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Thymoquinone (TQ), which is one of the main bioactive constituents of Nigella sativa seeds, has demonstrated its potential against various cancer models. The poor solubility of TQ in aqueous solution limits its uses in clinical application. The present study aimed to develop a novel formulation of TQ to increase its bioavailability and therapeutic potential with minimal toxicity. Polyethylene glycol (PEG)-coated DSPC/cholesterol comprising TQ liposomes (PEG-Lip-TQ) were prepared and characterized on various aspects. A computational investigation using molecular docking was used to assess the possible binding interactions of TQ with 12 prospective anticancer drug targets. The in vitro anticancer activity was assessed in A549 and H460 lung cancer cells in a time- and dose-dependent manner, while the oral acute toxicity assay was evaluated in silico as well as in vivo in mice. TQ docked to the Hsp90 target had the lowest binding energy of −6.05 kcal/mol, whereas caspase 3 was recognized as the least likely target for TQ with a binding energy of −1.19 kcal/mol. The results showed 96% EE with 120 nm size, and −10.85 mv, ζ-potential of PEG-Lip-TQ, respectively. The cell cytotoxicity data demonstrated high sensitivity of PEG-Lip-TQ and a several fold decrease in the IC50 while comparing free TQ. The cell cycle analysis showed changes in the distribution of cells with doses. The in vivo data revealed an ~9-fold increase in the LD50 of PEG-Lip-TQ on free TQ as an estimated 775 and 89.5 mg/kg b.w, respectively. This study indicates that the pharmacological and efficacy profile of PEG-lip-TQ is superior to free TQ, which will pave the way for an exploration of the effect of TQ formulation in the treatment of lung cancer in clinical settings.

Purpose Thymoquinone (TQ), a phytoconstituent of Nigella sativa seeds, has been studied extensively in various cancer models. However, TQ’s limited water solubility restricts its therapeutic applicability. Our work aims to prepare the novel formulation of TQ and assess its chemopreventive potential in chemically induced lung cancer animal model. Methods The polyethylene glycol coated DOPE/CHEMS incorporating TQ-loaded pH-sensitive liposomes (TQPSL) were prepared and characterized. Mice were exposed to benzo[ a ]pyrene (BaP) thrice a week for 4 weeks to induce lung cancer. TQPSL was administered three times a week for 21 weeks, starting 2 weeks before the first dose of BaP. Results The prepared TQPSL revealed 85% entrapment efficiency with 128 nm size and −19.5 mv ζ-potential showing high stability of the formulation. The pretreatment of TQPSL showed the recovery in BaP-modulated relative organ weight of lungs, cancer marker enzymes, and antioxidant enzymes in the serum. The histopathological analysis of the tissues showed that TQPSL protected the malignancy in the lungs. The flow cytometry data revealed the induction of apoptosis and decreased intracellular ROS by TQPSL. Molecular docking was performed to predict the TQ’s affinity for eight possible anticancer drug targets linked to lung cancer etiology. The data assisted to identify the serine/threonine-protein kinase BRAF as the most suitable target of TQ with binding energy −6.8 kcal/mol. Conclusion The current findings demonstrated the potential of TQPSL and its possible therapeutic targets of lung cancer. To our knowledge, this is the first research to outline the development of TQ formulation against lung cancer considering its low solubility as well as pulmonary delivery challenges.

The aim of the present study was to assess the short-term effects of Thymoquinone (TQ) on oxidative stress, glycaemic control, and renal functions in diabetic rats. DM was induced in groups II and III with a single dose of streptozotocin (STZ), while group I received no medication (control). The rats in groups I and II were then given distilled water, while the rats in group III were given TQ at a dose of 50 mg/kg body weight/day for 4 weeks. Lipid peroxidase, nitric oxide (NO), total antioxidant capacity (TAC), glycated haemoglobin (HbA1c), lipid profiles, and renal function were assessed. Moreover, the renal tissues were used for histopathological examination. STZ increased the levels of HbA1c, lipid peroxidase, NO, and creatinine in STZ-induced diabetic rats in comparison to control rats. TAC was lower in STZ-induced diabetic rats than in the control group. Furthermore, rats treated with TQ exhibited significantly lower levels of HbA1c, lipid peroxidase, and NO than did untreated diabetic rats. TAC was higher in diabetic rats treated with TQ than in untreated diabetic rats. The histopathological results showed that treatment with TQ greatly attenuated the effect of STZ-induced diabetic nephropathy. TQ effectively adjusts glycaemic control and reduces oxidative stress in STZ-induced diabetic rats without significant damaging effects on the renal function.

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory in eczema and contact dermatitis. The anti-inflammatory effect of a γ-lactone (5-hexyl-3H-furan-2-one) isolated from ostrich oil and its formulated nano-emulsion in formalin-induced paw edema was investigated in this study. Ostrich oil was saponified using a standard procedure; the aqueous residue was fractionated, purified, and characterized as γ-lactone (5-hexyl-3H-furan-2-one) through the interpretation of IR, NMR, and MS analyses. The γ-lactone was formulated as nano-emulsion using methylcellulose (MC) for oral solubilized form. The γ-lactone methylcellulose nanoparticles (γ-lactone-MC-NPs) were characterized for their size, shape, and encapsulation efficiency with a uniform size of 300 nm and 59.9% drug content. The γ-lactone was applied topically, while the formulated nanoparticles (NPs) were administered orally to rats. A non-steroidal anti-inflammatory drug (diclofenac gel) was used as a reference drug for topical use and ibuprofen suspension for oral administration. Edema was measured using the plethysmograph method. Both γ-lactone and γ-lactone-MC-NPs showed reduction of formalin-induced paw edema in rats and proved to be better than the reference drugs; diclofenac gel and ibuprofen emulsion. Histological examination of the skin tissue revealed increased skin thickness with subepidermal edema and mixed inflammatory cellular infiltration, which were significantly reduced by the γ-lactone compared to the positive control (p-value = 0.00013). Diuretic and toxicity studies of oral γ-lactone-MC-NPs were performed. No diuretic activity was observed. However, lethargy, drowsiness, and refusal to feeding observed may limit its oral administration.

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Objectives: Urinary tract infection (UTI) is one of the diseases with a highest prevalence in the world. This study evaluated the antibiotics resistant and the prescription pattern for UTI with the aim to participate as an effective monitoring study that enhances rational antibiotics’ prescription. Methods: We conducted a retrospective cross-sectional study at King Fahad Specialist Hospital from May 2018 to January 2019. We included a total of 306 patients with UTI. 204 patients diagnosed clinically and empirically treated (Group A), 102 patients underwent urine for culture and sensitivity tests (Group B). Results: UTI showed higher occurrence in female in both Groups A (61%) and B (65%). The mean age was higher in Group B (55.8 years) than Group A (39.44 years). The most commonly prescribed antibiotics for UTI were Trimethoprim + Sulfamethoxazole (TMP+SMX) (56%) and ciprofloxacin (15%). Escherichia coli was the most commonly isolated organism (36.3%) followed by Klebsiella pneumonia (30%). Although 41.17% of organisms were sensitive to TMP+SMX, 38.2% were resistant to it. The organisms were sensitive to amikacin in 80.4% and to gentamicin in 61.8% whereas, 61.8% were resistant to ampicillin. Luckily, no resistance was reported neither for nitrofurantoin nor for vancomycin. Conclusion: The study showed significant resistance to the commonly prescribed TMP+SMX and ciprofloxacin compared to absolute sensitivity to the less prescribed nitrofurantoin. This necessitates special consideration for local susceptibility in empirical therapy.

Background: Parent’s misconception of fever, result in increased anxiety and antipyretics are commonly used in this situation. So any lack of parent’s knowledge regarding strategies of using them raises the possibility of drug-related problems. Objective: This study evaluated the parents’ knowledge, attitude and beliefs in dealing with the children’s fever. Methods: An ethically approved cross-sectional study was conducted in Qassim region -Saudi Arabia. Results: A total of 490 parents were participated in this study, 83.7% of them were mothers. Half of parents use the armpit site for measuring temperature. The majority of parents considered the temperature ≤37°C as normal and more than half of them considered ≥38°C as fever temperature. Convulsion was believed to be a complication of fever in 71% of parents and there was a significant association between the number of children and the practice of giving antipyretics. A wrong practice of assessing fever was using hand touch, and this study revealed that this behavioral was presented in a nearly third of parents. Acetaminophen was the commonly used antipyretics beside ice packs as a common non pharmacological therapy. The study also showed the majority of parents didn’t know the importance of weight in considering antipyretic. Conclusion: Over all, parents participated in this study have inadequate knowledge about fever, its assessment and decision of giving a medication. However, past experiences and the number of sibling highly influence their practice and knowledge. Therefore, there is a need of effort to maximize parents’ information and awareness about fever.