Eugenol is a bioactive compound widely available in many herbs like clove, cinnamon, tulsi, pepper etc. The compound is known for its antioxidant, antimicrobial, anesthetic, anti-inflammatory, neuroprotective, anti-diabetic, and anti-cancer activities. In pharmaceutical analysis, eugenol is used as a marker for single drugs and drug products. Dental care, household, and personal hygiene products are other areas where it has established its potential. In the food industry, eugenol is used as a flavouring agent in non-alcoholic beverages, baked foods, and chewing gums. Considering the huge potential of eugenol, this review is an attempt to collate the regulatory information, physico-chemical properties, toxicity profile, marketed conventional and novel formulations, analytical methods, extraction procedures, recent patents and clinical trials of the moiety. Based on literature survey a schematic diagram of mechanism of action has also been made.
30 August 2018 in Organic & Medicinal Chemistry International Journal
Organic and Medicinal chemistry international Journal is an open access journal that is committed to publish the papers on various topics of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties For any analytical method development and validation, it is require developing arobust, accurate, precise, and linear method which is the heart for the development activities for drug product and drug substances. It is vital importance to initiate through a systematic process that the analytical method under question is acceptable for its intended purpose. Determining the limit of what and require for the quantitative determination is according of regulatory authorities globally..
The aim of the current study was to develop the phytosomal gel of aloe vera extract for improved topical delivery. Aloe vera extract loaded phytosomal system was developed by fixing the amount of aloe vera extract and ethanol and by varying the concentration of lecithin (0.15–0.25% w/v) and speed of rotation (80–120 rpm). Different formulation batches were prepared as per the Design expert software. A 22 Factorial design was applied to optimize the formulation on the basis of vesicular size and entrapment efficiency. Developed formulations were evaluated for vesicular size, entrapment efficiency, PDI, zeta potential and in-vitro release. Further stability studies were also performed. For the optimized formulation (F09), vesicular size, entrapment efficiency and PDI were found as 123.1 ± 1.44 nm, 95.67 ± 0.27% and 0.98 ± 0.06. Zeta potential of −11.9 mV and drug release of 56.91 ± 4.1% obtained in 24 h. Drug release kinetics from the phytosomes follows Higuchi model. TEM micrograph confirms the uniform structure of phytosomes. Phytosomal gel of optimized phytosomal formulation (F09) was developed with 1% Carbopol 934 and physically characterized on the basis of pH, viscosity, homogeneity and drug content. Ex-vivo permeation study showed the better permeation and flux profile of phytosomal gel with the conventional aloe vera extract gel. Also, studies on phytosomal formulation and gel showed stability up-to 3 months. Thus overall, it can be concluded that the phytosomal gel is a good carrier for topical delivery of herbal extract such as aloe vera.
Thymoquinone (THY) is a bioactive compound present in the seed powder of Nigella sativa (NS). This research aims to precisely and accurately estimate THY using high-performance liquid chromatography (HPLC) with a Quality by Design (QbD) application. Box-Behnken design (BBD) was employed to optimize the chromatographic conditions for HPLC method development, taking mobile phase flow rate, pH of the buffer, and λmax as independent variables and retention time and tailing factor as the measured responses. The mobile phase composition was methanol: acetonitrile: buffer (2.2 mM ammonium formate) at the ratio of 35:50:15 v/v/v on a Symmetry® C18 (5 μm, 3.9 × 150 mm) column. In isocratic mode, it had a flow rate 0.9 mL min−1 and eluted analyte was detected at 249 nm. Validation parameters followed the International Council for Harmonization (ICH) guidelines for the new HPLC method. The method was linear over the range 6.25–100 µg mL−1 with a coefficient of determination (r2) of 0.9957. The limit of detection (LOD) and limit of quantification (LOQ) were 2.05 and 6.25 µg mL−1, respectively. The %RSD of system suitability for retention time was 1.42% and for the tailing factor it was 0.695%. In addition, the developed method was precise, accurate, and robust according to ICH criteria. The developed HPLC method is simple, accurate, quick, and robust, and it could be used for the routine analysis of THY in different kinds of formulations.
The objective of the current research is to develop ZnO-Manjistha extract (ZnO-MJE) nanoparticles (NPs) and to investigate their transdermal delivery as well as antimicrobial and antioxidant activity. The optimized formulation was further evaluated based on different parameters. The ZnO-MJE-NPs were prepared by mixing 10 mM ZnSO4·7H2O and 0.8% w/v NaOH in distilled water. To the above, a solution of 10 mL MJE (10 mg) in 50 mL of zinc sulfate was added. Box–Behnken design (Design-Expert software 12.0.1.0) was used for the optimization of ZnO-MJE-NP formulations. The ZnO-MJE-NPs were evaluated for their physicochemical characterization, in vitro release activity, ex vivo permeation across rat skin, antimicrobial activity using sterilized agar media, and antioxidant activity by the DPPH free radical method. The optimized ZnO-MJE-NP formulation (F13) showed a particle size of 257.1 ± 0.76 nm, PDI value of 0.289 ± 0.003, and entrapment efficiency of 79 ± 0.33%. Drug release kinetic models showed that the formulation followed the Korsmeyer–Peppas model with a drug release of 34.50 ± 2.56 at pH 7.4 in 24 h. In ex vivo studies ZnO-MJE-NPs-opt permeation was 63.26%. The antibacterial activity was found to be enhanced in ZnO-MJE-NPs-opt and antioxidant activity was found to be highest (93.14 ± 4.05%) at 100 µg/mL concentrations. The ZnO-MJE-NPs-opt formulation showed prolonged release of the MJE and intensified permeation. Moreover, the formulation was found to show significantly (p < 0.05) better antimicrobial and antioxidant activity as compared to conventional suspension formulations.
28 June 2021 in Journal of Dispersion Science and Technology
The objective of the current research to investigate the transdermal delivery of phytosomal Manjistha extract gel (MJE gel). The optimized formulation was prepared and evaluated for different parameters. MJE-loaded phytosomes were prepared by solvent evaporation method using rotary evaporator. The formulation was prepared with a variable concentration of lecithin (0.15–0.25% w/v), with stirring speed of the round bottom flask (80–160 rpm). Design expert software was used for the optimization of MJE-loaded phytosomal formulations. Central composite design-based factorial design was applied and evaluated for vesicular size and entrapment efficiency as dependent variables. The optimized formulation was further characterized with vesicle size, zeta potential, in vitro release. The Carbopol 934 was used to convert the phytosomal formulation (F10) into phytosomal gel and evaluated for ex vivo permeation to check the difference in permeation profile in compare to conventional MJE gel. The optimized MJE-loaded phytosomal formulation (F10) showed the vesicular size of 122.15 ± 3.73 nm, entrapment efficiency of 96.25 ± 2.45% with PDI value of 0.98 ± 0.06. Among the drug release kinetic models, the formulation followed the Higuchi model with drug release of 84.2 ± 4.1% in 12 h. Transmission electron micrograph showed the uniform structure and spherical shape. The prepared phytosomal gel shows prolonged release and enhanced permeation compared to conventional MJE gel. Graphical Abstract