Composite films for vaginal delivery of tenofovir disoproxil fumarate and emtricitabine

Mafalda Pereira Cautela1,2, Hen Moshe3, Alejandro Sosnik3, Bruno Sarmento1,2,4, José das Neves1,5,4
1i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal
2INEB – Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal
3Laboratory of Pharmaceutical Nanomaterials Science, Department of Materials Science and Engineering, Technion-Israel Institute of Technology, Technion City, Haifa, Israel
4CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde & Instituto Universitário de Ciências da Saúde, Gandra, Portugal
5INEB - Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal

Tài liệu tham khảo

World Health Organization, Guideline on when to start antiretroviral therapy and on pre-exposure prophylaxis for HIV, Geneva, Switzerland, 2015. PrEPWatch, Country Updates. Available from URL: <http://www.prepwatch.org/advocacy/country-updates/> (accessed Dec 9, 2017). Baeten, 2012, Antiretroviral prophylaxis for HIV prevention in heterosexual men and women, N. Engl. J. Med., 367, 399, 10.1056/NEJMoa1108524 Thigpen, 2012, Antiretroviral preexposure prophylaxis for heterosexual HIV transmission in Botswana, N. Engl. J. Med., 367, 423, 10.1056/NEJMoa1110711 McCormack, 2016, Pre-exposure prophylaxis to prevent the acquisition of HIV-1 infection (PROUD): effectiveness results from the pilot phase of a pragmatic open-label randomised trial, Lancet, 387, 53, 10.1016/S0140-6736(15)00056-2 Marrazzo, 2015, VOICE Study Team, Tenofovir-based preexposure prophylaxis for HIV infection among African women, N. Engl. J. Med., 372, 509, 10.1056/NEJMoa1402269 Van Damme, 2012, Preexposure prophylaxis for HIV infection among African women, N. Engl. J. Med., 367, 411, 10.1056/NEJMoa1202614 Murnane, 2013, Efficacy of preexposure prophylaxis for HIV-1 prevention among high-risk heterosexuals: subgroup analyses from a randomized trial, AIDS, 27, 2155, 10.1097/QAD.0b013e3283629037 Sheth, 2016, HIV pre-exposure prophylaxis for women, J. Virus Erad., 2, 149, 10.1016/S2055-6640(20)30458-1 Cottrell, 2016, A translational pharmacology approach to predicting outcomes of preexposure prophylaxis against HIV in men and women using tenofovir disoproxil fumarate with or without emtricitabine, J. Infect. Dis., 214, 55, 10.1093/infdis/jiw077 Donnell, 2014, HIV protective efficacy and correlates of tenofovir blood concentrations in a clinical trial of PrEP for HIV prevention, J. Acquir. Immune Defic. Syndr., 66, 340, 10.1097/QAI.0000000000000172 Molina, 2015, On-demand preexposure prophylaxis in men at high risk for HIV-1 infection, N. Engl. J. Med., 373, 2237, 10.1056/NEJMoa1506273 Baeten, 2013, Systemic and topical drugs for the prevention of HIV infection: antiretroviral pre-exposure prophylaxis, Annu. Rev. Med., 64, 219, 10.1146/annurev-med-050911-163701 Cottrell, 2014, Topical microbicides and HIV prevention in the female genital tract, J. Clin. Pharmacol., 54, 603, 10.1002/jcph.292 Abdool Karim, 2010, Effectiveness and safety of tenofovir gel, an antiretroviral microbicide, for the prevention of HIV infection in women, Science, 329, 1168, 10.1126/science.1193748 Baeten, 2016, MTN-Aspire Study Team, Use of a vaginal ring containing dapivirine for HIV-1 prevention in women, N. Engl. J. Med., 375, 2121, 10.1056/NEJMoa1506110 Nel, 2016, Safety and efficacy of a dapivirine vaginal ring for HIV prevention in women, N. Engl. J. Med., 375, 2133, 10.1056/NEJMoa1602046 Srinivasan, 2016, Topical delivery of tenofovir disoproxil fumarate and emtricitabine from pod-intravaginal rings protects macaques from multiple SHIV exposures, PLoS One, 11, e0157061, 10.1371/journal.pone.0157061 Moss, 2014, Pharmacokinetics and preliminary safety study of pod-intravaginal rings delivering antiretroviral combinations for HIV prophylaxis in a macaque model, Antimicrob. Agents Chemother., 58, 5125, 10.1128/AAC.02871-14 Clark, 2014, Evaluation of rapidly disintegrating vaginal tablets of tenofovir, emtricitabine and their combination for HIV-1 prevention, Pharmaceutics, 6, 616, 10.3390/pharmaceutics6040616 Nel, 2011, Acceptability of vaginal film, soft-gel capsule, and tablet as potential microbicide delivery methods among African women, J. Womens Health (Larchmt.), 20, 1207, 10.1089/jwh.2010.2476 Rohan, 2014, Vaginal microbicide films, 291 Caramella, 2015, Mucoadhesive and thermogelling systems for vaginal drug delivery, Adv. Drug Deliv. Rev., 92, 39, 10.1016/j.addr.2015.02.001 das Neves, 2017, Antiretroviral drug-loaded nanoparticles-in-films: a new option for developing vaginal microbicides?, Expert Opin. Drug Deliv., 14, 449, 10.1080/17425247.2017.1270938 Sosnik, 2015, Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers, Adv. Colloid Interface Sci., 223, 40, 10.1016/j.cis.2015.05.003 Destache, 2016, Topical tenofovir disoproxil fumarate nanoparticles prevent HIV-1 vaginal transmission in a humanized mouse model, Antimicrob. Agents Chemother., 60, 3633, 10.1128/AAC.00450-16 Cunha-Reis, 2016, Nanoparticles-in-film for the combined vaginal delivery of anti-HIV microbicide drugs, J. Control. Release, 243, 43, 10.1016/j.jconrel.2016.09.020 Smith, 2013, Intravaginal ring eluting tenofovir disoproxil fumarate completely protects macaques from multiple vaginal simian-HIV challenges, Proc. Natl. Acad. Sci. U.S.A., 110, 16145, 10.1073/pnas.1311355110 Machado, 2016, Development and in vivo safety assessment of tenofovir-loaded nanoparticles-in-film as a novel vaginal microbicide delivery system, Acta Biomater., 44, 332, 10.1016/j.actbio.2016.08.018 Owen, 1999, A vaginal fluid simulant, Contraception, 59, 91, 10.1016/S0010-7824(99)00010-4 Moore, 1996, Mathematical comparison of dissolution profiles, Pharm. Tech., 20, 64 International Organization for Standardization, ISO 10993-5:2009 Biological Evaluation of Medical Devices – Part 5: Tests for In Vitro Cytotoxicity, Geneva, Switzerland. Gallay, 2017, Prevention of vaginal and rectal HIV transmission by antiretroviral combinations in humanized mice, PLoS One, 12, e0184303, 10.1371/journal.pone.0184303 Laborde, 2017, Impact of the dapivirine vaginal ring on sexual experiences and intimate partnerships of women in an HIV prevention clinical trial: managing ring detection and hot sex, AIDS Behav. Ramazani, 2016, Strategies for encapsulation of small hydrophilic and amphiphilic drugs in PLGA microspheres: state-of-the-art and challenges, Int. J. Pharm., 499, 358, 10.1016/j.ijpharm.2016.01.020 Thakral, 2013, Eudragit: a technology evaluation, Expert Opin. Drug Deliv., 10, 131, 10.1517/17425247.2013.736962 Larsson, 2012, Suspension stability; why particle size, zeta potential and rheology are important, Ann. Trans. Nord. Rheol. Soc., 20, 209 Bootz, 2004, Comparison of scanning electron microscopy, dynamic light scattering and analytical ultracentrifugation for the sizing of poly(butyl cyanoacrylate) nanoparticles, Eur. J. Pharm. Biopharm., 57, 369, 10.1016/S0939-6411(03)00193-0 Pokharkar, 2015, Engineering of a hybrid polymer-lipid nanocarrier for the nasal delivery of tenofovir disoproxil fumarate: physicochemical, molecular, microstructural, and stability evaluation, Eur. J. Pharm. Sci., 71, 99, 10.1016/j.ejps.2015.02.009 Mandal, 2017, An enhanced emtricitabine-loaded long-acting nanoformulation for prevention or treatment of HIV infection, Antimicrob. Agents Chemother., 61, e01475-16, 10.1128/AAC.01475-16 Schafroth, 2012, Nano and microparticle engineering of water insoluble drugs using a novel spray-drying process, Colloids Surf. B Biointerfaces, 90, 8, 10.1016/j.colsurfb.2011.09.038 Seremeta, 2014, Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability, Colloids Surf. B Biointerfaces, 123, 515, 10.1016/j.colsurfb.2014.09.055 Akil, 2015, Formulation and characterization of polymeric films containing combinations of antiretrovirals (ARVs) for HIV prevention, Pharm. Res., 32, 458, 10.1007/s11095-014-1474-4 Cunha, 2014, Characterization of commercially available vaginal lubricants: a safety perspective, Pharmaceutics, 6, 530, 10.3390/pharmaceutics6030530 Preis, 2014, Mechanical strength test for orodispersible and buccal films, Int. J. Pharm., 461, 22, 10.1016/j.ijpharm.2013.11.033 Fan, 2016, Preferred physical characteristics of vaginal film microbicides for HIV prevention in Pittsburgh women, Arch. Sex. Behav., 46, 1111, 10.1007/s10508-016-0816-1 Dezzutti, 2012, Is wetter better? An evaluation of over-the-counter personal lubricants for safety and anti-HIV-1 activity, PLoS One, 7, e48328, 10.1371/journal.pone.0048328 Levin, 2003, A journey through two lumens!, Int. J. Impot. Res., 15, 2, 10.1038/sj.ijir.3900977 Fernández-Romero, 2015, Preclinical assessments of vaginal microbicide candidate safety and efficacy, Adv. Drug Deliv. Rev., 92, 27, 10.1016/j.addr.2014.12.005 das Neves, 2015, Precise engineering of dapivirine-loaded nanoparticles for the development of anti-HIV vaginal microbicides, Acta Biomater., 18, 77, 10.1016/j.actbio.2015.02.007 Catalone, 2005, Comparative safety evaluation of the candidate vaginal microbicide C31G, Antimicrob. Agents Chemother., 49, 1509, 10.1128/AAC.49.4.1509-1520.2005 Gali, 2010, In vitro evaluation of viability, integrity and inflammation in genital epithelia upon exposure to pharmaceutical excipients and candidate microbicides, Antimicrob. Agents Chemother., 54, 5105, 10.1128/AAC.00456-10 Hillier, 2005, In vitro and in vivo: the story of nonoxynol 9, J. Acquir. Immune Defic. Syndr., 39, 1, 10.1097/01.qai.0000159671.25950.74