Displaying publications 1 - 20 of 78 in total

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  1. Fulltext A survey of therapeutic drug monitoring services in Malaysia
    Ab Rahman AF, Ahmed Abdelrahim HE, Mohamed Ibrahim MI
    Saudi Pharm J, 2013 Jan;21(1):19-24.
    PMID: 23960816 DOI: 10.1016/j.jsps.2012.01.002
    In Malaysia, therapeutic drug monitoring (TDM) service was started in the 1980s. Since then, the number of hospitals that offer the service has increased. In this paper, we report the findings of a nationwide survey describing the practice of TDM in these hospitals. Questionnaires were mailed to 128 government hospitals. Data were collected for general characteristics of the hospitals, administrative, and laboratory activities related to TDM service. One hundred and twenty-one hospitals responded to the survey. Thirty-four hospitals (28.1%) provided the service with their own TDM laboratories, 44 hospitals (36.4%) provided the service using other hospitals' laboratories and 43 hospitals (35.5%) did not provide the service at all. TDM services were more likely to be offered in larger hospitals with various medical specialties. Since it is managed entirely by hospital pharmacists, these pharmacists assume an important role in ensuring optimum use of the TDM service.
  2. Fulltext A review on extraction techniques and therapeutic value of polar bioactives from Asian medicinal herbs: Case study on Orthosiphon aristatus, Eurycoma longifolia and Andrographis paniculata
    Abd Aziz NA, Hasham R, Sarmidi MR, Suhaimi SH, Idris MKH
    Saudi Pharm J, 2021 Feb;29(2):143-165.
    PMID: 33679177 DOI: 10.1016/j.jsps.2020.12.016
    Medicinal plants have gained much interest in the prevention and treatment of common human disease such as cold and fever, hypertension and postpartum. Bioactive compounds from medicinal plants were synthesised using effective extraction methods which have important roles in the pharmaceutical product development. Orthosiphon aristatus (OA), Eurycoma longifolia (EL) and Andrographis paniculata (AP) are among popular medicinal herbs in Southeast Asia. The major compounds for these medicinal plants are polar bioactive compounds (rosmarinic acid, eurycomanone and andrographolide) which have multiple benefits to human health. The bioactive compounds are used as a drug to function against a variety of diseases with the support of scientific evidence. This paper was intended to prepare a complete review about the extraction techniques (e.g. OA, EL and AP) of these medicinal plants based on existing studies and scientific works. Suitable solvents and techniques to obtain their major bioactive compounds and their therapeutic potentials were discussed.
  3. Fulltext Importance and globalization status of good manufacturing practice (GMP) requirements for pharmaceutical excipients
    Abdellah A, Noordin MI, Wan Ismail WA
    Saudi Pharm J, 2015 Jan;23(1):9-13.
    PMID: 25685037 DOI: 10.1016/j.jsps.2013.06.003
    Pharmaceutical excipients are no longer inert materials but it is effective and able to improve the characteristics of the products' quality, stability, functionality, safety, solubility and acceptance of patients. It can interact with the active ingredients and alter the medicament characteristics. The globalization of medicines' supply enhances the importance of globalized good manufacturing practice (GMP) requirements for pharmaceutical excipients. This review was intended to assess the globalization status of good manufacturing practice (GMP) requirements for pharmaceutical excipients. The review outcomes demonstrate that there is a lack of accurately defined methods to evaluate and measure excipients' safety. Furthermore good manufacturing practice requirements for excipients are not effectively globalized.
  4. Fulltext A narrative review of approved and emerging anti-obesity medications
    Abdi Beshir S, Ahmed Elnour A, Soorya A, Parveen Mohamed A, Sir Loon Goh S, Hussain N, et al.
    Saudi Pharm J, 2023 Oct;31(10):101757.
    PMID: 37712012 DOI: 10.1016/j.jsps.2023.101757
    BACKGROUND: Recently, many drugs have been approved for halting overweight and obesity-few types of research shifted to using Anti-obesity medications (AOM) solely for well-being and shape-keeping.

    OBJECTIVE: This narrative review's objective was to explore the use of AOM in relation to their medical indications, efficacy, and cardiovascular safety.

    METHODS AND MATERIALS: We have conducted a narrative review of the literature on approved/non-approved AOM used for obesity and overweight. We have shed light on the emerging trials of therapies and evolving remedies.

    RESULTS: Recently, there has been an enormous change in the use of AOM with high consumption that deserves extensive surveillance for the long-term consequences and impact on social, mental, and physical health. Nearly six AOMs and combined therapy are approved by the Food and Drug Administration. The recent guidelines for obesity management have shifted the focus from weight loss to goals that the patient considers essential and toward targeting the root cause of obesity.

    CONCLUSION: The use of AOM increased enormously despite its sometimes-dubious safety and ineffectiveness. The public and medical professionals should be vigilant to the real-world benefits of anti-obesity drugs and their achieved effectiveness with an improved safety profile.

  5. Fulltext Phaleria macrocarpa (Scheff.) Boerl.: An updated review of pharmacological effects, toxicity studies, and separation techniques
    Ahmad R, Khairul Nizam Mazlan M, Firdaus Abdul Aziz A, Mohd Gazzali A, Amir Rawa MS, Wahab HA
    Saudi Pharm J, 2023 Jun;31(6):874-888.
    PMID: 37234341 DOI: 10.1016/j.jsps.2023.04.006
    Phaleria macrocarpa (Scheff.) Boerl. is geographically distributed around Papua Island, Indonesia. Traditionally, P. macrocarpa is exercised to reduce pain, stomachache, diarrhea, tumor problems, blood glucose, cholesterol, and blood pressure. A growing interest in the medicinal values of P. macrocarpa especially in Asia reflects the usage of diverse extraction techniques, particularly modern approaches. In this review article, the extraction methods and solvents relevant to P. macrocarpa were discussed, with the extent of its pharmacological activities. Recent bibliographic databases such as Google Scholar, PubMed, and Elsevier between 2010 and 2022 were assessed. Based on the findings, the pharmacological studies of P. macrocarpa are still pertinent to its traditional uses but primarily emphasise anti-proliferative activity especially colon and breast cancer cells with low toxicity and fruit as the most studied plant part. The utilization of modern separation techniques has predominantly been aimed at extracting mangiferin and phenolic-rich compounds and evaluating their antioxidant capacity. However, the isolation of bioactive compounds remains a challenge, leading to the extensive utilization of the extracts in in vivo studies. This review endeavors to highlight modern extraction methods that could potentially be used as a point of reference in the future for exploring novel bioactive compounds and drug discovery on a multi-scale extraction level.
  6. Fulltext Incidence of Healthcare-Associated Infections (HAIs) and the adherence to the HAIs' prevention strategies in a military hospital in Alkharj
    Ahmed NJ, Haseeb A, Elazab EM, Kheir HM, Hassali AA, Khan AH
    Saudi Pharm J, 2021 Oct;29(10):1112-1119.
    PMID: 34703364 DOI: 10.1016/j.jsps.2021.08.012
    Background: Healthcare-associated infections (HAI) are considered one of the most common adverse events in health care service provision. In order to prevent the occurrence of HAIs, it is important to implement several prevention strategies.

    Objectives: This study aims to determine the incidence of healthcare-associated infections in a military hospital in Alkharj and the adherence to the HAIs' prevention strategies.

    Methods: This study included exporting data for all infected cases confirmed by the infection disease specialists in 2019. The data were collected from the reports that were written by infection control unit and infectious disease department.

    Results: The rate of healthcare associated infections (HAIs) in 2019 was 0.43% of total patient admissions. The rate of central line associated bloodstream infections in 2019 was 1.15 per 1000 central line days. The rate of catheter associated urinary tract infections in 2019 was 1.00 per 1000 catheter days. The rate of ventilator associated pneumonia in 2019 was 2.11 per 1000 ventilator days and the rate of surgical site infections in 2019 was 0.41 %.

    Conclusion: The rate of overall healthcare-associated infections (HAI) was low. The compliance rate of health care workers to preventive measures that control HAIs was generally high but there was a need for more awareness particularly regarding personal protective equipment and hand hygiene. So it is important to attend more awareness activities and workshops particularly regarding personal protective equipment and hand hygiene. Furthermore, infection control unit and infectious disease department in the hospital should support the robust HAI prevention programs.

  7. Fulltext Antibiotics for preventing infection at the surgical site: Single dose vs. multiple doses
    Ahmed NJ, Haseeb A, AlQarni A, AlGethamy M, Mahrous AJ, Alshehri AM, et al.
    Saudi Pharm J, 2023 Dec;31(12):101800.
    PMID: 38028220 DOI: 10.1016/j.jsps.2023.101800
    BACKGROUND: Surgical site infections are common and expensive infections that can cause fatalities or poor patient outcomes. To prevent these infections, antibiotic prophylaxis is used. However, excessive antibiotic use is related to higher costs and the emergence of antimicrobial resistance.

    OBJECTIVES: The present meta-analysis aimed to compare the effectiveness of a single dosage versus several doses of antibiotics in preventing the development of surgical site infections.

    METHODS: PubMed was used to find clinical trials evaluating the effectiveness of a single dosage versus several doses of antibiotics in avoiding the development of surgical site infections. The study included trials that were published between 1984 and 2022. Seventy-four clinical trials were included in the analysis. Odds ratios were used to compare groups with 95% confidence intervals. The data were displayed using OR to generate a forest plot. Review Manager (RevMan version 5.4) was used to do the meta-analysis.

    RESULTS: Regarding clean operations, there were 389 surgical site infections out of 5,634 patients in a single dose group (6.90%) and 349 surgical site infections out of 5,621 patients in multiple doses group (6.21%) (OR = 1.11, lower CI = 0.95, upper CI = 1.30). Regarding clean-contaminated operations, there were 137 surgical site infections out of 2,715 patients in a single dose group (5.05%) and 137 surgical site infections out of 2,355 patients in multiple doses group (5.82%) (OR = 0.87, lower CI = 0.68, upper CI = 1.11). Regarding contaminated operations, there were 302 surgical site infections out of 3,262 patients in a single dose group (9.26%) and 276 surgical site infections out of 3,212 patients in multiple doses group (8.59%) (OR = 1.11, lower CI = 0.84, upper CI = 1.47). In general, there were 828 surgical site infections out of 11,611 patients in a single dose group (7.13%) and 762 surgical site infections out of 11,188 patients in multiple doses group (6.81%) (OR = 1.05, lower CI = 0.93, upper CI = 1.20). The difference between groups was not significant.

    CONCLUSION: The present study showed that using a single-dose antimicrobial prophylaxis was equally effective as using multiple doses of antibiotics in decreasing surgical site infections.

  8. Fulltext Monitoring model drug microencapsulation in PLGA scaffolds using X-ray powder diffraction
    Aina A, Gupta M, Boukari Y, Morris A, Billa N, Doughty S
    Saudi Pharm J, 2016 Mar;24(2):227-31.
    PMID: 27013917 DOI: 10.1016/j.jsps.2015.03.015
    The microencapsulation of three model drugs; metronidazole, paracetamol and sulphapyridine into Poly (dl-Lactide-Co-Glycolide) (PLGA) scaffolds were probed using X-ray Powder Diffraction (XRPD). Changes in the diffraction patterns of the PLGA scaffolds after encapsulation was suggestive of a chemical interaction between the pure drugs and the scaffolds and not a physical intermixture.
  9. Fulltext Validation of the knowledge, attitude and perceived practice of asthma instrument among community pharmacists using Rasch analysis
    Akram W, Hussein MS, Ahmad S, Mamat MN, Ismail NE
    Saudi Pharm J, 2015 Oct;23(5):499-503.
    PMID: 26594115 DOI: 10.1016/j.jsps.2015.01.011
    There is no instrument which collectively assesses the knowledge, attitude and perceived practice of asthma among community pharmacists. Therefore, this study aimed to validate the instrument which measured the knowledge, attitude and perceived practice of asthma among community pharmacists by producing empirical evidence of validity and reliability of the items using Rasch model (Bond & Fox software®) for dichotomous and polytomous data. This baseline study recruited 33 community pharmacists from Penang, Malaysia. The results showed that all PTMEA Corr were in positive values, where an item was able to distinguish between the ability of respondents. Based on the MNSQ infit and outfit range (0.60-1.40), out of 55 items, 2 items from the instrument were suggested to be removed. The findings indicated that the instrument fitted with Rasch measurement model and showed the acceptable reliability values of 0.88 and 0.83 and 0.79 for knowledge, attitude and perceived practice respectively.
  10. Fulltext Inclusion complex of clausenidin with hydroxypropyl-β-cyclodextrin: Improved physicochemical properties and anti-colon cancer activity
    Al-Abboodi AS, Al-Sheikh WM, Eid EEM, Azam F, Al-Qubaisi MS
    Saudi Pharm J, 2021 Mar;29(3):223-235.
    PMID: 33981171 DOI: 10.1016/j.jsps.2021.01.006
    The long-term objective of the present study was to prepare, physicochemically characterize and determine the anticancer of clausenidin/hydroxypropyl-β-cyclodextrin (Clu/HPβCD) inclusion complex. We used differential scanning calorimetry, X-ray diffractometer, fourier transform infrared spectroscopy, ultraviolet-visible spectrophotometer and 13C and 1H nuclear magnetic resonance followed by in vitro anticancer assays. The orientation and intermolecular interactions of Clausenidin within cyclodextrin cavity were also ascertained by molecular docking simulation accomplished by AutoDock Vina. The guest molecule was welcomed by the hydrophobic cavity of the host molecule and sustained by hydrogen bond between host/guest molecules. The constant drug release with time, and increased solubility were found after successful complexation with HPβCD as confirmed by physicochemical characterizations. Clausenidin had greater cytotoxic effect on colon cancer HT29 cells when incorporated into HPβCD cavity than dissolved in DMSO. Also, from a comparison of cell viability between normal and cancer cells, a reduced side effect was observed. The Clu/HPβCD inclusion complex triggered reactive oxygen species-mediated cytotoxicity in HT29 cells. The inclusion complex-treated HT29 cells showed cell cycle arrest and death by apoptosis associated with caspases activation. The presence of HPβCD seems to aid the anticancer activity of clausenidin.
  11. Fulltext Preparation, characterization, in vitro drug release and anti-inflammatory of thymoquinone-loaded chitosan nanocomposite
    Al-Qubaisi MS, Al-Abboodi AS, Alhassan FH, Hussein-Al-Ali S, Flaifel MH, Eid EEM, et al.
    Saudi Pharm J, 2022 Apr;30(4):347-358.
    PMID: 35527823 DOI: 10.1016/j.jsps.2022.02.002
    In this study, we formulated Thymoquinone-loaded nanocomposites (TQ-NCs) using high-pressure homogenizer without sodium tripolyphosphate. The TQ-NCs were characterized and their anti-inflammatory determined by the response of the LPS-stimulated macrophage RAW 264.7 cells in the production of nitric oxide, prostaglandin E2, tumor necrosis factor-α, interleukin-6, and interleukin-1β. The physicochemical properties of TQ-NC were determined using different machines. TQ was fully incorporated in the highly thermal stable nanoparticles. The nanoparticles showed rapid release of TQ in the acidic medium of the gastric juice. In medium of pH 6.8, TQ-NC exhibited sustained release of TQ over a period of 100 h. The results suggest that TQ-NC nanoparticles have potential application as parenterally administered therapeutic compound. TQ-NC effectively reduce production of inflammatory cytokines by the LPS-stimulated RAW 264.7 cells, indicating that they have anti-inflammatory properties. In conclusion, TQ-NC nanoparticles have the characteristics of efficient carrier for TQ and an effective anti-inflammatory therapeutic compound.
  12. Fulltext Assessing mental health among students in the UAE: A cross-sectional study utilizing the DASS-21 scale
    Alalalmeh SO, Hegazi OE, Shahwan M, Hassan N, Humaid Alnuaimi GR, Alaila RF, et al.
    Saudi Pharm J, 2024 Apr;32(4):101987.
    PMID: 38405042 DOI: 10.1016/j.jsps.2024.101987
    BACKGROUND: The escalating worldwide concerns for mental health, significantly amplified by the COVID-19 pandemic, necessitates understanding the impact on vulnerable populations, such as university students. This study aims to investigate the prevalence and implications of depression, anxiety, and stress among university students in the United Arab Emirates (UAE) using the Depression, Anxiety, and Stress Scale-21 Items (DASS-21).

    METHODS: This study utilized convenience sampling to investigate the mental health of undergraduates in UAE universities using a bilingual DASS-21 questionnaire via Google Forms. Analysis was conducted using SPSS version 29.0, employing descriptive statistics, Chi-squared tests, Mann-Whitney tests, Kruskal-Wallis tests, and Multinomial Logistic Regression to analyze relationships between sociodemographic variables and mental health scores.

    RESULTS: The study examined 332 students, with most female participants (81 %, n = 269) and individuals aged 18-20 (89.8 %, n = 298). It revealed higher mean DASS scores among females: Depression (M = 15.80, p = 0.030), Anxiety (M = 17.63, p 

  13. Fulltext Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity
    Alasmary FAS, Awaad AS, Alafeefy AM, El-Meligy RM, Alqasoumi SI
    Saudi Pharm J, 2018 Jan;26(1):138-143.
    PMID: 29379346 DOI: 10.1016/j.jsps.2017.09.011
    Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl-3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4-aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & Anti-Ulcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P 
  14. Fulltext Factors influencing community pharmacist decision to dispense generic or branded medicines; Eastern Province, Alahsa, Saudi Arabia
    Albadr Y, Khan TM
    Saudi Pharm J, 2015 Apr;23(2):143-6.
    PMID: 25972733 DOI: 10.1016/j.jsps.2014.07.002
    Rising costs of medicines have increased the interest of policy makers in generic medicines. However, consumers' and health care providers' perception and attitude towards generic medicine act as a main barrier to the promotion of generic medicines.
  15. Fulltext An integrated multi-pronged reverse vaccinology and biophysical approaches for identification of potential vaccine candidates against Nipah virus
    Albutti A
    Saudi Pharm J, 2023 Dec;31(12):101826.
    PMID: 38028215 DOI: 10.1016/j.jsps.2023.101826
    Nipah virus, a paramyxovirus linked to Hendra virus that first appeared in Malaysia and is the etiological agent of viral lethal encephalitis, has emerged as a strong threat to the health community in recent decades. Viral infections are seriously affecting global health. Since there are now no efficient therapeutic options, it will take considerable effort to develop appropriate therapeutic management for the Nipah virus. The main purpose of this study was to design a messenger RNA-based multi-epitope vaccine construct against Nipah virus. This purpose was achieved through multiple immunogenic epitopes prediction using Nipah virus antigenic protein using the immune epitope database and analysis resource (IEDB) followed by the vaccine construction and processing. As in multi-epitopes vaccine construction we selected immunogenic potential fragments of viral proteins, therefore in host immune stimulation we observed proper immune responses toward a multi-epitopes vaccine. In this study, the Nipah virus V protein was used to identify immunodominant epitopes utilizing several reverse vaccinology, immunoinformatics and biophysical methods. The potential antigenic predicted epitopes were further analyzed for immunoinformatics analysis and only selected probable antigenic and non-toxic epitopes were used in designing a multi-epitope mRNA based in silico vaccine against the target pathogen. In vaccine designing a total number of 03B cell epitopes, 09 Cytotoxic T lymphocytes (CTLs) and 01 Helper T lymphocytes (HTL) were prioritized as a good vaccine candidate. In the vaccine construction phase, the selected epitopes were linked together using EAAAK, GPGPG, KK, and AAY linkers, and B-defensin (adjuvant), and MITD sequences were also added to the vaccine construct to increase the potency. After vaccine construction, the physiochemical properties of the vaccine construct were evaluated which predicted that the vaccine construct comprises 320 amino acids with 34.29 kDa (kDa) molecular weight. The instability index was 36.55 proving its stability with the aliphatic index of 82.88. Furthermore, 9.0 theoretical pI and -0.317, GRAVY (Grand Average of Hydropathy) values were predicted in physicochemical properties analysis. A solubility check was applied against the vaccine construct depicting that the vaccine construct is soluble with its calculated value of 0.6. Additionally, after prediction the 3D structure was modeled and refined for docking analysis, the refined 3D structure of the vaccine candidate was further checked for binding affinity with immune cell receptors through docking analysis, in the docking analysis we observed that the vaccine construct has a good binding affinity with immune cells receptor and can induce a proper immune response in host cells. As we predicted effective binding of the designed vaccine construct, hence it can further facilitate the development of vaccine formulation against the Nipah virus. Additionally, molecular dynamic simulation was done using the AMBER v20 package for analysis of the dynamic behaviour of the docked complexes and we observed proper binding stability of the vaccine with target receptor. In C-immune simulation, different humoral and cellular antibody titer was observed in response to the vaccine. Overall using bioinformatics, immunoinformatics, and biophysical approaches we observed that this mRNA base epitopes vaccine construct could facilitate the proof of concept for the formation of the experimental base vaccine against the Nipah virus, as the in silico predictions indicated that the vaccine is highly promising in terms of developing protective immunity. However experimental validation is required to disclose the real immune-protective efficacy of the vaccine.
  16. Fulltext Challenges to and the future of medication safety in Saudi Arabia: A qualitative study
    Aljadhey H, Mahmoud MA, Hassali MA, Alrasheedy A, Alahmad A, Saleem F, et al.
    Saudi Pharm J, 2014 Sep;22(4):326-32.
    PMID: 25161376 DOI: 10.1016/j.jsps.2013.08.001
    Medication safety is a global concern among healthcare providers. However, the challenges to and the future of medication safety in Saudi Arabia have not been explored.
  17. Fulltext Medication safety officer preparatory course: Outcomes and experiences
    Aljadhey H, Alkhani S, Khan TM
    Saudi Pharm J, 2017 Nov;25(7):1011-1014.
    PMID: 29158708 DOI: 10.1016/j.jsps.2017.03.002
    Purpose: Few hospitals employ a medication safety officer. A medication safety officer preparatory course was planned using a structured curriculum to prepare pharmacists with the knowledge and skills to start medication safety officer activities. The current study aims to assess the outcome, as change in knowledge, of a hospital medication safety officer preparatory course.

    Methods: We conducted a three-day course in February 2011 in Riyadh, Saudi Arabia. It was developed to provide attendees with the essential knowledge and skills to become a medication safety officer. Teaching methodologies included didactic teaching, group discussions, case presentations, and an independent study of medication safety materials. The content of the course focused on the various roles of a medication safety officer, the importance of medication safety in a health care setting, the incidence of adverse drug events in a hospital setting, strategies to identify and prevent adverse events, the use of root cause analysis and failure mode and effect analysis, the role of an officer in hospital accreditation, and ways for promoting safety culture. Assessment of the course outcome was accomplished by comparing scores of knowledge level before and after the course. The knowledge level was assessed by a 20-item exam which was developed and validated by course instructors.

    Results: Twenty-one participants attended the course and completed both the baseline and after-course assessment questionnaires. The majority was male (N = 14, % = 66.7) with a job experience of 1-5 five years (N = 10, % = 47.6). The knowledge score increased from 14.3 ± 1.90 (mean ± standard deviation) at baseline to 18.5 ± 1.43 after successfully completing the course (P 

  18. Fulltext Students' attitude toward use of over the counter medicines during exams in Saudi Arabia
    Almalak H, Albluwi AI, Alkhelb DA, Alsaleh HM, Khan TM, Hassali MA, et al.
    Saudi Pharm J, 2014 Apr;22(2):107-12.
    PMID: 24648821 DOI: 10.1016/j.jsps.2013.02.004
    To explore the use of over the counter (OTC) medicines among students during exams in Riyadh City, Kingdom of Saudi Arabia.
  19. Fulltext Mechanism of action of Orthosiphon stamineus against non-alcoholic fatty liver disease: Insights from systems pharmacology and molecular docking approaches
    Alshehade SA, Al Zarzour RH, Murugaiyah V, Lim SYM, El-Refae HG, Alshawsh MA
    Saudi Pharm J, 2022 Nov;30(11):1572-1588.
    PMID: 36465851 DOI: 10.1016/j.jsps.2022.09.001
    Non-alcoholic fatty liver disease (NAFLD) is one of the most common complications of a metabolic syndrome caused by excessive accumulation of fat in the liver. Orthosiphon stamineus also known as Orthosiphon aristatus is a medicinal plant with possible potential beneficial effects on various metabolic disorders. This study aims to investigate the in vitro inhibitory effects of O. stamineus on hepatic fat accumulation and to further use the computational systems pharmacology approach to identify the pharmacokinetic properties of the bioactive compounds of O. stamineus and to predict their molecular mechanisms against NAFLD.

    METHODS: The effects of an ethanolic extract of O. stamineus leaves on cytotoxicity, fat accumulation and antioxidant activity were assessed using HepG2 cells. The bioactive compounds of O. stamineus were identified using LC/MS and two bioinformatics databases, namely the Traditional Chinese Medicine Integrated Database (TCMID) and the Bioinformatics Analysis Tool for the Molecular Mechanism of Traditional Chinese Medicine (BATMAN-TCM). Pathway enrichment analysis was performed on the predicted targets of the bioactive compounds to provide a systematic overview of the molecular mechanism of action, while molecular docking was used to validate the predicted targets.

    RESULTS: A total of 27 bioactive compounds corresponding to 50 potential NAFLD-related targets were identified. O. stamineus exerts its anti-NAFLD effects by modulating a variety of cellular processes, including oxidative stress, mitochondrial β-oxidation, inflammatory signalling pathways, insulin signalling, and fatty acid homeostasis pathways. O. stamineus is significantly targeting many oxidative stress regulators, including JNK, mammalian target of rapamycin (mTOR), NFKB1, PPAR, and AKT1. Molecular docking analysis confirmed the expected high affinity for the potential targets, while the in vitro assay indicates the ability of O. stamineus to inhibit hepatic fat accumulation.

    CONCLUSION: Using the computational systems pharmacology approach, the potentially beneficial effect of O. stamineus in NAFLD was indicated through the combination of multiple compounds, multiple targets, and multicellular components.

  20. QbD driven targeted pulmonary delivery of dexamethasone-loaded chitosan microspheres: Biodistribution and pharmacokinetic study
    Asha BR, Goudanavar P, Koteswara Rao GSN, Gandla K, Raghavendra Naveen N, Majeed S, et al.
    Saudi Pharm J, 2023 Sep;31(9):101711.
    PMID: 37564747 DOI: 10.1016/j.jsps.2023.101711
    Inhaling drugs, on the other hand, is limited mainly by the natural mechanisms of the respiratory system, which push drug particles out of the lungs or make them inefficient once they are there. Because of this, many ways have been found to work around the problems with drug transport through the lungs. Researchers have made polymeric microparticles (MP) and nanoparticles as a possible way to get drugs into the lungs. They showed that the drug could be trapped in large amounts and retained in the lungs for a long time, with as little contact as possible with the bloodstream. MP were formulated in this study to get dexamethasone (DMC) into the pulmonary area. The Box-Behnken design optimized microspheres preparation to meet the pulmonary delivery prerequisites. Optimized formulation was figured out based on the desirability approach. The mass median aerodynamic diameter (MMAD) of the optimized formula (O-DMC-MP) was 8.46 ± 1.45 µm, and the fine particle fraction (FPF) was 77.69 ± 1.26%. This showed that it made suitable drug delivery system, which could make it possible for MP to settle deeply in the lung space after being breathed in. With the first burst of drug release, it was seen that drug release could last up to 16 h. Also, there was no clear sign that the optimized formulation was toxic to the alveoli basal epithelial cells in the lungs, as supported by cytotoxic studies in HUVEC, A549, and H1299 cell lines. Most importantly, loading DMC inside MP cuts the amount of drug into the bloodstream compared to plain DMC, as evident from biodistribution studies. Stability tests have shown that the product can stay the same over time at both the storage conditions. Using chitosan DMC-MP can be a better therapeutic formulation to treat acute respiratory distress syndrome (ARDS).
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