ArticleThe AAPS journal2008
Characterization of cyclodextrin inclusion complexes of the anti-HIV non-nucleoside reverse transcriptase inhibitor UC781.
Article in The AAPS journal, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Weak complexation of 5-fluorouracil with β-cyclodextrin, carbonate, and dianhydride crosslinked β-cyclodextrin:Research in pharmaceutical sciences · 2022Article
- Enhanced Nanoencapsulation of Sepiapterin within PEG-PCL Nanoparticles by Complexation with Triacetyl-Beta Cyclodextrin.Molecules (Basel, Switzerland) · 2019Article
- Nano-ART and NeuroAIDS.Drug delivery and translational research · 2016Review
- A promising antitumor activity of evodiamine incorporated in hydroxypropyl-β-cyclodextrin: pro-apoptotic activity in human hepatoma HepG2 cells.Chemistry Central journal · 2016Article
- Clinical use of vaginal or rectally applied microbicides in patients suffering from HIV/AIDS.HIV/AIDS (Auckland, N.Z.) · 2013Review
- Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.Bioorganic & medicinal chemistry letters · 2013Article
- Characterization of UC781-tenofovir combination gel products for HIV-1 infection prevention in an ex vivo ectocervical model.Antimicrobial agents and chemotherapy · 2012Article
- A thermodynamic study of the cyclodextrin-UC781 inclusion complex using a HPLC method.Journal of inclusion phenomena and macrocyclic chemistry · 2012Article
- Changes in the intestinal absorption mechanism of icariin in the nanocavities of cyclodextrins.International journal of nanomedicine · 2012Article
- Microbicides: a new hope for HIV prevention.The Indian journal of medical research · 2011Review
- Development and Characterization of a Vaginal Film Containing Dapivirine, a Non- nucleoside Reverse Transcriptase Inhibitor (NNRTI), for prevention of HIV-1 sexual transmission.Drug delivery and translational research · 2011Article
- Progress in antiretroviral drug delivery using nanotechnology.International journal of nanomedicine · 2010Review
- Targeting Trojan Horse leukocytes for HIV prevention.AIDS (London, England) · 2010Review
- Influence of Ethanol as a Co-Solvent in Cyclodextrin Inclusion Complexation: A Molecular Dynamics Study.Scientia pharmaceuticaArticle
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Authors and funding
5 authors.
Funding
Abstract
The highly potent anti-HIV agent UC781 is being evaluated for use in topical microbicides to prevent HIV transmission. However, UC781 is extremely hydrophobic with poor water solubility, a property that may complicate appropriate formulation of the drug. In this study, we examined the ability of several cyclodextrins, beta-cyclodextrin (beta CD), methyl-beta-cyclodextrin (M beta CD), and 2-hydroxylpropyl-beta-cyclodextrin (HP beta CD), to enhance the aqueous solubility of UC781. Each of the cyclodextrins provided dramatic increases in UC781 aqueous solubility, the order being M beta CD>HP beta CD>beta CD. The complexation constants (K (1:1)) of the inclusion complexes were determined via a phase solubility technique using high-performance liquid chromatography and showed that UC781 solubility increased linearly as a function of cyclodextrin concentration. Ultraviolet spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and 2D (1)H ROESY NMR spectroscopy were used to further characterize these UC781/cyclodextrin complexes. The inhibitory potency of UC781 and its HP beta CD inclusion complex were evaluated using an in vitro HIV-1 reverse transcriptase inhibition assay The inhibitory potency of the UC781/HP beta CD complex was 30-fold greater than that of UC781 alone, showing that the complexed drug is able to provide substantial inhibition of its target. The enhancement of UC781 aqueous solubility is essential for the development of a useful vaginal microbicide dosage form, and our data suggest that UC781/cyclodextrin inclusion complexes may be useful in this context.
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