Efavirenz loaded nanostructured lipid carriers for effient and prolonged viral inhibition in HIV-infected macrophages was written by Mahajan, Ketan;Rojekar, Satish;Desai, Dipen;Kulkarni, Smita;Vavia, Pradeep. And the article was included in Pharmaceutical Sciences in 2021.Computed Properties of C20H18N2O2S The following contents are mentioned in the article:
The clin. outcome of anti-HIV therapy is poor due to the inherent fallouts of anti-HIV therapy. It is further worsened due to the presence of viral reservoirs in immune cells like the macrophages. An ideal anti-HIV therapy must reach, deliver the drug and exert its action inside macrophages. To address this, we developed novel cationic nanostructured lipid carriers of efavirenz (cationic EFV-NLC). Th developed cationic EFV NLCs were evaluated for particle size, zeta potential, encapsulation effiency, in-vitro drug release, DSC, XRD, TEM, cytotoxicity, cellular uptake studies and anti-HIV efficy in a monocyte-derived macrophage cell line (THP-1). Cationic EFV-NLCs showed high encapsulation effiency (90.54 ± 1.7%), uniform particle size distribution (PDI 0.3-0.5 range) and high colloidal stability with pos. zeta potential (+23.86 ± 0.49 mV). DSC and XRD studies confirmed the encapsulation of EFV within NLCs. Cytotoxicity studies (MTT assay) revealed excellent cytocompatibility (CC50 13.23 ± 0.54 μg/mL). Fluorescence microscopy confirmed the effient uptake of cationic EFVNLCs, while flow cytometry revealed time and concentration dependant uptake within THP-1 cells. Cationic EFV-NLCs showed higher retention and sustained release with 2.32-fold higher percent inhibition of HIV-1 in infected macrophages as compared to EFV solution at equimolar concentrations Interestingly, they demonstrated 1.23-fold superior anti-HIV efficy over EFVloaded NLCs at equimolar concentrations Cationic NLCs were capable of inhibiting the viral replication at higher limits consistently for 6 days suggesting successful prevention of HIV-1 replication in infected macrophages and thus can prove to be an attractive tool for promising anti-HIV therapy. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Computed Properties of C20H18N2O2S).
3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Computed Properties of C20H18N2O2S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica