{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,19]],"date-time":"2025-11-19T11:34:52Z","timestamp":1763552092656,"version":"build-2065373602"},"reference-count":69,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2020,12,30]],"date-time":"2020-12-30T00:00:00Z","timestamp":1609286400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100006769","name":"Russian Science Foundation","doi-asserted-by":"publisher","award":["16-13-10344"],"award-info":[{"award-number":["16-13-10344"]}],"id":[{"id":"10.13039\/501100006769","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Despite the world\u2019s combined efforts, human immunodeficiency virus (HIV), the causative agent of AIDS, remains one of the world\u2019s most serious public health challenges. High genetic variability of HIV complicates the development of anti-HIV vaccine, and there is an actual clinical need for increasing the efficiency of anti-HIV drugs in terms of targeted delivery and controlled release. Tenofovir (TFV), a nucleotide-analog reverse transcriptase inhibitor, has gained wide acceptance as a drug for pre-exposure prophylaxis or treatment of HIV infection. In our study, we explored the potential of tenofovir disoproxil (TFD) adducts with block copolymers of poly(ethylene glycol) monomethyl ether and poly(ethylene phosphoric acid) (mPEG-b-PEPA) as candidates for developing a long-acting\/controlled-release formulation of TFV. Two types of mPEG-b-PEPA with numbers of ethylene phosphoric acid (EPA) fragments of 13 and 49 were synthesized by catalytic ring-opening polymerization, and used for preparing four types of adducts with TFD. Antiviral activity of [mPEG-b-PEPA]TFD or tenofovir disoproxil fumarate (TDF) was evaluated using the model of experimental HIV infection in vitro (MT-4\/HIV-1IIIB). Judging by the values of the selectivity index (SI), TFD exhibited an up to 14-fold higher anti-HIV activity in the form of mPEG-b-PEPA adducts, thus demonstrating significant promise for further development of long-acting\/controlled-release injectable TFV formulations.<\/jats:p>","DOI":"10.3390\/ijms22010340","type":"journal-article","created":{"date-parts":[[2020,12,30]],"date-time":"2020-12-30T20:13:41Z","timestamp":1609359221000},"page":"340","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["A New Approach to Developing Long-Acting Injectable Formulations of Anti-HIV Drugs: Poly(Ethylene Phosphoric Acid) Block Copolymers Increase the Efficiency of Tenofovir against HIV-1 in MT-4 Cells"],"prefix":"10.3390","volume":"22","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-9151-1890","authenticated-orcid":false,"given":"Ilya","family":"Nifant\u2019ev","sequence":"first","affiliation":[{"name":"Chemistry Department, M.V. Lomonosov Moscow State University, 1\u20133 Leninskie Gory, 119991 Moscow, Russia"},{"name":"A.V. Topchiev Institute of Petrochemical Synthesis RAS, 29 Leninsky Pr., 119991 Moscow, Russia"},{"name":"Faculty of Chemistry, National Research University Higher School of Economics, Miasnitskaya Str. 20, 101000 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7576-2059","authenticated-orcid":false,"given":"Andrei","family":"Siniavin","sequence":"additional","affiliation":[{"name":"N.F. Gamaleya National Research Center for Epidemiology and Microbiology MHRF, 18 Gamaleya Str., 123098 Moscow, Russia"},{"name":"Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eduard","family":"Karamov","sequence":"additional","affiliation":[{"name":"N.F. Gamaleya National Research Center for Epidemiology and Microbiology MHRF, 18 Gamaleya Str., 123098 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maxim","family":"Kosarev","sequence":"additional","affiliation":[{"name":"Chemistry Department, M.V. Lomonosov Moscow State University, 1\u20133 Leninskie Gory, 119991 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sergey","family":"Kovalchuk","sequence":"additional","affiliation":[{"name":"Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ali","family":"Turgiev","sequence":"additional","affiliation":[{"name":"N.F. Gamaleya National Research Center for Epidemiology and Microbiology MHRF, 18 Gamaleya Str., 123098 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sergey","family":"Nametkin","sequence":"additional","affiliation":[{"name":"Chemistry Department, M.V. Lomonosov Moscow State University, 1\u20133 Leninskie Gory, 119991 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Vladimir","family":"Bagrov","sequence":"additional","affiliation":[{"name":"Chemistry Department, M.V. Lomonosov Moscow State University, 1\u20133 Leninskie Gory, 119991 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Alexander","family":"Tavtorkin","sequence":"additional","affiliation":[{"name":"A.V. Topchiev Institute of Petrochemical Synthesis RAS, 29 Leninsky Pr., 119991 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0181-5952","authenticated-orcid":false,"given":"Pavel","family":"Ivchenko","sequence":"additional","affiliation":[{"name":"Chemistry Department, M.V. Lomonosov Moscow State University, 1\u20133 Leninskie Gory, 119991 Moscow, Russia"},{"name":"A.V. Topchiev Institute of Petrochemical Synthesis RAS, 29 Leninsky Pr., 119991 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2020,12,30]]},"reference":[{"key":"ref_1","unstructured":"(2020, December 01). Global HIV & AIDS Statistics\u20142020 Fact Sheet. 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