Preparation and Characterization of Benzathine Penicillin G Solid Dispersions Using Different Hydrophilic Carriers

Several technical factors related to penicillin G intramuscular injection can affect its bioavailability and hence reduce the efficacy of rheumatic fever prevention program. When small amount of diluent is used, the powder is not completely dissolved and the thick suspension frequently causes obstruction of injection needle. The study aimed to characterize the solid-state properties of solid dispersion systems of benzathine penicillin G (BPG) prepared with hydrophilic carriers by applying solvent evaporation method. The results of spectroscopic studies; Fourier transform-infra red (FTIR), Nuclear Magnetic Spectroscopy (1HNMR) and Differential Scanning Calorimetry (DSC) revealed no chemical interaction between the drug and carriers. No significant changes in drug crystalline state were observed by X-ray diffraction and Scanning Electron Microscope (SEM) studies, even with using amorphous carriers; polyvinyl pyrrolidone (PVP-K30) and hydroxypropyl methylcellulose (HPMC). All the prepared solid dispersions demonstrated 76-93% yield and % drug content dependent on the polymer type and concentration. The hydrophilic polymers demonstrated potential effect on improving the flowability, wettability and dissolution characters of the drug. The results revealed that it is possible to enhance the dissolution rate of BPG (hydrophobic drug) by increasing the surface area of the drug adsorbed on the surface of hydrophilic polymer by solid dispersion method. Finally, solid dispersion BPG: PEG 4000 at ratio 50:50 gave uniform flowability of the powder (around 30), wettability (12 min) and faster dissolution rates among all the formulations. Thus, it was selected as the best formulation in this study

Preparation and Characterization of Benzathine Penicillin G Solid Dispersions Using Different Hydrophilic Carriers

Several technical factors related to penicillin G intramuscular injection can affect its bioavailability and hence reduce the efficacy of rheumatic fever prevention program. When small amount of diluent is used, the powder is not completely dissolved and the thick suspension frequently causes obstruction of injection needle. The study aimed to characterize the solid-state properties of solid dispersion systems of benzathine penicillin G (BPG) prepared with hydrophilic carriers by applying solvent evaporation method. The results of spectroscopic studies; Fourier transform-infra red (FTIR), Nuclear Magnetic Spectroscopy (1HNMR) and Differential Scanning Calorimetry (DSC) revealed no chemical interaction between the drug and carriers. No significant changes in drug crystalline state were observed by X-ray diffraction and Scanning Electron Microscope (SEM) studies, even with using amorphous carriers; polyvinyl pyrrolidone (PVP-K30) and hydroxypropyl methylcellulose (HPMC). All the prepared solid dispersions demonstrated 76-93% yield and % drug content dependent on the polymer type and concentration. The hydrophilic polymers demonstrated potential effect on improving the flowability, wettability and dissolution characters of the drug. The results revealed that it is possible to enhance the dissolution rate of BPG (hydrophobic drug) by increasing the surface area of the drug adsorbed on the surface of hydrophilic polymer by solid dispersion method. Finally, solid dispersion BPG: PEG 4000 at ratio 50:50 gave uniform flowability of the powder (around 30), wettability (12 min) and faster dissolution rates among all the formulations. Thus, it was selected as the best formulation in this study

Cytotoxic properties of some herbal plants in Oman

AbstractOrganic extracts from five medicinal plants collected in Oman were assayed for in vitro cytotoxic property. Dried samples from latex, leaves, roots and stem bark of these species were macerated in ethanol to give crude extracts which were Kupchan's partitioned into hexane, chloroform and ethyl acetate fractions. Six different concentrations of each fraction were subjected to brine shrimp test to determine their lethality values. Percent mortalities from each fraction were then converted to LC50 values by Finney probit analysis. Chloroform and ethyl acetate extracts from Calotropis procera latex and aerial part of Rhazya stricta were the most active. LC50 values for C. procera latex were 3.0 and 8.2μg/ml, respectively, while that of R. stricta were 18.1 and 13.9μg/ml, respectively. C. procera and R. stricta growing in Oman are good sources of cytotoxic compounds

Evaluation of Antiproliferative, Antimicrobial, Antioxidant, Antidiabetic and Phytochemical Analysis of Anogeissus dhofarica A. J. Scott

In the current study, methanol (ADAM) extracts and their fractions, including chloroform (ADAC), ethyl acetate (ADAE), n-hexane (ADAH), and aqueous (ADAA) fractions, were prepared from aerial parts of Anogeissus dhofarica and evaluated for phytochemical assessment, high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) analysis, and in vitro bioassays. The qualitative analysis determined that, except alkaloids, all the representative groups were found to be present in the analyzed samples. Samples under quantitative study displayed the highest amount of total phenolic contents in the ADAE fraction, while total flavonoid contents were highest in the ADAM extract. The ADAM extract was subjected to HR-ESI-MS to identify the chemical constituents that presented twenty-two bioactive ingredients, outlined for the first time from A. dhofarica, mainly contributed by sub-class flavanones. In the case of antimicrobial activity, the ADAE extract revealed an effective zone of inhibition (ZOI) against the Gram-positive bacterial strain (Staphylococcus aureus) with an MIC value of 0.78 ± 0.3 mg/mL, while the ADAA extract exhibited higher ZOI (34 ± 0.12 mm) against the fungal strain Candida kruzei with an MIC of 0.78 mg/mL. In the DPPH (2,2-diphenyl-1-picrylhydrazyl) analysis, the ADAE extract exhibited a maximum scavenging potential with an IC50 of 9.8 ± 1.2 μg/mL, succeeded by the ADAM extract with an IC50 of 17.4 ± 0.4 μg/mL free radical scavenging capability. In the antidiabetic assessment, the ADAE extract was the most effective, with an IC50 of 6.40 ± 0.1 μg/mL, while the same extract demonstrated prominent activity with 30.8% viability and an IC50 of 6.2 ± 0.3 μg/mL against breast cancer cell lines. The brine shrimp lethality assay demonstrated a correlation with the in vitro cytotoxicity assay, showing the ADAE extract as the most active, with a 70% mortality rate and an LC50 of 300.1 μg/mL. In conclusion, all the tested samples, especially the ADAE and ADAM extracts, have significant capabilities for the investigated activities that could be due to the presence of the bioactive compounds

Evaluation of Antiproliferative, Antimicrobial, Antioxidant, Antidiabetic and Phytochemical Analysis of <i>Anogeissus dhofarica</i> A. J. Scott

In the current study, methanol (ADAM) extracts and their fractions, including chloroform (ADAC), ethyl acetate (ADAE), n-hexane (ADAH), and aqueous (ADAA) fractions, were prepared from aerial parts of Anogeissus dhofarica and evaluated for phytochemical assessment, high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) analysis, and in vitro bioassays. The qualitative analysis determined that, except alkaloids, all the representative groups were found to be present in the analyzed samples. Samples under quantitative study displayed the highest amount of total phenolic contents in the ADAE fraction, while total flavonoid contents were highest in the ADAM extract. The ADAM extract was subjected to HR-ESI-MS to identify the chemical constituents that presented twenty-two bioactive ingredients, outlined for the first time from A. dhofarica, mainly contributed by sub-class flavanones. In the case of antimicrobial activity, the ADAE extract revealed an effective zone of inhibition (ZOI) against the Gram-positive bacterial strain (Staphylococcus aureus) with an MIC value of 0.78 ± 0.3 mg/mL, while the ADAA extract exhibited higher ZOI (34 ± 0.12 mm) against the fungal strain Candida kruzei with an MIC of 0.78 mg/mL. In the DPPH (2,2-diphenyl-1-picrylhydrazyl) analysis, the ADAE extract exhibited a maximum scavenging potential with an IC50 of 9.8 ± 1.2 μg/mL, succeeded by the ADAM extract with an IC50 of 17.4 ± 0.4 μg/mL free radical scavenging capability. In the antidiabetic assessment, the ADAE extract was the most effective, with an IC50 of 6.40 ± 0.1 μg/mL, while the same extract demonstrated prominent activity with 30.8% viability and an IC50 of 6.2 ± 0.3 μg/mL against breast cancer cell lines. The brine shrimp lethality assay demonstrated a correlation with the in vitro cytotoxicity assay, showing the ADAE extract as the most active, with a 70% mortality rate and an LC50 of 300.1 μg/mL. In conclusion, all the tested samples, especially the ADAE and ADAM extracts, have significant capabilities for the investigated activities that could be due to the presence of the bioactive compounds