drug delivery, drug targeting, safety, antiviral activity, mucoadhesive behavior, drug distribution and tissue penetration, and pharmacokinetics. The present manuscript provides a comprehensive and holistic overview of these topics as relevant to the development of vaginal and rectal microbicides. In particular, recent advances pertaining inherently active microbicide nanosystems and microbicide drug nanocarriers are discussed.
authors.affiliation: i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde & Instituto Universitário de Ciências da Saúde, Gandra, Portugal. Electronic address: j.dasneves@ineb.up.pt.
authors.forename: José
authors.initials: J
authors.lastname: das Neves
authors.affiliation: i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal; ICBAS-Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto, Porto, Portugal.
authors.forename: Rute
authors.initials: R
authors.lastname: Nunes
authors.affiliation: REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.
authors.forename: Francisca
authors.initials: F
authors.lastname: Rodrigues
authors.affiliation: i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde & Instituto Universitário de Ciências da Saúde, Gandra, Portugal. Electronic address: bruno.sarmento@ineb.up.pt.
authors.forename: Bruno
authors.initials: B
authors.lastname: Sarmento
mesh_terms: D000890:Anti-Infective Agents; D016503:Drug Delivery Systems; D015195:Drug Design; D005260:Female; D015658:HIV Infections / Q000628:therapy*; D006801:Humans; D050997:Nanomedicine; D036103:Nanotechnology
chemical_list: D000890:Anti-Infective Agents
keywords: AIDS; Anti-retroviral agents; Dapivirine (PubChem CID: 214347); Dendrimers; Efavirenz (PubChem CID: 64139); Etravirine (PubChem CID: 193962); Maraviroc (PubChem CID: 3002977); Mucous membrane; Nanoparticles; Nanotechnology; Pre-exposure prophylaxis; Rilpivirine (PubChem CID: 6451164); Saquinavir (PubChem CID: 441243); Tenofovir (PubChem CID: 464205); Vaginal drug delivery