Silver nanoparticles biogenically synthesised using Maclurodendron porteri extract and their bioactivities.

Silver nanoparticle is widely used in various field including medical, cosmetic, food and industrial purposes due to their unique properties in electrical conductivity, thermal, and biological activities. In the medical field, silver nanoparticles (AgNPs) have been reported to have strong antimicrobial and cytotoxic activities. This study aimed to synthesize and characterize silver nanoparticles (AgNPs) using Maclurodendron porteri (MP) extract and to evaluate the antimicrobial and cytotoxic activities of the synthesised MP-AgNPs. Green method of Ultrasound Assisted Extraction (UAE) was used to extract the leaves of M. porter. Liquid Chromatography -Mass Spectrometry/Quadrupole time-of-flight (LC-MS/QTOF) was used to identify the compounds in the leaf extract of M. porteri. Characterisation of the synthesised nanoparticles involved ultraviolet-visible (UV-Vis), Fourier Transform Infrared (FTIR), scanning electromagnetic microscopy (SEM), Zeta potential Analyzer and Particle Size Analyzer. The cytotoxic assay was conducted on MCF-7 and Caco-2 cell lines by MTT assay. Antimicrobial activity was tested on Gram-negative and Gram-positive bacteria using the disc diffusion method. Based on LC-MS/QTOF analysis, 430 compounds were found. The identified major compounds consist of amino acids, polyphenols, steroids, terpenoids and heterocyclic compounds which possibly act as reducing agents. 1 mM, 5 mM and 10 mM of silver nitrate solution were mixed with the leaf extract to form silver nanoparticles. 1.2 mg/ml of MP-AgNPs were found to have antibacterial activity against B. subtilis, S. aureus, E. coli, and P. aeruginosa with inhibitory zones of 8.0 ± 0.36 mm, 8.5 ± 0.45 mm, 7.5 ± 0.36 mm, and 9.0 ± 0.40 mm respectively. MP-AgNPs showed no cytotoxic activity against Caco-2 and MCF-7 cells. In conclusion, the presence of major amine compounds such as 10,11-dihydro-10,11-dihydroxyprotriptyline and harderoporphyrin in the extract facilitated the synthesis of AgNPs and the nanoparticle showed weak bioactivities in the assay conducted.

Effect of multicomponent crystal of piperine-nicotinic acid on antihyperlipidemic activity in rats.

The alkaloid piperine is the main bioactive compound in black pepper (Piper nigrum L) and exhibits antihyperlipidemic activity. Piperine is a Biopharmaceutical Classification System (BCS) Class II compound, which has low water solubility, resulting in low bioavailability. This study aims to examine the effects of multicomponent nicotinic acid-piperine crystals on antihyperlipidemic activity in rats fed a high-fat diet. To increase the effectiveness of piperine, we prepared multicomponent crystals by the solvent-drop grinding method, using nicotinic acid as a co-former. The antihyperlipidemic activity of the preparation was estimated by measuring total cholesterol (TC), total triglycerides (TG), low-density lipoprotein cholesterol (LDLc) and high-density lipoprotein cholesterol (HDLc), using the enzymatic colorimetric method. Rats fed a high-fat diet exhibited an increase in plasma lipid levels. However, rats administered the multicomponent piperine-nicotinic acid crystals at a dose of 40 mg/kg/BW showed significantly (p<0.050) reduced plasma lipid levels. Compared with hyperlipidemic rats, multicomponent crystals of piperine-nicotinic acid decreased TC from 237.8±8.02 mg/dL to 174.53±7.07mg/dL, TG levels from 208.33±5.79 to 85.95±7.41mg/dL and LDLc levels from 144.225±15.99 mg/dL to 88.55±10.83mg/dL but increased HDLc levels from 51.93±10.92mg/dL to 68.78±2.56 mg/dL. Thus, the results demonstrate that the multicomponent piperine-nicotinic acid crystals lowered TC, TG and LDLc but increased HDLc.

Simultaneous TLC-densitometric analysis of catechin, pyrocatechol and quercetine in gambir block from Pesisir Selatan.

The goal of this study is to use the TLC-densitometric method to determine the concentration of catechin, pyrocatechol, and quercetine in gambir block extracts in a reliable and efficient manner. The best eluent is a mixture of chloroform: ethyl acetate: glacial acetic acid (4:4:2). The concentration of catechin, pyrocatechol and quercetine in gambir block was found to be 25.50 ± 3.13, 0.91 ± 0.60 and 0.83 ± 0.34% (w/w) w/w respectively. The linearity was obtained between 750-2500, 50-350, and 50-350 µg/spot. 12.49-41.63, 0.48-1.60, 3,85-12.83 µg/spots were found to represent the LOD and LOQ, respectively. The proposed approach exhibited great sensitivity, precision, and accuracy, as well as strong linearity.

Multicomponent Crystal of Mefenamic Acid and N-Methyl-d-Glucamine: Crystal Structures and Dissolution Study.

A novel multicomponent crystal (MC) of mefenamic acid (MA) and N-methyl-d-glucamine (MG) had been prepared to improve the physicochemical properties of poorly soluble drugs, and was characterized for its physicochemical properties by powder X-ray diffraction analysis, differential scanning calorimetry thermal analysis, FT-IR spectroscopy, in vitro dissolution rate, and physical stability. In addition, the crystal structure was determined by single-crystal X-ray diffraction analysis. The differential scanning calorimetry thermogram of the MA-MG binary system exhibits a single and sharp endothermic peak at 151.20°C, which was attributed to the melting point of a MC of MA-MG. FT-IR spectroscopy analysis showed the occurrence of solid-state interaction by involving proton transfer between MA and MG. The crystal structure analysis confirmed that MA-MG formed 1:1 ratio salt type MC. The formation of a MC of MA with MG significantly improved the dissolution rate of MA in compared to intact MA, and also the crystal demonstrated a good stability under a high relative humidity. These good properties would be attributed to the layer structure of MA and MG in the crystal.

Effect of Irbesartan-Poloxamer-188 Solid Dispersion on Intercellular Cell Adhesion Molecule-1 and Interleukin-8 on Hypertension Rats.

BACKGROUND: Based on the Biopharmaceutics Classification System (BCS) system, irbesartan is a drug that belongs to the class II BCS group which has limitations in terms of dissolution rates with low bioavailability of 26% -60%. These limitations to bioavailability can be overcome by solid dispersion with hydrophilic matrices such as Poloxamer. Irbesartan is an angiotensin receptor blocker. At present, it is widely used in dealing with hypertension due to endothelial dysfunction. AIM: This study aims to determine endothelial function blood markers can be examined, such as adhesion molecules (ICAM-1) and IL-8 pro-inflammatory cytokines. MATERIAL AND METHODS: Research on the effects of irbesartan-poloxamer-188 solid dispersion on ICAM-1 and IL-8 in hypertensive rats has been carried out. The formation of solid dispersion through dissolution method while induction of hypertension using 2.5% NaCl and prednisone 1.5 mg/Kg BB orally in 3 treatment groups, irbesartan dose was 13.5 mg/kg. The parameters observed were serum ICAM-1 and IL-8 levels. RESULTS: The result showed that the solid dispersion of irbesartan-poloxamer-188 could reduce ICAM-1 and IL-8 levels in hypertensive rats which differed significantly from the positive control group (p < 0.05). CONCLUSION: This study concluded that the solid dispersion of irbesartan-poloxamer-188 effects and decreases ICAM-1 levels in the serum of hypertensive rats. Solid dispersion of irbesartan-poloxamer-188 can influence and reduce IL-8 in the serum of hypertensive rats.

Cocrystal of Ibuprofen⁻Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation.

Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phase of ibuprofen-nicotinamide, determine the solubility, and evaluate its in vivo analgesic activity. The cocrystal of ibuprofen-nicotinamide was prepared by a slow evaporation method. The solid-state characterization was conducted by powder X-ray diffraction (PXRD) analysis, differential thermal analysis (DTA), and scanning electron microscopy (SEM). To investigate the in vivo analgesic activity, 28 male Swiss-Webster mice were injected with acetic acid 0.5% following oral administration of intact ibuprofen, physical mixture, and its cocrystalline phase with nicotinamide (equivalent to 26 mg/kg ibuprofen). The number of writhes was counted, and pain inhibition was calculated. All data were analyzed with one-way ANOVA followed by Duncan's Multiple Range Test (95% confidence interval). The results revealed that a new cocrystalline phase was successfully formed. The solubility testing showed that the cocrystal formation enhanced the solubility significantly as compared with the physical mixture and intact ibuprofen. A significant increase in the analgesic activity of cocrystal ibuprofen-nicotinamide was also confirmed.

Influence of Milling Process on Efavirenz Solubility.

INTRODUCTION: The aim of this study was to investigate the influence of the milling process on the solubility of efavirenz. MATERIALS AND METHODS: Milling process was done using Nanomilling for 30, 60, and 180 min. Intact and milled efavirenz were characterized by powder X-ray diffraction, scanning electron microscopy (SEM), spectroscopy infrared (IR), differential scanning calorimetry (DSC), and solubility test. RESULTS: The X-ray diffractogram showed a decline on peak intensity of milled efavirenz compared to intact efavirenz. The SEM graph depicted the change from crystalline to amorphous habit after milling process. The IR spectrum showed there was no difference between intact and milled efavirenz. Thermal analysis which performed by DSC showed a reduction on endothermic peak after milling process which related to decreasing of crystallinity. Solubility test of intact and milled efavirenz was conducted in distilled water free CO2 with 0.25% sodium lauryl sulfate media and measured using high-performance liquid chromatography method with acetonitrile: distilled water (80:20) as mobile phases. The solubility was significantly increased (P < 0.05) after milling processes, which the intact efavirenz was 27.12 ± 2.05, while the milled efavirenz for 30, 60, and 180 min were 75.53 ± 1.59, 82.34 ± 1.23, and 104.75 ± 0.96 µg/mL, respectively. CONCLUSIONS: Based on the results, the solubility of efavirenz improved after milling process.

Crystal structure of olivetolic acid: a natural product from Cetrelia sanguinea (Schaer.).

The title compound, C12H16O4 (systematic name: 2,4-dihy-droxy-6-pentyl-benzoic acid) is a natural product isolated from C. sanguinea (Schaer.) and is reported to have various pharmacological activities. The mol-ecule is approximately planar (r.m.s. deviation for the non-H atoms = 0.096 Å) and features an intra-molecular O-H⋯O hydrogen bond. In the crystal, each olivetolic acid mol-ecule is connected to three neighbours via O-H⋯O hydrogen bonds, generating (10-1) sheets. This crystal is essentially isostructural with a related resorcinolic acid with a longer alkyl chain.

Preparation and characterization of solid dispersion freeze-dried efavirenz - polyvinylpyrrolidone K-30.

The aim of this research is to prepare and characterize solid dispersion of efavirenz - polyvinylpyrrolidone (PVP) K-30 by freeze drying to increase its solubility. Solid dispersion of efavirenz - PVP K-30 was prepared by solvent evaporation method with ratio 2:1, 1:1, and 1:2 and dried using a freeze dryer. Characterizations were done by scanning electron microscopy (SEM), powder X-ray diffraction analysis, differential thermal analysis (DTA), and Fourier transform infrared (FT-IR) spectroscopy. Solubility test was carried out in CO2-free distilled water, and efavirenz assay was conducted using high-performance liquid chromatography with acetonitrile:acetic acid (80:20) as the mobile phases. Powder X-ray diffractogram showed a decrease in the peak intensity, which indicated the crystalline altered to amorphous phase. DTA thermal analysis showed a decrease in the melting point of the solid dispersion compared to intact efavirenz. SEM results indicated the changes in the morphology of the crystal into an amorphous form compared to pure components. FT-IR spectroscopy analysis showed a shift wavenumber of the spectrum efavirenz and PVP K-30. The solubility of solid dispersion at ratio 2:1, 1:1, and 1:2 was 6.777 µg/mL, 6.936 µg/mL, and 14,672 µg/mL, respectively, whereas the solubility of intact efavirenz was 0.250 µg/mL. In conclusion, the solubility of solid dispersion increased significantly (P < 0.05).