Introduction: Epidermal growth factor receptor (EGFR) inhibition is an imperative therapeutic approach targeting various types of cancer including colorectal, lung, breast, and pancreatic cancer types. Moreover, cyclooxygenase-2 (COX-2) is frequently overexpressed in different types of cancers and has a role in the promotion of malignancy, apoptosis inhibition, and metastasis of tumor cells. Combination therapy has been emerged to improve the therapeutic benefit against cancer and curb intrinsic and acquired resistance. Methods: Three semi-synthetic series of compounds (C1-4, P1-4, and G1-4) were prepared and evaluated biologically as potential dual epidermal growth factor receptor (EGFR) and COX-2 inhibitors. The main phenolic constituents of Amaranthus spinosus L. (p-coumaric, caffeic and gallic) acids have been isolated and subsequently subjected to diazo coupling with various amines to get novel three chemical scaffolds with potential anticancer activities. Results: Compounds C4 and G4 showed superior inhibitory activity against EGFR (IC₅₀: 0.9 and 0.5 μM, respectively) and displayed good COX-2 inhibition (IC₅₀: 4.35 and 2.47 μM, respectively). Moreover, the final compounds were further evaluated for their cytotoxic activity against human colon cancer (HT-29), pancreatic cancer (PaCa-2), human malignant melanoma (A375), lung cancer (H-460), and pancreatic ductal cancer (Panc-1) cell lines. Interestingly, compounds C4 and G4 exhibited the highest cytotoxic activity with average IC₅₀ values of 1.5 μM and 2.8 μM against H-460 and Panc-1, respectively. The virtual docking study was conducted to gain proper understandings of the plausible-binding modes of target compounds within EGFR and COX-2 binding sites. Discussion: The NMR of prepared compounds showed characteristic peaks that confirmed the structure of the target compounds. The synthesized benzoxazolyl scaffold containing compounds showed inhibitory activities for both COXs and EGFR which are consistent with the virtual docking study.

Type 2 Diabetes mellitus is a major public health concern with an alarming global growth rate. According to the World Health Organization (WHO), Saudi Arabia ranks seventh in the world and second in the Middle East for the largest estimated burden of diabetic cases. Evidence shows that pharmacist-led care programs can be beneficial for the effective treatment of diabetes mellitus. Current study was aimed to evaluate the impact of Pharmacist-Based Diabetic Intervention (PDIM) for Type 2 Diabetes patients on knowledge of the disease, adherence to medications and self-care practices during the first wave of COVID-19. A multi-arm pre-post study was conducted among type 2 diabetic patients from April to October 2021 in Sakaka, Saudi Arabia. Patients were randomly divided into an intervention and a control group. The intervention group received the PDIM, whereas the control group only received the usual care. The pharmacist-based diabetes intervention model consisted of a diabetic educational module and medication improvement strategies. Furthermore, the intervention group also received specific telepharmacy services (calls, messages or emails) to address their medication-related problems, inquire about medication adherence and follow-up. At the end of six months, disease knowledge, self-care practices, and medication adherence score were analyzed. Furthermore, HbA1c and lipid profile were also compared. A total of 109 patients were included in the study. A significant difference was observed in the knowledge score between the intervention and control group (16.89 ± 2.01 versus 15.24 ± 2.03, p-value < 0.001). Similarly, self-care practices also improved in the intervention group as compared to the control group (4.39 ± 1.10 versus 3.16 ± 0.97, p-value < 0.001). Furthermore, the medication adherence and HbA1c significantly improved during between the group analysis (p < 0.05). Our study demonstrates that pharmacist-based diabetes intervention model is effective in improving patients’ knowledge of diabetes, self-care practices, medication adherence and glycemic control.

LC-MS-assisted metabolomic profiling of the Red Sea-derived brown algae Sargassum cinereum “Sargassaceae” dereplicated eleven compounds 1–11. Further phytochemical investigation afforded two new aryl cresol 12–13, along with eight known compounds 14–21. Both new metabolites, along with 19, showed moderate in vitro antiproliferative activity against HepG2, MCF-7, and Caco-2. Pharmacophore-based virtual screening suggested both 5-LOX and 15-LOX as the most probable target linked to their observed antiproliferative activity. The in vitro enzyme assays revealed 12 and 13 were able to inhibit 5-LOX more preferentially than 15-LOX, while 19 showed a convergent inhibitory activity toward both enzymes. Further in-depth in silico investigation revealed the molecular interactions inside both enzymes’ active sites and explained the varying inhibitory activity for 12 and 13 toward 5-LOX and 15-LOX.

The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a comparative dissolution study. Further, the samples were assessed for FTIR, DSC, XRD, and NMR for the confirmation of complex formation. Finally, antioxidant and antimicrobial studies and cytotoxicity studies on a breast cancer (MCF-7) cell line were conducted. The dissolution study result showed a marked increment in GS dissolution/release after incorporation in binary (GS: HP β CD, 1:1) and ternary (GS: HP β CD: PL 188; 1:1:0.5) inclusion complexes. Moreover, the ternary complex exhibited a significant enhancement (p < 0.05) in dissolution than did the binary complexes. This might be due to the presence of PL 188, which helps in solubility enhancement of GS. DSC, XRD and SEM evaluation confirmed the modification in the structure of GS. FTIR and NMR results indicated the formation of an inclusion complex. The antioxidant and antimicrobial activity results revealed that GS TC has shown significant (p < 0.05) higher activity than pure GS. The cytotoxicity study results also depicted concentration-dependent cytotoxicity. GS TC exhibited significantly (p < 0.05) high cytotoxicity to cancer cells (IC₅₀ = 225 µg/mL) than pure GS (IC₅₀ = 480 µg/mL). Finally, it was concluded that a remarkable enhancement in the dissolution was observed after the inclusion of GS in the ternary complex and it therefore has significant potential for the treatment of breast cancer.

Background: Evaluation of patients`satisfaction towards pharmacy services is of utmost importance to ensure the quality of care. It helps in identifying domains requiring improvements to provide high quality pharmacy services to ensure the provision of enhanced pharmaceutical care. The current study aims to ascertain the extent of satisfaction towards pharmacy services among patients attending outpatient pharmacies in Kingdom of Saudi Arabia. Methods: A hospital-based cross-sectional study involving 746 patients attending outpatient pharmacies of various public hospitals was conducted from 01 January to 15 February 2020. Information on socio-demographic profile of the study subjects along with their satisfaction towards outpatient pharmacy was extracted by using a 23-items questionnaire. These questions were divided into two domains including 7 questions related to the pharmacy facilities (questions from 1F to 7F) and 8 questions for pharmacy services (questions from 1S to 8S), where F and S denotes facilities and services, respectively. The cumulative satisfaction score was estimated by a 5-item Likert scale with a maximum score of 5 for each item. The relationship between demographics and satisfaction scores was evaluated by using appropriate statistics. Results: There were 746 patients with male preponderance (58.8%). The overall satisfaction score was 2.97 ± 0.65. Satisfaction towards pharmacy services scored lower (mean score: 3.91 ± 0.77) than pharmacy facilities (mean score: 4.03 ± 0.66). Items related to patient`s counseling (3F, 2S, 3S, 6S) scored least during the analysis. Older patients (p = 0.006), male gender (p<0.001), Saudi nationality (0.035), patients attending primary care centers (p = 0.02), and patients with chronic illnesses were significantly associated with lower satisfaction score. Conclusion: This study reported that the satisfaction level of patients attending outpatient pharmacies was low and differed among various socio-demographic groups. Approximately one-half of the patients were not satisfied with outpatient pharmacy services. These findings underscore the dire need for managerial interventions including the hiring of trained professionals, onsite training of pharmacy staff, initiation of clinical or patient centered pharmacy services, evaluation of patient`s response towards the services and appropriate controlling measures, irrespective to the type of hospitals.

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.