Showing papers in "Journal of The Saudi Pharmaceutical Society in 2017"
TL;DR: arget and sustained drug delivery decreases the drug related toxicity and increase patient’s compliance with less frequent dosing, also providing advancement in diagnostic testing.
Abstract: The development of nanoparticle-based drug formulations has yielded the opportunities to address and treat challenging diseases. Nanoparticles vary in size but are generally ranging from 100 to 500 nm. Through the manipulation of size, surface characteristics and material used, the nanoparticles can be developed into smart systems, encasing therapeutic and imaging agents as well as bearing stealth property. Further, these systems can deliver drug to specific tissues and provide controlled release therapy. This targeted and sustained drug delivery decreases the drug related toxicity and increase patient’s compliance with less frequent dosing. Nanotechnology has proven beneficial in the treatment of cancer, AIDS and many other disease, also providing advancement in diagnostic testing.
781 citations
TL;DR: The present review highlights current information and health-promoting effects of rutin and safety pharmacology issues and SAR of the same have also been discussed.
Abstract: The contemporary scientific community has presently recognized flavonoids to be a unique class of therapeutic molecules due to their diverse therapeutic properties. Of these, rutin, also known as vitamin P or rutoside, has been explored for a number of pharmacological effects. Tea leaves, apples, and many more possess rutin as one of the active constituents. Today, rutin has been observed for its nutraceutical effect. The present review highlights current information and health-promoting effects of rutin. Along with this, safety pharmacology issues and SAR of the same have also been discussed.
737 citations
TL;DR: The present review encompasses a total of 174 peer-reviewed original articles from 1967 till date and suggests that antioxidant has superior potential of ameliorating chemotherapeutic induced toxicity.
Abstract: Cancer is the leading cause of mortality worldwide, accounting for almost 13% of deaths in the world. Among the conventional cancer treatments, chemotherapy is most frequently carried out to treat malignant cancer rather than localised lesions which is amenable to surgery and radiotherapy. However, anticancer drugs are associated with a plethora of side effects. Each drug, within every class, has its own set of adverse reactions which may cause patient incompliance and deterioration of the quality of life. One of the major causes of adverse reactions, especially for drugs targeting DNA, is the excessive production of reactive oxygen species (ROS) and subsequent build up of oxidative stress. To curb these undesired side effects, several dietary supplements have been tested, amongst which antioxidants have gained increasing popularity as adjuvant in chemotherapy. However, many oncologists discourage the use of antioxidant rich food supplements because these may interfere with the modalities which kill cancer by generating free radicals. In the present review, all studies reporting concomitant use of several antioxidants with chemotherapy are indiscriminately included and discussed impartially. The effect of supplementation of thirteen different antioxidants and their analogues as a single agent or in combination with chemotherapy has been compiled in this article. The present review encompasses a total of 174 peer-reviewed original articles from 1967 till date comprising 93 clinical trials with a cumulative number of 18,208 patients, 56 animal studies and 35 in vitro studies. Our comprehensive data suggests that antioxidant has superior potential of ameliorating chemotherapeutic induced toxicity. Antioxidant supplementation during chemotherapy also promises higher therapeutic efficiency and increased survival times in patients.
170 citations
TL;DR: The Ag-NP used in the study was found to play dual role of enhancement of both plant growth and diosgenin synthesis, and is of immense application as it opens up development of new methods based on nanoelicitors to enhance the biosynthesis of medicinal natural products in plants.
Abstract: Various methods have been used to enhance production of chemically diverse phytochemicals especially medicinal natural products. With the advancement in nanotechnology, nanoparticles have been reported to have varying impact in plant growth and inducibility of phytochemical composition. Major objective of the study was to study the secondary metabolite modulatory effect of silver nanoparticles. In the current study, treatment of fenugreek seedlings with biosynthesized silver nanoparticles (Ag-NPs) was found to have significant impact on its growth parameters such as leaf number, root length, shoot length and wet weight. On HPLC based analysis, Ag-NPs treated seedlings showed an enhancement in the production of major phytochemical diosgenin to a level of 214.06 ± 17.07 μg/mL. An untreated control gave an yield of only 164.44 ± 7.67 μg/mL of diosgenin, and the observed phytochemical enhancement effect induced by Ag-NP was very significant. Most remarkably, the Ag-NP used in the study was found to play dual role of enhancement of both plant growth and diosgenin synthesis. Hence the study is of immense application as it opens up development of new methods based on nanoelicitors to enhance the biosynthesis of medicinal natural products in plants.
169 citations
TL;DR: The first multiplication atom-bond connectivity index of several common drugs structure are studied, and the accurate expressions are determined, and theoretical conclusions provide practical guiding significance for pharmaceutical engineering.
Abstract: In the field of medicine, there are a large number of new drugs synthesis every year. Before entering the clinical stage, it needs a lot of work on drug testing of the various properties. Due to the lack of a large number of laboratory technician, laboratory equipment and reagents, the drug testing of many biochemical properties are not completed. Theoretical medicine provides a theoretical way for medical researchers to obtain the pharmaceutical properties of compounds by calculation tricks. In this paper, the first multiplication atom-bond connectivity index of several common drugs structure are studied, and the accurate expressions are determined. These theoretical conclusions provide practical guiding significance for pharmaceutical engineering.
100 citations
TL;DR: Several vertex distance-based indices of hexagonal jagged-rectangle from the mathematical point of view are determined and the Wiener related indices of distance-regular structure are considered.
Abstract: In theoretical medicine, topological indices are defined to test the medicine and pharmacy characteristics, such as melting point, boiling point, toxicity and other biological activities. As basic molecular structures, hexagonal jagged-rectangle and distance-regular structure are widely appeared in medicine, pharmacy and biology engineering. In this paper, we study the chemical properties of hexagonal jagged-rectangle from the mathematical point of view. Several vertex distance-based indices are determined. Furthermore, the Wiener related indices of distance-regular structure are also considered.
98 citations
TL;DR: An updated review on the use of CAM practices in Saudi Arabia including commonly used types, common conditions for which it has been used and who uses CAM is presented.
Abstract: Introduction: There is worldwide interest in the use of CAM. Studying CAM in Saudi population is important as it will reflect the influence of psychosocial, cultural and religious factors on health beliefs and behaviors. The objective of this study was to present an updated review on the use of CAM practices in Saudi Arabia including commonly used types, common conditions for which it has been used and who uses CAM. Methods: This review used data from national surveys conducted in Saudi Arabia and published between 2000 and 2015. The literature search was performed considering standards adopted such as Moose guidelines for observational studies. Two authors independently reviewed each article. The search yielded 73 articles, and a total of 36 articles were included. Further careful data extraction was carried out by two independents reviewers. Results: Most of the reviewed studies were cross-sectional in design and were published between 2014 and 2015, and mostly in Riyadh region. Substantial difference in the findings for the patterns of CAM use was revealed. The most commonly employed practice was of spiritual type such as prayer and reciting Quran alone or on water. Other types include herbs (8–76%), honey (14–73%) and dietary products (6–82%). Cupping (Alhijamah) was least used (4–45%). Acupuncture was more practiced among professionals. Conclusion: The utilization of CAM is widely practiced in Saudi Arabia. There is need for efforts to promote research in the field of CAM to address each practice individually. Population surveys should be encouraged supported by mass media to raise knowledge and awareness about the practice of different CAM modalities. The national center of CAM should play a major role in these efforts.
88 citations
TL;DR: Network-based systems pharmacology models using ligand binding principles could be an effective way of understanding drug-related adverse effects and facilitate and strengthen the development of rational drug therapy in clinical practice.
Abstract: The study of the magnitude and variation of drug response is defined as pharmacodynamics (PDs). PD models examine plasma concentration and effect relationship. It can predict the archetypal effect (E) of a drug as a function of the drug concentration (C) and estimate an unknown PD parameter (θpd). The PD models have been described as fixed, linear, log-linear, Emax, sigmoid Emax, and indirect PD response. Ligand binding model is an example of a PD model that works on the underpinning PD principle of a drug, eliciting its pharmacological effect at the receptor site. The pharmacological effect is produced by the drug binding to the receptor to either activate or antagonise the receptor. Ligand binding models describe a system of interacting components, i.e. the interaction of one or more ligands with one or more binding sites. The Emax model is the central method that provides an empirical justification for the concentration/dose-effect relationship. However, for ligand binding models justification is provided by theory of receptor occupancy. In essence, for ligand binding models, the term fractional occupancy is best used to describe the fraction of receptors occupied at a particular ligand concentration. It is stated that the fractional occupancy = occupied binding sites/total binding sites, which means the effect of a drug should depend on the fraction of receptors that are occupied. In the future, network-based systems pharmacology models using ligand binding principles could be an effective way of understanding drug-related adverse effects. This will facilitate and strengthen the development of rational drug therapy in clinical practice.
83 citations
TL;DR: The biochemistry, physiology and proteomics of human oral histatin peptides, secreted from parotid and submandibular salivary glands in human, are highlighted and the potential for therapeutic bio-dental applications has been elaborated.
Abstract: There are many human oral antimicrobial peptides responsible for playing important roles including maintenance, repairing of oral tissues (hard or soft) and defense against oral microbes. In this review we have highlighted the biochemistry, physiology and proteomics of human oral histatin peptides, secreted from parotid and submandibular salivary glands in human. The significance of these peptides includes capability for ionic binding that can kill fungal Candida albicans. They have histidine rich amino acid sequences (7–12 family members; corresponding to residues 12–24, 13–24, 12–25, 13–25, 5–11, and 5–12, respectively) for Histatin-3. However, Histatin-3 can be synthesized proteolytically from histatin 5 or 6. Due to their fungicidal response and high biocompatibility (little or no toxicity), these peptides can be considered as therapeutic agents with most probable applications for example, artificial saliva for denture wearers and salivary gland dysfunction conditions. The objectives of current article are to explore the human histatin peptides for its types, chemical and biological aspects. In addition, the potential for therapeutic bio-dental applications has been elaborated.
82 citations
TL;DR: Only the immobilized drug encapsulated in Alginate gel demonstrated very good antimicrobial activity against various bacteria.
Abstract: The influence of an inorganic support – halloysite nanotubes – on the release rate and biological activity of the antibiotic encapsulated in alginate-based dressings was studied. The halloysite samples were loaded with approx. 10 wt.% of the antibiotic and then encapsulated in Alginate and Gelatin/Alginate gels. The material functionalized with aliphatic amine significantly extended the release of vancomycin from alginate-based gels as compared to that achieved when silica was used. After 24 h, the released amounts of the antibiotic immobilized at silica reached 70%, while for the drug immobilized at halloysite the released amount of vancomycin reached 44% for Alginate discs. The addition of gelatin resulted in even more prolonged sustained release of the drug. The antibiotic was released from the system with a double barrier with Higuchi kinetic model and Fickian diffusion mechanism. Only the immobilized drug encapsulated in Alginate gel demonstrated very good antimicrobial activity against various bacteria. The inhibition zones were greater than those of the standard discs for the staphylococci and enterococci bacteria tested. The addition of gelatin adversely affected the biological activity of the system. The inhibition zones were smaller than those of the reference samples. A reduction in the drug dose by half had no significant effect on changing the release rate and microbiological activity. The in vivo toxicity studies of the material with immobilized drug were carried out with Acutodesmus acuminatus and Daphnia magna . The material studied had no effect on the living organisms used in the bioassays. The proposed system with a double barrier demonstrated high storage stability.
79 citations
TL;DR: A series of ten novel chalcone incorporated quinazoline derivatives (11a–11j) showed more potent anticancer activity than the control drug, Combretastatin – A4.
Abstract: A series of ten novel chalcone incorporated quinazoline derivatives (11a-11j) were designed and synthesized. All the synthesized compounds were evaluated for their anticancer activities against four human cancer cell lines (A549, HT-29, MCF-7 and A375). Among them, four compounds, 11f, 11g, 11i and 11j showed more potent anticancer activity than the control drug, Combretastatin - A4.
TL;DR: This study represents a first step in the study of the chemical composition of H. italicum (Roth) G. Don collected from north Algeria and its antimicrobial properties.
Abstract: The aerial parts of Helichrysum italicum (Roth) G. Don were subjected to hydrodistillation to obtain essential oils which had been analyzed by gas chromatography and gas chromatography coupled with mass spectrometry and tested for antimicrobial activity against 12 bacteria, two yeasts and four fungi by agar diffusion method. The essential oil yielded 0.44% (v/w) and 67 compounds accounting for 99.24% of the oil were identified with a high content of oxygenated sesquiterpenes (61.42%). The most oxygenated sesquiterpene compounds were α-Cedrene (13.61%), α-Curcumene (11.41%), Geranyl acetate (10.05%), Limonene (6.07%), Nerol (5.04%), Neryl acetate (4.91%) and α-Pinene (3.78%). The antimicrobial activity of the essential oil was assayed by using the disk diffusion method on Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 6538, Micrococcus luteus ATCC 4698, Klebsiella pneumonia ATCC 4352, Enterococcus cereus ATCC 2035, Bacillus cereus ATCC 10876, Staphylococcus epidermidis ATCC 12228, Bacillus subtilis ATCC 9372, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 49452, Proteus mirabilis ATCC 35659, Listeria monocytogenes ATCC 15313 and yeasts Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 9763 and fungi, Fusarium solani var. coeruleum, Aspergillus niger, Alternaria alternata, Ascochyta rabiei. H. italicum inhibited the growth of all the tested microorganisms except three bacteria, E. coli ATCC 25922, K. pneumonia ATCC 4352 and L. monocytogenes ATCC 15313. The most sensitive bacterium was E. cereus ATCC 2035 with minimum inhibitory and bactericidal concentrations of 0.79 μg ml-1. A minimum fungistatic and fungicide concentration of 6.325 μg ml-1 and 12.65 μg ml-1 respectively was obtained with C. albicans ATCC 10231 and S. cerevisiae ATCC 9763. However the four fungi were more resistant with fungistatic minimum concentration ranging from 6.325 μg ml-1 to 50.6 μg ml-1 and a fungicide minimum concentration of 50.6 μg ml-1. This antimicrobial activity could be attributed to the essential oil chemical composition. Thus this study represents a first step in the study of the chemical composition of H. italicum (Roth) G. Don collected from north Algeria and its antimicrobial properties.
TL;DR: Using cryoprotectants along with surface coating, the CS-NPs could achieve the desired physicochemical characteristics for a prolonged duration.
Abstract: The aim of the present study was to determine the effect of different cryoprotectants and their concentration on the physicochemical characteristics of chitosan nanoparticles (CS-NPs). The effect of coating of CS-NPs with hyaluronic acid (HA) and alginic acid (ALG) before and after lyophilization was also evaluated. The ionic gelation method was used for the preparation of NPs and six different types of cryoprotectants (sucrose, glucose, trehalose, mannitol, polyethylene glycol-2000, and polyethylene glycol-10,000) were investigated at 5%, 10%, 20%, and 50% concentration levels. Coating of CS-NPs with HA and their protection with high amount of cryoprotectants indicated better particle size stability. Samples that were lyophilized without cryoprotectants resulted in an increase in average size due to high agglomeration. All cryoprotectants with varying amount provided some sort of size stability for the NPs except for the PEG-10,000 which had no protective effect at higher concentrations. Sucrose and trehalose sugars were found to have the highest protective effect with HA coated and uncoated CS-NPs. In conclusion, using cryoprotectants along with surface coating, the CS-NPs could achieve the desired physicochemical characteristics for a prolonged duration.
TL;DR: It was concluded that the developed nano-transfersomes surmount the limitation of low penetration ability of the traditional liposomes across the rat skin and establishes this system as an encouraging dosage form for the delivery of EM via skin route.
Abstract: The objective of the present work was to formulate, optimize and evaluate the potential of novel soft nanovesicles i.e. nano-transfersomes, containing eprosartan mesylate (EM) for transdermal delivery. Nano-transfersomes of EM were developed using Phospholipon 90G, Span 80 (SP) and sodium deoxycholate (SDC) and characterized for vesicle size, shape, entrapment efficiency, in vitro skin permeation study and confocal laser scanning microscopy. The optimized nano-transfersomes formulation showed vesicles size of 108.53 ± 0.06 nm and entrapment efficiency of 63.00 ± 2.76%. The optimized nano-transfersomes provided an improved transdermal flux of 27.22 ± 0.29 µg/cm2/h with an enhancement ratio of 16.80 over traditional liposomes through Wistar rat skin. Confocal laser microscopy of rat skin treated with the optimized formulation showed that the formulation was eventually distributed and permeated deep into the rat skin. The present investigation has shown that the nature and concentration of surfactants (edge activators) influence immense control on the characteristics of nano-transfersomes. It was concluded that the developed nano-transfersomes surmount the limitation of low penetration ability of the traditional liposomes across the rat skin. Improved drug delivery presented by nano-transfersomes establishes this system as an encouraging dosage form for the delivery of EM via skin route.
TL;DR: All the EO tested exhibited antimicrobial activity, however, Cinnamomum zeylanicum EO was the most effective against Pseudomonas spp.
Abstract: Natural products of plant origin, which include essential oils (EO) could be used as a growth inhibitor of pathogenic and spoilage microflora in food. The objective of this study was to determine the antibacterial and antioxidant activity of 21 EO against 10 Pseudomonas species isolated from freshwater fish. The chemical composition of EO was determined by gas chromatography/mass spectrometry. The disc diffusion method and detection of minimum inhibitory concentration (MIC) were used for the determination of the antimicrobial activity. All the EO tested exhibited antimicrobial activity, however, Cinnamomum zeylanicum EO was the most effective against Pseudomonas spp. both according to the disc diffusion and MIC methods. The EOs of Cymbopogon nardus, Origanum vulgare, Foeniculum vulgare and Thymus serpyllum showed the highest antioxidant activity of 93.86 μg, 83.47 μg, 76.74 μg and 74.28 μg TEAC/mL. Application of EO could be an effective tool for inhibition of growth of Pseudomonas spp. on fish.
TL;DR: The marketing used by synthetic detergent companies showed maturity to deal with changes in theories and strategies for promotion and even with the constant social reform that its consumer lived, accompanying them intelligently to be able to capture their changing needs and desires, and so assemble the best way to connect to them.
Abstract: In the year 2016 the synthetic detergents complete 100 years and in this story they evolved as cleaners. They are already part of the routine of thousands of people worldwide. For a higher power of cleaning of the detergent, today, are added phosphates, the main responsible for environmental problems. After 100 years of synthetic detergents, the effect of the combination of various cleaners on the environment is a gap. Legislation and guidelines about the other components of the formula of cleaners still missing. Even the term biodegradable can be best placed on the diversity of products currently entitled biodegradable. A lot attitudes can still be taken to continuously improve the relationship between the parties involved, animals, plants, waters and men, so that in another 100 years continues to exist this interaction with the environment without destroying it. The marketing used by synthetic detergent companies evolved a lot over the years and showed maturity to deal with changes in theories and strategies for promotion and even with the constant social reform that its consumer lived, accompanying them intelligently to be able to capture their changing needs and desires, and so assemble the best way to connect to them. This paper focuses on the subject synthetic detergents as well as (i) types and applications, (ii) threats, (iii) sustainability, (iv) legislation, (v) packaging and (vi) marketing strategies.
TL;DR: A series of new coumarin containing compounds were synthesized from 4-bromomethylcoumarin derivatives 2a, b and different heteroaromatic systems 4a-e, 6a-d, 8, 10via methylene thiolinker and showed strong activity against both MCF-7 and HepG-2 cell lines.
Abstract: A series of new coumarin containing compounds were synthesized from 4-bromomethylcoumarin derivatives 2a, b and different heteroaromatic systems 4a-e, 6a-d, 8, 10via methylene thiolinker. Twenty-four compounds were screened biologically against two human tumor cell lines, breast carcinoma MCF-7 and hepatocellular carcinoma HePG-2, at the national cancer institute, Cairo, Egypt using 5-fluorouracil as standard drug. Compounds 5h, 7d, 7h, 9a, 13a and 13d showed strong activity against both MCF-7 and HepG-2 cell lines with being compound 13a is the most active with IC50 values of 5.5 µg/ml and 6.9 µg/ml respectively. Docking was performed with protein 1KE9 to study the binding mode of the designed compounds.
TL;DR: The results indicate that M. nigra may be a novel candidate for the development of new natural product based therapeutic agents against prostate cancer.
Abstract: Background: Morus nigra L. belongs to the family Moraceae and is frequently used in traditional medicine. Numerous studies have investigated the antiproliferative effects of various extracts of different Morus species, but studies involving the in vitro cytotoxic effect of M. nigra extract are very limited. The purpose of this study was to evaluate the phenolic composition and antioxidant activity of dimethyl sulfoxide extract of M. nigra (DEM) and to investigate, for the first time, the probable cytotoxic effect in human prostate adenocarcinoma (PC-3) cells together with the mechanism involved. Methods: Total polyphenolic contents (TPC), ferric reducing antioxidant power (FRAP) and phenolic compounds of DEM were evaluated using spectrophotometric procedures and HPLC. The cytotoxic effect of DEM on PC-3 cells was revealed using the MTT assay. Mechanisms involved in the cytotoxic effect of DEM on PC-3 cells were then investigated in terms of apoptosis, mitochondrial membrane potential and cell cycle using flow cytometry, while caspase activity was investigated using luminometric analysis. Results: TPC and FRAP values were 20.7 ± 0.3 mg gallic acid equivalents and 48.8 ± 1.6 mg trolox equivalents per g sample, respectively. Ascorbic acid and chlorogenic acid were the major phenolic compounds detected at HPLC analysis. DEM arrested the cell cycle of PC-3 cells at the G1 phase, induced apoptosis via increased caspase activity and reduced mitochondrial membrane potential. Conclusions: Our results indicate that M. nigra may be a novel candidate for the development of new natural product based therapeutic agents against prostate cancer.
TL;DR: Overall this study shows that hospital pharmacists in Kuwait had good knowledge and positive attitude toward PV and ADR reporting, however, the majority of them have never reported ADRs.
Abstract: Introduction: Pharmacovigilance (PV) is essential to detect and prevent adverse drug reactions (ADR) after a drug is marketed. However, ADRs are significantly underreported worldwide. Objective: The aims of this study were to document the knowledge, attitude and practices (KAP) of pharmacists toward PV and ADR reporting and to explore the barriers to implementing a fully functional PV program in Kuwait. Material and methods: Pharmacists working at governmental hospitals were asked to complete a paper-based 25-item questionnaire. Results: A total of 414 pharmacists received the questionnaire and 342 agreed to participate, giving a response rate of 82.6%. Most pharmacists were knowledgeable about the concepts of PV (61.5%) and ADRs (72.6%) and the majority (88.6%) was willing to implement ADR reporting in their clinical practice. Despite this positive attitude, only 26.8% of participants had previously reported an ADR and the main reason for underreporting was stated as not knowing how to report (68.9%). Barriers that hinder the implementation of a PV center included lack of cooperation and communication by healthcare professionals and patients (n = 62), lack of time and proper management (n = 57), lack of awareness of staff and patients (n = 48) and no qualified person to report ADRs (n = 35). Conclusions: Overall this study shows that hospital pharmacists in Kuwait had good knowledge and positive attitude toward PV and ADRs reporting. However, the majority of them have never reported ADRs. These results suggest that targeted educational interventions and a well-defined policy for ADR reporting may help increase ADR reporting and support the implementation of a fully functional independent PV center in Kuwait.
TL;DR: With the rising unemployment rate among Saudi dentists, the governmental bodies that are responsible of dental labor market regulations such as the ministries of health, economy and planning, and labor should come up with a policy to gradually but carefully replace the non-Saudi dentists in both public and private sectors with Saudi Dentists.
Abstract: Background The Kingdom of Saudi Arabia has shown steady growth in the dental workforce over the last 20 years. Although the number of dental colleges has significantly increased in the last decade, there is not any study so far that described the status of the licensed dentist workforce in the kingdom. The present study aimed to explore the demographic distribution and professional characteristics of licensed dentist workforce in Saudi Arabia. Methods This was a descriptive cross-sectional study using the Saudi Commission for Health Specialties (SCFHS) database to identify the number of licensed dentists in Saudi Arabia as well as their professional and demographic characteristics as of December 2016. The data was categorized based on gender, nationality, dental specialty, health sector, geographic location, and professional rank. Results The number of licensed dentists working in the kingdom as of December 2016 was 16887 dentists, and the vast majority of them are professionally registered as general dentists (70.27%). The percentage of general dentists among the professionally registered female dentists is significantly higher than their male counterparts (79.71% vs. 64.80%; P Conclusions Most of the dental care in Saudi Arabia is provided by non-Saudi dentists in both private and public health sectors. With the rising unemployment rate among Saudi dentists, the governmental bodies that are responsible of dental labor market regulations such as the ministries of health, economy and planning, and labor should come up with a policy to gradually but carefully replace the non-Saudi dentists in both public and private sectors with Saudi dentists.
TL;DR: The findings showed that a substantial number of participants still had unused drugs at home and disposed of them inappropriately, but it is understood that they started to exhibit more favorable behaviors in recent years.
Abstract: Objective Keeping unnecessary drugs at home is a situation showing both causes and consequences of irrational use of medicine. This study aimed to evaluate the approaches of a company’s employees regarding drug storage, use, and disposal. Method This online-based descriptive study was held in a multi-centered private-sector company in a voluntary basis. The survey assessing participants’ drug handling and storage behaviors was answered by 1121 employees from across eight provinces of Turkey in 2016. Main outcome measures were storage and disposal of unused/unwanted drugs at home in a rational way. Results The percentage of participants who declared that they keep unused/unwanted drugs at home was 28.0%. About one-third of participants disposed their unused/unwanted drugs via the “garbage, sink, toilet, etc.”. Participants ≥30 years old and living with Conclusion While our findings showed that a substantial number of participants still had unused drugs at home and disposed of them inappropriately, it is understood that they started to exhibit more favorable behaviors in recent years.
TL;DR: A new series of quinazoline derivatives was synthesized and characterized via physicochemical and spectral means and exhibited significant in vitro cytotoxicity against both HeLa and MDA-MB231 cancer cell lines.
Abstract: In this study, a new series of quinazoline derivatives (3–26) was synthesized and characterized via physicochemical and spectral means. Treatment of 2-amino-5-methylbenzoic acid with butyl isothiocyanate resulted in the new 2-thioxoquinazolin-4-one (3). Alkylation and hydrazinolysis of the inherent thioxo group in (1–3) afforded the corresponding thioethers (4–23) and hydrazine derivatives (24 and 25), then 24 was further transformed into tricyclic derivative 26 via cyclocondensation reaction. Compounds 1 and 2, which were previously synthesized, were found to exhibit anticancer activity. The cytotoxicity of all compounds was evaluated in vitro against the HeLa and MDA-MB231 cancer cell lines, including 1 and 2 for comparison, using MTT assay. The treatment of the cells was performed with the synthesized compounds and gefitinib at 0, 1, 5, 10, 25, and 50 μM and incubated for 24 h in 50% DMSO. The IC50 values of the target compounds were reported in μM, using gefitinib as a standard. Our results indicated that all compounds exhibited significant in vitro cytotoxicity against both cell lines. While compounds 1–3 showed good activity, compounds 21–23 were found to be more potent than gefitinib. Thus, compounds 21–23 may be potential anticancer agents, with IC50 values ranging from 1.85 to 2.81 μM in relation to gefitinib (IC50 = 4.3 and 28.3 μM against HeLa and MDA-MB231 cells, respectively).
TL;DR: By increasing the polymers concentration, the rate of drug release decreased for both natural and synthetic polymers, and the best formulation was found to be F3 which contained 40% Hibiscus rosa-sinensis mucilage polymer and showed comparable dissolution profile to the reference drug.
Abstract: Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipient. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. Therefore, Ketoprofen matrix tablets were formulated by employing Hibiscus rosa-sinensis leaves mucilage as natural polymer and HPMC (K100M) as a synthetic polymer to sustain the drug release from matrix system. Direct compression method was used to develop sustained released matrix tablets. The formulated matrix tablets were evaluated in terms of physical appearance, weight variation, thickness, diameter, hardness, friability and in vitro drug release. The difference between the natural and synthetic polymers was investigated concurrently. Matrix tablets developed from each formulation passed all standard physical evaluation tests. The dissolution studies of formulated tablets revealed sustained drug release up to 24 h compared to the reference drug Apo Keto® SR tablets. The dissolution data later were fitted into kinetic models such as zero order equation, first order equation, Higuchi equation, Hixson Crowell equation and Korsmeyer-Peppas equation to study the release of drugs from each formulation. The best formulations were selected based on the similarity factor (f2) value of 50% and more. Through the research, it is found that by increasing the polymers concentration, the rate of drug release decreased for both natural and synthetic polymers. The best formulation was found to be F3 which contained 40% Hibiscus rosa-sinensis mucilage polymer and showed comparable dissolution profile to the reference drug with f2 value of 78.03%. The release kinetics of this formulation has shown to follow non-Fickian type which involved both diffusion and erosion mechanism. Additionally, the statistical results indicated that there was no significant difference (p > 0.05) between the F3 and reference drug in terms of MDT and T50% with p-values of 1.00 and 0.995 respectively.
TL;DR: In vitro studies in Caco-2 cell lines confirmed the safety profile of the developed nanoemulsions with percentage of cell viability above 90% for all formulations and d-α-tocopherol was selected as active ingredient because of its well-recognized interesting anti-oxidant properties.
Abstract: The aim of this study was the assessment of the physicochemical stability of d-α-tocopherol formulated in medium chain triglyceride nanoemulsions, stabilized with Tween®80 and Lipoid®S75 as surfactant and co-surfactant, respectively. d-α-tocopherol was selected as active ingredient because of its well-recognized interesting anti-oxidant properties (such as radical scavenger) for food and pharmaceutical industries. A series of nanoemulsions of mean droplet size below 90 nm (polydispersity index < 0.15) have been produced by high-pressure homogenization, and their surface electrical charge (zeta potential), pH, surface tension, osmolarity, and rheological behavior, were characterized as a function of the d-α-tocopherol loading. In vitro studies in Caco-2 cell lines confirmed the safety profile of the developed nanoemulsions with percentage of cell viability above 90% for all formulations.
TL;DR: The results suggest that the inhibitive effect of oridonin is likely to be driven by the inhibition of Notch signaling pathway and the resulting increased apoptosis.
Abstract: Background: Oridonin is a diterpenoid isolated from Rabdosia rubescens with potent anticancer activity. The aim of our study is to investigate the role of oridonin to inhibit growth and metastasis of human breast cancer cells. Methods: The effect of oridonin on proliferation was evaluated by MTT assay, cell migration and invasion were evaluated by transwell migration and invasion assays in human breast cancer cells. The inhibitive effect of oridonin in vivo was determined by using xenografted nude mice. In addition, the expression of Notch receptors (Notch 1–4) was detected by western blot. Results: Oridonin inhibited human breast cancer cells in vitro and in vivo . In addition, oridonin significantly induced human breast cancer cells apoptosis. Furthermore, the oridonin treatment not only inhibited cancer cell migration and invasion, but more significantly, decreased the expression of Notch 1-4 protein. Conclusion: Our results suggest that the inhibitive effect of oridonin is likely to be driven by the inhibition of Notch signaling pathway and the resulting increased apoptosis.
TL;DR: The overall standard of medication counseling services provided to patients to improve usage of their medications, and consequently, their well-being was poor and the quality of counseling services delivered to patients in community pharmacies in Saudi Arabia was poor.
Abstract: Introduction Pharmacists have a unique opportunity to promote good health through assuring the quality use of medicines. One of the most important tools to achieve this is medication counseling. Counseling plays an important role in enhancing medication adherence and optimizing medication therapy. Therefore, for improving the quality of services delivered by community pharmacists, it is essential to assess the current situation of counseling services delivered to patients. Aims and objectives To date, there is a paucity of data regarding the quality of counseling services delivered to patients in community pharmacies in Saudi Arabia. This study aims to fill this gap through evaluating the counseling skills and counseling content delivered by pharmacists in a sample of community pharmacies in Qassim region, Saudi Arabia. Methods The study was conducted at eleven community pharmacies in Qassim region. A convenient sample of community pharmacies was chosen based on their willingness to participate. To gather information, a form was prepared based on the core and complementary drug use indicators for evaluation of drug use in healthcare settings developed by the WHO. The study was conducted through observing the counseling services performed by the community pharmacists who participated in the study. Results Two hundred and thirty-five forms were completed in eleven community pharmacies. A total of 44.4% of the counseling skills was found to be performed adequately, while only 20.1% of the counseling contents were performed adequately. Conclusions The overall standard of medication counseling services provided to patients to improve usage of their medications, and consequently, their well-being was poor.
TL;DR: The study concludes with biogenic and ecofriendly route for synthesizing nanoparticles with antibacterial activity against drug resistant pathogens and attributes growing interest on endophytes as an emerging source for synthesis of nanoparticles.
Abstract: The present study emphasizes on synthesis of bimetallic silver–gold nanoparticles from cell free supernatant of Pseudomonas veronii strain AS41G inhabiting Annona squamosa L. The synthesized nanoparticles were characterized using hyphenated techniques with UV–Visible spectra ascertained absorbance peak between 400 and 800 nm. Possible interaction of biomolecules in mediating and stabilization of nanoparticles was depicted with Fourier transform infrared spectroscopy (FTIR). X-ray diffraction (XRD) displayed Bragg’s peak conferring the 1 0 0, 1 1 1, 2 0 0, and 2 2 0 facets of the face centered cubic symmetry of nanoparticles suggesting that these nanoparticles were crystalline in nature. Size and shape of the nanoparticles were determined using Transmission electron microscopy (TEM) microgram with size ranging from 5 to 50 nm forming myriad shapes. Antibacterial activity of nanoparticles against significant human pathogens was conferred with well diffusion assay and its synergistic effect with standard antibiotics revealed 87.5% fold increased activity with antibiotic “bacitracin” against bacitracin resistant strains Bacillus subtilis, Escherichia coli and Klebsiella pneumoniae followed by kanamycin with 18.5%, gentamicin with 11.15%, streptomycin with 10%, erythromycin with 9.7% and chloramphenicol with 9.4%. Thus the study concludes with biogenic and ecofriendly route for synthesizing nanoparticles with antibacterial activity against drug resistant pathogens and attributes growing interest on endophytes as an emerging source for synthesis of nanoparticles.
TL;DR: There is compelling evidence in the published literature to demonstrate the beneficial role of Botox in a wide range of non-cosmetic conditions pertaining to the head and neck (mainly level 1 evidence).
Abstract: Botulinum toxin (Botox) is an exotoxin produced from Clostridium botulinum. It blocks the release of acetylcholine from the cholinergic nerve end plates resulting in inactivity of the muscles or glands innervated. The efficacy of Botox in facial aesthetics is well established; however, recent literature has highlighted its utilization in multiple non-cosmetic medical and surgical conditions. The present article reviews the current evidence pertaining to Botox use in the non-cosmetic head and neck conditions. A literature search was conducted using MEDLINE, EMBASE, ISI Web of Science and the Cochrane databases limited to English Language articles published from January 1980 to December 2014. The findings showed that there is level 1 evidence supporting the efficacy of Botox in the treatment of laryngeal dystonia, headache, cervical dystonia, masticatory myalgia, sialorrhoea, temporomandibular joint disorders, bruxism, blepharospasm, hemifacial spasm and rhinitis. For chronic neck pain there is level 1 evidence to show that Botox is ineffective. Level 2 evidence exists for vocal tics and trigeminal. For stuttering, facial nerve paresis, Frey's syndrome and oromandibular dystonia the evidence is level 4. Thus, there is compelling evidence in the published literature to demonstrate the beneficial role of Botox in a wide range of non-cosmetic conditions pertaining to the head and neck (mainly level 1 evidence). With more and more research, the range of clinical applications and number of individuals getting Botox will doubtlessly increase. Botox appears to justify its title as 'the poison that heals'.
TL;DR: Nonwoven nano fibers of cellulose acetate phthalate and curcumin-loaded fibers developed successfully demonstrated controlled in vitro transdermal delivery of CUR for up to 24 h.
Abstract: Novel curcumin (CUR)-loaded cellulose acetate phthalate (CAP) nonwoven electrospun nanofiber (NF) transdermal mat was developed and evaluated for its in vitro CUR diffusion properties. Various CAP solutions from 5 to 20 wt% were tested; 17.5 wt% was found to be a suitable concentration for NF fabrication without defects, such as bubble or ribbon structures. The selected wt% CAP solution was loaded with CUR and electrospun into NFs. The prepared CUR-loaded NFs were characterized using scanning electron microscopy, X-ray diffraction, ultraviolet–visible spectroscopy, thermogravimetric analysis (TGA), and in vitro diffusion studies. The as-prepared fibers demonstrated controlled in vitro transdermal delivery of CUR for up to 24 h.
TL;DR: Intranasal mucoadhesive Desvenlafaxine PLGA-chitosan nanoparticles could be potentially used for the treatment of depression by nose to brain delivery route for superior pharmacokinetic and pharmacodynamic profile of Desvenfaxine.
Abstract: Depression is a debilitating psychiatric condition that remains the second most common cause of disability worldwide. Currently, depression affects more than 4 per cent of the world’s population. Most of the drugs intended for clinical management of depression augment the availability of neurotransmitters at the synapse by inhibiting their neuronal reuptake. However, the therapeutic efficacy of antidepressants is often compromised as they are unable to reach brain by the conventional routes of administration. The purpose of the present study was to reconnoiter the potential of mucoadhesive PLGA-chitosan nanoparticles for the delivery of encapsulated Desvenlafaxine to the brain by nose to brain delivery route for superior pharmacokinetic and pharmacodynamic profile of Desvenlafaxine. Desvenlafaxine loaded PLGA-chitosan nanoparticles were prepared by solvent emulsion evaporation technique and optimized for various physiochemical characteristics. The antidepressant efficacy of optimized Desvenlafaxine was evaluated in various rodent depression models together with the biochemical estimation of monoamines in their brain. Further, the levels of Desvenlafaxine in brain and blood plasma were determined at various time intervals for calculation of different pharmacokinetic parameters. The optimized Desvenlafaxine loaded PLGA-chitosan nanoparticles (∼172 nm/+35 mV) on intranasal administration significantly reduced the symptoms of depression and enhanced the level of monoamines in the brain in comparison with orally administered Desvenlafaxine. Nose to brain delivery of Desvenlafaxine PLGA-chitosan nanoparticles also enhanced the pharmacokinetic profile of Desvenlafaxine in brain together with their brain/blood ratio at different time points. Thus, intranasal mucoadhesive Desvenlafaxine PLGA-chitosan nanoparticles could be potentially used for the treatment of depression.