Creation of a long-acting rilpivirine prodrug nanoformulation
نویسندگان
چکیده
منابع مشابه
Long-acting rilpivirine for HIV prevention.
PURPOSE OF REVIEW Long-acting injectable antiretroviral (ARV) formulations are being developed for the treatment and prevention of HIV infection. The purpose of this review is to summarize recent preclinical and clinical data on TMC278 (rilpivirine), a nonnucleoside reverse transcriptase inhibitor (NNRTI), that is being developed for both a treatment and prevention indication. RECENT FINDINGS...
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The next-generation human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase inhibitor rilpivirine (TMC278) was administered in rats and dogs as single intramuscular (IM) or subcutaneous (SC) injections, formulated as a 200-nm nanosuspension. The plasma pharmacokinetics, injection site concentrations, disposition to lymphoid tissues, and tolerability were evaluated in sup...
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Rilpivirine long-acting (RPV-LA) is a parenteral formulation enabling prolonged plasma exposure. We explored its multiple-compartment pharmacokinetics (PK) after a single dose, for pre-exposure prophylaxis. Sixty-six HIV-negative volunteers were enrolled: women received an intramuscular dose of 300, 600, or 1,200 mg, with plasma and genital levels measured to 84 days postdose; men receiving 600...
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A nanoformulated myristoylated dolutegravir prodrug (NMDTG) was prepared using good laboratory practice protocols. Intramuscular injection of NMDTG (118 ± 8 mg/ml, 25.5 mg of DTG equivalents/kg of body weight) to three rhesus macaques led to plasma DTG levels of 86 ± 12 and 28 ± 1 ng/ml on days 35 and 91, respectively. The NMDTG platform showed no significant adverse events. Further modificatio...
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The synthesis of twenty five esters of testosterone (17β -hydroxyandrost- 4-en-3-one) is described. All esters are derivatives of cycloalkycarboxylic acids. Some of the esters possess α- , β -and/or & - substitution in the ester side-chain. The work was undertaken in order to evaluate long-acting male antifertility effect of such esters. Most of the compounds, especially compound No.1, wer...
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ژورنال
عنوان ژورنال: Journal of Controlled Release
سال: 2019
ISSN: 0168-3659
DOI: 10.1016/j.jconrel.2019.09.001