Anita Singh

Hepatocellular carcinoma (HCC) causes the third highest mortality worldwide. Liver ablation, surgery, and embolization are conventional methods for treatment. However, these methods have limitations. To overcome these issues, nanomedicines have potential due to their high stability, high drug load capacity, and controlled release. Thus, we prepared quercetin-loaded polylactic-co-glycolic acid (PLGA) nanoparticles coated with folic acid-chitosan (QPCF-NPs) to improve drug delivery and targetability applications of quercetin for the treatment of HCC. We prepared QPCF-NPs by solvent evaporation and coated them with chitosan-folic acid (CS-FA). QPCF-NPs were examined using Fourier-Transform infrared (FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and X-ray diffraction (XRD). In addition, the drug release rate and cytotoxicity were studied. Moreover, in vivo HCC studies such as histopathology and biochemical parameters were conducted. Subsequently, QPCF-NPs with a spherical shape and an average size of 200–290 nm have been demonstrated to have formed by FTIR, XRD, SEM, and TEM. Further, we observed sustained drug release from QPCF-NPs compared to quercetin. Cellular cytotoxicity showed significant inhibition in the HEPG2-cell line with QPCF-NPs treatment. Biochemical estimate and oxidative stress regulation were considerably more regulated in the treatment groups than the HCC group in a dose-dependent way after subcutaneous administration of QPCF-NPs. ELISA of interleukin and caspase-3 demonstrated the anticipated results in comparison to the carcinogen control group. Compared to earlier preparations, the QPCF-NPs generated demonstrated better drug targetability and potency for treating HCC.

The pharmacophore concept was first put forward as a useful picture of drug interactions almost a century ago, and with the rise in computational power over the last few decades, has become a well-established CADD method with numerous different applications in drug discovery. Depending on the prior knowledge of the system, pharmacophores can be used to identify derivatives of compounds, change the scaffold to new compounds with a similar target, virtual screen for novel inhibitors, profile compounds for ADME-tox, investigate possible off-targets, or just complement other molecular methods “chemical groups” or functions in a molecule were responsible for a biological effect, and molecules with similar effect had similar functions in common. The word pharmacophore was coined much later, by Schueler in his 1960 book Chemobiodynamics and Drug Design, and was defined as “a molecular framework that carries (phoros) the essential features responsible for a drug’s (Pharmacon) biological activity.

Pleurospermum angelicoidesBenth is an important medicinal herb of the family Apiaceae, roots of the plant are used as condiments in the Uttarakhand region. This study aimed to investigate the chemical composition andin-vitroantioxidant activity ofP. angelicoidesroots. The essential oil was isolated from the dried roots ofP. angelicoidescollected from high altitude region of Uttarakhand by the hydro-distillation method and subjected to gas chromatography-mass spectrometry (GC/MS). The antioxidant activity of the essential oil, hydroalcoholic, and aqueous extract was carried out by using the ABTS method. GC/MS analysis of essential oil identified 24 different chemical constituents including beta-ocimene (12.5 %), Z-lingustilide (10.5 %), alpha-phellandrene (9.6 %) as major compounds. The majority of chemical constituents present in the essential oil ofP. angelicoideshave not been earlier reported. Antioxidant activity of the hydroalcoholic extract ofP. angelicoidesexhibited high radical scavenging ability as compared to aqueous extract and essential oil. The essential oil fromP. angelicoidesroots identified various important compounds that could serve their role in aromatherapy, nutrition, and pharmaceutical industries. The roots of the plant showed potential antioxidant activity and could be used as a nutritional supplement.

Objective: In this study, Myrica esculenta (ME) leaves extract along with Coenzyme Q10 was entrapped in nanostructured lipid carriers (NLCs). The formulation variables were successfully optimized using 23 factorial design.Methods: Preparation of NLC was carried out by solvent injection technique. The formulation of NLC was consisting of the methanolic extract of Myrica esculenta leaves and Coenzyme Q10 as key ingredients. Oleic Acid (OA) was taken as liquid lipid, Precirol ATO 5 (PATO) as solid lipid, and Poloxamer 407 (P407). The formulation variables were statically optimized using 23 factorial design, followed by the characterization of the formulation.Results: The results demonstrated that the best optimized NLC formulation F5 of Coenzyme Q10 and plant extract exhibited the smallest size 169.46 nm and highest entrapment efficiency 90.06±0.171 %. Furthermore, it showed good physical stability at 28 d after preparation.Conclusion: The developed NLCs of Q10-ME extract from this study could be explored as the effective anti-ageing formulation.