, S. TAMIZHARASI, T. SIVAKUMAR Nandha College of Pharmacy and Research Institute, Erode 630052, Tamilnadu, IndiaEmail: sumoraji@gmail.comObjective: The objective of this study was to formulate and evaluate the poorly soluble drug, naringenin (NAR) into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspenion of naringenin (NARNS) was prepared using high-pressure homogenization method using Soya lecithin, Polaxamer-407, Polaxamer-188, Hydroxypropyl methyl cellulose (HPMC) and Tween-80. Ten formulations were prepared to show the effect of stabilizer and its ratio. D-α-Tocopheryl polyethene glycol succinate 1000 (TPGS) was added as a co-stabilizer. All these formulations were evaluated for their particle size, PDI, zeta potential, FT-IR study, drug content, saturation solubility studies, entrapment efficiency, in vitro permeability and in vitro drug release. The formulation was further evaluated for scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Powder X-ray diffraction (P-XRD) and hemocompatibility assessment.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation was found 1:1.5:1 (drug: stabilizer: co-stabilizer ratio). Dramatic effect of the particle size reduction was found by the addition of the co-stabilizer (TPGS) in formulation N2 that has P. S 80.52±0.13 nm. The solubility and dissolution of NAR in the form of NARNS were significantly higher than those of pure NAR. SEM report shows that naringenin nanosuspension revealed a smooth texture. P-XRD crystallography diffraction and DSC studies indicated that the crystalline state of NAR was converted into amorphous nature. The safety evaluation showed that NARNS provided a lower rate of erythrocyte hemolysis.Keywords: Naringenin, High-Pressure Homogenization, Nanosuspenion, Solubility, Bioavailability Conclusion:In this study, (NARNS) was successfully carried out by high-pressure homogenization technique and characterized. The physiochemical characterization shown that crystalline naringenin was converted to a polymorphic form (DSC and P-XRD Study) which evidenced by enhanced dissolution rate in comparisons of the formulation with (NAR) pure drug. The NARNS has shown 7.5±0.4 fold increased relative bioavailability when compared to the NAR. The increased drug dissolution rate may have a significant impact in absorption which in turn the improved oral bioavailability of naringenin. Thus, this delivery system may prefer to improve the dissolution of poorly soluble drugs like NAR and thus enhanced oral bioavailability. The safety evaluation showed that nanoformulation (NF2) shows a lower rate of erythrocyte hemolysis. These findings suggest that the selected formulation may represent a promising new drug formulation for intravenous administration in the treatment of certain cancers.

No abstract

No abstract

Naringenin is prominent citrus flavonoids that are found mostly in grapes and oranges. It has long been thought to be a helpful therapeutic agent, but its usage has been limited due to its poor water solubility and bioavailability. The goal of this study was to improve naringenin bioavailability and therapeutic efficacy utilization by innovative liposome formulations created using the thin lipid film technique using soya lecithin and cholesterol as surface modifiers. The liposome that was successfully formulated (F3) was spherical in shape, and had a regulated release profile in-vitro. The tiny particle size (100 nm), high encapsulation efficiency (>88%), and drug loading capacity (>94%) revealed that naringenin and the liposome core had a strong affinity. Release kinetics models such as zero order, first order, Higuchi, and Peppas are constantly used to predict drug release profiles in order to develop a better in vitro–in vivo association. The majority of these models rely on diffusion equations based on liposome composition and release conditions. The drug release from the formulation follows zero order kinetics, according to the correlation coefficient values (R2) derived from several models. When tested with the Korsmeyer-peppas model, all of the formulations were linear. The erosion and swelling of the polymer dominated the drug release. The release exponent in the Korsmeyer-peppas model suggests that the process win drug release is a case II super transport. Based on these observations, it was anticipated that liposomal formulations could be useful nanocarriers for bypassing the oral delivery constraint of hydrophobic substances

The present work demonstrates the influence of plant extract composition (antioxidant and total phenolic content) on the size and morphology of the produced AgNPs. In this study, silver nanoparticles (AgNPs) were synthesized using aqueous flower extract of Allamanda neriifolia plant. The biosynthetic procedure was rapid and simple and was easily monitored via colour changes and examined AgNPs (AN-AgNPs) by ultraviolet-visible spectroscopy, Fourier transform infrared (FTIR) spectroscopy and scanning electron microscope (SEM). The results obtained from various characterizations revealed that average size of synthesized AgNPs was 50 nm and in spherical structure. The anticancer potential of AN-AgNPs was investigated against human breast cancer cells (MCF-7). The cytotoxic response was assessed by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT), and morphological changes by apoptosis. The biosynthesized AgNPs-induced cell death in MCF- 7 cells suggested the anticancer potential of AN-AgNPs. Therefore, they may be used to treat the breast cancer cells.