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Abstract
We report that a combination of anti-HIV-1 drug efavirenz (EFV), anti-microbial-spermicidal curcumin (Cur) and lactoferrin nanoparticles (ECNPs) act as MPT formulation. These nanoparticles are of well dispersed spherical shape with 40–70 nm size, with encapsulation efficiency of 63 ± 1.9% of Cur & 61.5% ± 1.6 of EFV, significantly higher than that of single drug nanoparticles (Cur, 59 ± 1.34%; EFV: 58.4 ± 1.79). ECNPs were found to be sensitive at pH 5 and 6 and have not effected viability of vaginal micro-flora, Lactobacillus. Studies in rats showed that ECNPs delivers 88–124% more drugs in vaginal lavage as compared to its soluble form, either as single or combination of EFV and Cur. The ECNPs also shows 1.39–4.73 fold lower concentration of absorption in vaginal tissue and plasma compared to soluble EFV + Cur. Furthermore, ECNPs show significant reduction in inflammatory responses by 1.6–3.0 fold in terms of IL-6 and TNF-α in vaginal tissue and plasma compared to soluble EFV + Cur. ECNPs showed improved pharmacokinetics profiles in vaginal lavage with more than 50% of enhancement in AUC, AUMC, Cmax and t1/2 suggesting longer exposure of Cur and EFV in vaginal lavage compared to soluble EFV + Cur. Histopathological analysis of vaginal tissue shows remarkably lower toxicity of ECNPs compared to soluble EFV + Cur. In conclusion, ECNPs are significantly safe and exhibit higher bioavailability thus constitute an effective MPT against HIV.
Highlights
A rate of 76.4 ± 54.8 μ gg−1 and remained constant for seven days after the removal of IVR15
The objective of our study is to develop a triple-combination topical formulation that can simultaneously act on HIV, HIV-mediated inflammation, other viral and bacterial infections with contraceptive action, based on the principle of multipurpose prevention technologies (MPT)
The principle steps in realizing the objectives of this studies are (1) preparation and characterization of lactoferrin nanoparticles loaded with curcumin and EFV; (2) Studying bioavailability and pharmacokinetic profile of curcumin and EFV in vaginal lavage upon topical application of nanoformulation, and (3) Evaluation of safety of nanoformulation in terms of inflammation
Summary
A rate of 76.4 ± 54.8 μ gg−1 and remained constant for seven days after the removal of IVR15. NPs provide several additional benefits, e.g. protection of the drugs against degradation, facilitates targeted action, and delivery of varieties of biological bits, like peptide, protein and nucleotides. The objective of our study is to develop a triple-combination topical formulation that can simultaneously act on HIV, HIV-mediated inflammation, other viral and bacterial infections with contraceptive action, based on the principle of multipurpose prevention technologies (MPT). This is a triple combination of broad spectrum lactoferrin (as vehicle) and curcumin as preventive and protective agent and EFV as therapeutic agent against HIV. The principle steps in realizing the objectives of this studies are (1) preparation and characterization of lactoferrin nanoparticles loaded with curcumin and EFV; (2) Studying bioavailability and pharmacokinetic profile of curcumin and EFV in vaginal lavage upon topical application of nanoformulation, and (3) Evaluation of safety of nanoformulation in terms of inflammation
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