Al Mustansiriyah Journal of Pharmaceutical Sciences

Influenza is an infectious respiratory disease caused by the influenza virus and is a significant global public health concern. This infection displays a tendency for recurring outbreaks during specific seasons and occasional epidemics. A number of drugs and vaccines have been approved to treat this infection. Oseltamivir is an FDA-Approved anti-influenza drug acts by inhibiting influenza Neuramidase enzyme and used as therapeutic management and prophylaxis of influenza types A and B and by this way preventing virus budding and release and mitigating the intensity and duration of influenza infection. Oseltamivir is administered as a prodrug in the form of an ethyl ester and in the body hepatic esterases convert it to the active oseltamivir carboxylate. An approach of synthesizing Oseltamivir carboxamides with certain amino acids (series one) and Oseltamivir-amino acid-Hydroxamic acid conjugates, as hybrid molecules (series two) are considered and these may enhance efficacy, penetration into lung tissues, and manage resistance of Oseltamivir. These two series were subjected to molecular docking using GOLD Suite (version 5.7.1) on Neuramidase. These hybrids have recorded slightly higher PLP fitness, binding affinities represented as docking scores (59.14-72.23 Kcal/mol) based on the lowest docking scores on the target enzyme compared to Oseltamivir acid (56.24 Kcal/mol).

Econazole nitrate, a chemically produced triazole drug, is utilized to manage fungal keratitis. It has potent antifungal properties against many species; the readily available formula exhibits inadequate corneal permeability, visual aberrations, excessive tearing, dilution of tears, and leakage via the nasolacrimal duct.

This research aimed to study the effect of polyvinyl alcohol concentration on the properties of econazole nitrate polymeric micelles eye drops. Polymeric micelles loaded with econazole nitrate eye drops were prepared with different polyvinyl alcohol concentrations and evaluated for particle size, polydispersity index, zeta potential, and drug content. Formulations evaluated for ex vivo drug permeation using Franz diffusion cell. The cumulative drug permeation (CDP) percentage of the optimum formulation exhibits a significant variation of 64.4 % which has 2% of PVA as compared to econazole nitrate pure drug suspension 12.69% CDP. The cumulative drug permeation (CDP) percentage of the optimum formulation F3D demonstrated a 5-fold increase in ex vivo permeability through the goat ocular membrane compared to the econazole nitrate suspension may be attributed to the PVA use as a thickening agent. Using econazole nitrate polymeric micelle as eye drop containing 2% PVA led to system that is efficient and superior in overcoming ocular obstacles and facilitating the appropriate administration of lipophilic medicines by increasing contact time at the ocular surface and improving bioavailability.

Doxorubicin is an effective broad-spectrum anticancer drug; however, hepatotoxicity limits its clinical usage. Erythropoietin, a glycoprotein hormone primarily recognized for its crucial function in promoting erythropoiesis. Recently, it has been shown that it possesses significant cytoprotective effects in several organs, including the liver, heart, and brain.

The objective of this study was to assess the hepatoprotective properties of erythropoietin in the context of doxorubicin-induced liver injury.

Thirty-six male Wistar rats were separated into six groups: a negative control group and an induction group administered with doxorubicin. Additionally, there were three groups that received pretreatment with erythropoietin at three different doses (1000, 3000, and 6000 IU/kg), and a group that received conventional treatment and was pretreated with silymarin (100mg/kg). Liver samples were then collected on day 9 of the experiment from each group for histopathological examination.

Results showed that the induction group, treated with doxorubicin, revealed signs of doxorubicin-induced hepatotoxicity that include hepatocellular necrosis, severe zonal hepatic degeneration, congestion, and inflammation. On the other side, groups pre-treated with erythropoietin in all three doses revealed pronounced improvement in liver morphology especially at the higher doses used. In conclusion, erythropoietin pre-treatment can mitigate the hepatotoxicity induced by doxorubicin in a manner that is dependent on the dose, and it was more effective than the conventional therapy silymarin especially at the highest dose used.

Liver injury can arise post-exposure to drugs or their metabolites, as well as herbal and dietary supplements. Tamoxifen is a frequently used drug in breast cancer treatment. Unfortunately, Epidemiological studies have identified that Long-term tamoxifen treatment has been associated with the development of hepatotoxicity so it was used in this study to induce liver damage. Oxidative stress was the major implicated mechanism contributing to tamoxifen hepatotoxicity. Nebivolol is a third-generation selective beta1-adrenergic receptor blocker with vasodilator characteristics with significant antioxidant activity.

The presented study was conducted to investigate the possible protective role of nebivolol against rat hepatotoxicity induced by tamoxifen. Rats utilized in this study were randomized into five groups (6 in each group); Group 1- (Control) rats received distilled water (5mL/kg body weight orally) for 14 consecutive days. Group 2- Rats received distilled water for 12 consecutive days and tamoxifen (75mg/kg b.w., orally) on days 13 and 14 only. Group 3- Rats received Nebivolol (5 mg/kg b.w., orally for 14 consecutive days) and tamoxifen (75mg/kg b.w., orally) only on days 13 and 14. Group 4- Rats received Nebivolol (8 mg/kg b.w., orally for 14 consecutive days) and tamoxifen (75mg/kg b.w., orally) only on days 13 and 14. Group 5- Rats received Nebivolol (10 mg/kg b.w., orally for 14 consecutive days) and tamoxifen (75mg/kg b.w., orally) on days 13 and 14 only. The current study concluded that pre-administration of nebivolol with tamoxifen showed significant upregulation (P<0.05) in glutathione peroxidase (GPx) and significant downregulation (p<0.05) in malondialdehyde (MDA) each compared to corresponding levels in the tamoxifen-only treated group. In conclusion, this study demonstrated that pre-administration of nebivolol with tamoxifen attenuated its hepatotoxicity considering that nebivolol is a good choice, particularly for patients with hypertension requiring beta blockers and at risk for liver damage.

Vancomycin is a glycopeptide antibiotic used to treat anaerobic and aerobic gram-positive bacteria, for example, methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis. Vancomycin had some side effects, such as nephrotoxicity, ototoxicity, hypersensitivity reactions, and more. The present study aimed to evaluate the potential apoptotic effect of vancomycin on renal tissue and also evaluate the reno-protective effects of sulbutiamine, thiamine, riboflavin, and their combinations through inhibiting apoptosis.

Forty-two male rats were employed in this study, divided randomly into seven groups: the first group was the control group, the second group (the vancomycin group received 200 mg/ml twice daily) from the 15th-21st day of the study, and the other three groups were pretreated with sulbutiamine (50 mg/kg, orally once daily), thiamine (100 mg/kg, orally once daily), and riboflavin (100 mg/kg, orally once daily), respectively, for 21 days of the study. The sixth group was a combination group that received a mix of sulbutiamine and riboflavin, and the seventh group received a mix of thiamine and riboflavin for 21 days. The last five groups received vancomycin 200 mg/ml twice daily from the 15th-21st day of the study. The result of this study showed a significant increase p<0.05 in caspase-3, caspase-9, and NGAL in the induction group, while in the other group that was pretreated with sulbutiamine, thiamine, riboflavin, and their combinations, the mean tissue CASP-3, CASP-9, and concentration were significantly decreased. We concluded that the sulbutiamine, thiamine, and riboflavin-treated groups showed a significant decrease in caspase 3, caspase 9, and NGAL levels compared to the vancomycin-treated group. The combination group (sulbutiamine and riboflavin) showed the most significant decrease in mean tissue concentrations of CASP3, CASP9, and NGAL due to the additive effects of both treatments.

Bioactive compounds known as nutraceuticals have a significant impact in human well-being. Recently, there has been a significant understanding of the numerous health-promoting properties and exceptional nutritional value of mushrooms. Macrofungi have been considered functional in treating several health issues such as tumor, hypertension, owing to their rich composition of primary and secondary metabolites.

This review explores the nutraceutical capabilities of Macrofungi, particularly focusing on their polysaccharides, which showcase a variety of properties such as anticancer, antibacterial, antidiabetic, and immunostimulatory effects. The potential of medicinal mushrooms is discussed, with an acknowledgment of the significant drawback of their taste. It is emphasized that claims about their benefits need robust support from scientific studies to uphold trust and confidence. Further scientific investigation is crucial to assess the efficacy of nutraceuticals sourced from macrofungi, while also tackling prevailing apprehensions regarding the inadequacy of quality assurance protocols within this domain

Nanoemulsions (NEs) are colloidal dispersion systems made of two immiscible liquids combined with co-surfactants and surfactants (emulsifying agents), to form a thermodynamically stable. Numerous synthetic and natural compounds with the aim of enhancing bioactivity, delivery, and stability have been developed utilizing these delivery systems. This review focuses on the use of surface active agents (SAAs) in the formulation of NE in different drug delivery systems including intranasal, ophthalmic, buccal, dermal and vaginal, including how the type and concentration of SAAs influence the drug delivery system that is used for the NE and the type of NE that is formed (w/o or o/w).

This work intended to evaluate the dissolution of poor water soluble weakly basic drug like carvedilol (Carv) via two methods used to study and assess the effect of pH changes from the stomach to the small intestine on the drug dissolution and precipitation (ppt): dumping and transfer. Three approaches were used to increase solubility and decrease the precipitation of carvedilol; first, the acid modification principle was by incorporating Carv with fumaric acids (FA) to keep the drug at a low pH in the intestine. The second approach was solvent evaporation, which converted the drug from a low soluble crystalline form to a highly soluble amorphous form, and the last approach was forming a slow-release floating dosage form. The prepared samples were investigated by FESEM and FTIR. There is a slight shift in the peaks related to the hydroxyl group in approaches (acid modification and solvent evaporation) compared to the peak’s position in the Carv spectrograms, and the FESEM shows a decrease in particle sizes of prepared samples. The Carv prepared samples in vitro dissolution of dumping, and the transfer showed different in vitro dissolution profiles with enhanced dissolution profiles and lower ppt amount. The amorphization technique’s ppt was highly decreased in both dissolution dumping and transfer methods compared to the in vitro dissolution of the control of Carv.

Betaferon or interferon beta-1b (INFβ-1b) is a drug that used for multiple sclerosis (MS) treatment, this drug demonstrated an efficacy in relapse MS, but it can cause hepatotoxicity or liver injury, which present as brief elevations in liver aminotransferase enzymes. Quercetin which acts as antioxidant, anti-apoptotic and anti-inflammatory was used as a hepatoprotective in the current study.

This study aimed to investigate the histopathological changes of the liver tissue by betaferon and study the effect of different doses of quercetin on the liver pathological changes.

Methodology: (36) male rats were divided into 6 groups include the negative control group (given only normal saline i.p), betaferon or induction group (given only betaferon 250µg/kg i.p), treatment groups (quercetin 25,50,100 mg/kg + betaferon 250µg/kg) and silymarin group (silymarin 100 mg/kg i.p). In the current study, liver histopathological changes were examined by Hematoxylin and Eosin staining.

Results: In the control group the histological appearance of the liver showed normal tissues (no histopathological changes). Betaferon group the histopathological appearance of the liver showed sever hepatitis with multiple focal necrosis, sever dilation of central vein and marked cellular swelling (Ballooning cells) of hepatocytes. Histopathological examination of the groups pretreated with different doses of quercetin reflected dose-dependent hepatoprotective effects. Pretreatment with (25mg/kg) quercetin mildly improved the histopathological appearance of the liver. When the dose was increased to (50mg/kg), the score improved additionally, with the hepatic injury resolving at (100 mg/kg) of quercetin pretreatment as in silymarin group. Conclusions: Quercetin can improve histopathological changes on the tissue of the liver of male rats indicates that it possesses advantageous properties in reducing the histopathological damage induced by betaferon.

Polyelectrolyte complexes (PECs) are class of macromolecule compound formed by electrostatic interaction of oppositely charged polymers. The main objective of this review is to show the formation mechanism of PECs and their characterization, factors affecting their formation,

their pharmaceutical application in drug delivery system with some of the dosage form that utilize PEC technique in their formulation, also this review talks about the most common polymers used in the preparation of PECs.