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Showing papers in "Journal of The Saudi Pharmaceutical Society in 2016"


Journal ArticleDOI
TL;DR: The basic aim of this review was to summarize the basics of oxidative stress in diabetes mellitus.
Abstract: Human body is continuously exposed to different types of agents that results in the production of reactive species called as free radicals (ROS/RNS) which by the transfer of their free unpaired electron causes the oxidation of cellular machinery. In order to encounter the deleterious effects of such species, body has got endogenous antioxidant systems or it obtains exogenous antioxidants from diet that neutralizes such species and keeps the homeostasis of body. Any imbalance between the RS and antioxidants leads to produce a condition known as “oxidative stress” that results in the development of pathological condition among which one is diabetes. Most of the studies reveal the inference of oxidative stress in diabetes pathogenesis by the alteration in enzymatic systems, lipid peroxidation, impaired Glutathione metabolism and decreased Vitamin C levels. Lipids, proteins, DNA damage, Glutathione, catalane and superoxide dismutase are various biomarkers of oxidative stress in diabetes mellitus. Oxidative stress induced complications of diabetes may include stroke, neuropathy, retinopathy and nephropathy. The basic aim of this review was to summarize the basics of oxidative stress in diabetes mellitus.

1,062 citations


Journal ArticleDOI
TL;DR: The plants are used successfully in the synthesis of various greener nanoparticles such as cobalt, copper, silver, gold, palladium, platinum, zinc oxide and magnetite, and the biological synthesis of metallic nanoparticles is inexpensive, single step and eco-friendly methods.
Abstract: The field of nanotechnology mainly encompasses with biology, physics, chemistry and material sciences and it develops novel therapeutic nanosized materials for biomedical and pharmaceutical applications. The biological syntheses of nanoparticles are being carried out by different macro-microscopic organisms such as plant, bacteria, fungi, seaweeds and microalgae. The biosynthesized nanomaterials have been effectively controlling the various endemic diseases with less adverse effect. Plant contains abundant natural compounds such as alkaloids, flavonoids, saponins, steroids, tannins and other nutritional compounds. These natural products are derived from various parts of plant such as leaves, stems, roots shoots, flowers, barks, and seeds. Recently, many studies have proved that the plant extracts act as a potential precursor for the synthesis of nanomaterial in non-hazardous ways. Since the plant extract contains various secondary metabolites, it acts as reducing and stabilizing agents for the bioreduction reaction to synthesized novel metallic nanoparticles. The non-biological methods (chemical and physical) are used in the synthesis of nanoparticles, which has a serious hazardous and high toxicity for living organisms. In addition, the biological synthesis of metallic nanoparticles is inexpensive, single step and eco-friendly methods. The plants are used successfully in the synthesis of various greener nanoparticles such as cobalt, copper, silver, gold, palladium, platinum, zinc oxide and magnetite. Also, the plant mediated nanoparticles are potential remedy for various diseases such as malaria, cancer, HIV, hepatitis and other acute diseases.

681 citations


Journal ArticleDOI
TL;DR: Physically cross-linked methods for preparation of hydrogel are the alternate solution of cross-linker toxicity and chemical cross-linking is the highly resourceful method for the formation of Hydrogels having an excellent mechanical strength.
Abstract: Hydrogels are being investigated recently for the bioactive molecules (in particular pharmaceutical proteins) controlled release, such as matrices, and for the living cells encapsulation. Biodegradable nature of hydrogels has created much interest for drug delivery systems. The original three-dimensional structure disintegrates into nontoxic substances to ascertain an excellent biocompatibility of the gel. Chemical cross-linking is the highly resourceful method for the formation of hydrogels having an excellent mechanical strength. Cross-linkers used in hydrogel preparation should be extracted from the hydrogels before use due to their reported toxicity. Physically cross-linked methods for preparation of hydrogel are the alternate solution of cross-linker toxicity.

340 citations


Journal ArticleDOI
TL;DR: This review article emphasizes on the recent advancements made in the delivery of protein and peptides by a non-invasive (peroral) route into the body.
Abstract: In the modern world, a number of therapeutic proteins such as vaccines, antigens, and hormones are being developed utilizing different sophisticated biotechnological techniques like recombinant DNA technology and protein purification. However, the major glitches in the optimal utilization of therapeutic proteins and peptides by the oral route are their extensive hepatic first-pass metabolism, degradation in the gastrointestinal tract (presence of enzymes and pH-dependent factors), large molecular size and poor permeation. These problems can be overcome by adopting techniques such as chemical transformation of protein structures, enzyme inhibitors, mucoadhesive polymers and permeation enhancers. Being invasive, parenteral route is inconvenient for the administration of protein and peptides, several research endeavors have been undertaken to formulate a better delivery system for proteins and peptides with major emphasis on non-invasive routes such as oral, transdermal, vaginal, rectal, pulmonary and intrauterine. This review article emphasizes on the recent advancements made in the delivery of protein and peptides by a non-invasive (peroral) route into the body.

274 citations


Journal ArticleDOI
TL;DR: Orally disintegrating films have potential for business and market exploitation because of their myriad of benefits over orally disintegrating tablets and the market prospect of this innovative dosage form is also targeted.
Abstract: Over the past few decades, tendency toward innovative drug delivery systems has majorly increased attempts to ensure efficacy, safety and patient acceptability. As discovery and development of new chemical agents is a complex, expensive and time consuming process, so recent trends are shifting toward designing and developing innovative drug delivery systems for existing drugs. Out of those, drug delivery system being very eminent among pediatrics and geriatrics is orally disintegrating films (ODFs). These fast disintegrating films have superiority over fast disintegrating tablets as the latter are associated with the risks of choking and friability. This drug delivery system has numerous advantages over conventional fast disintegrating tablets as they can be used for dysphasic and schizophrenic patients and are taken without water due to their ability to disintegrate within a few seconds releasing medication in mouth. Various approaches are employed for formulating ODFs and among which solvent casting and spraying methods are frequently used. Generally, hydrophilic polymers along with other excipients are used for preparing ODFs which allow films to disintegrate quickly releasing incorporated active pharmaceutical ingredient (API) within seconds. Orally disintegrating films have potential for business and market exploitation because of their myriad of benefits over orally disintegrating tablets. This present review attempts to focus on benefits, composition, approaches for formulation and evaluation of ODFs. Additionally, the market prospect of this innovative dosage form is also targeted.

208 citations


Journal ArticleDOI
TL;DR: By means of drug molecular structure analysis and edge dividing technology, this article presents the forgotten topological index of several widely used chemical structures which often appear in drug molecular graphs.
Abstract: A massive of early drug tests implies that there exist strong inner relationships between the bio-medical and pharmacology characteristics of drugs and their molecular structures. The forgotten topological index was defined to be used in the analysis of drug molecular structures, which is quite helpful for pharmaceutical and medical scientists to grasp the biological and chemical characteristics of new drugs. Such tricks are popularly employed in developing countries where enough money is lacked to afford the relevant chemical reagents and equipment. In our article, by means of drug molecular structure analysis and edge dividing technology, we present the forgotten topological index of several widely used chemical structures which often appear in drug molecular graphs.

136 citations


Journal ArticleDOI
TL;DR: There is an urgent need for relevant clinical data from nanogels so as to allow translation of the nanogel concept into a viable therapeutic application for the treatment of cancer.
Abstract: Nanogels are being explored as drug delivery agents for targeting cancer due to their easy tailoring properties and ability to efficiently encapsulate therapeutics of diverse nature through simple mechanisms. Nanogels are proficiently internalized by the target cells, avoid accumulating in nontarget tissues thereby lower the therapeutic dosage and minimize harmful side effects. However, there is an urgent need for relevant clinical data from nanogels so as to allow translation of the nanogel concept into a viable therapeutic application for the treatment of cancer. This review highlights some of the recent progress in nanogels as a carrier in the field of nanomedicine for the treatment of cancer. The present review critically analyzes the use of extracellular pH targeting for nanogels, siRNA delivery, PEGylated nanogels, multi-responsive nanogels and intracellular delivery of nanogels for improved therapy of cancer.

132 citations


Journal ArticleDOI
TL;DR: The aim of this review was to discuss the types and functions of oral AMPs and their role in combating microorganisms and infections in the oral cavity.
Abstract: Antimicrobial peptides (AMPs) are a wide-ranging class of host-defense molecules that act early to contest against microbial invasion and challenge. These are small cationic peptides that play an important in the development of innate immunity. In the oral cavity, the AMPs are produced by the salivary glands and the oral epithelium and serve defensive purposes. The aim of this review was to discuss the types and functions of oral AMPs and their role in combating microorganisms and infections in the oral cavity.

125 citations


Journal ArticleDOI
TL;DR: The present investigation reports facile fabrication of silver nanoparticles from endophytic fungi that exhibited bactericidal activity against selected human pathogens and DNA damage activity.
Abstract: Mycosynthesis of silver nanoparticles was achieved by endophytic Colletotrichum sp ALF2-6 inhabiting Andrographis paniculata Well dispersed nanoparticles were characterized using UV-Visible spectrometry with maximum absorption conferring at 420 nm FTIR analysis revealed possible biomolecules reducing the metal salt and stabilization of nanoparticles XRD analysis depicted the diffraction intensities exhibiting between 20 and 80 °C at 2theta angle thus conferring the crystalline nature of nanoparticles Morphological characteristic using TEM revealed the polydispersity of nanoparticles with size ranging from 20 to 50 nm Synthesized nanoparticles exhibited bactericidal activity against selected human pathogens Nanoparticles mode of action was carried out to reveal DNA damage activity Thus the present investigation reports facile fabrication of silver nanoparticles from endophytic fungi

120 citations


Journal ArticleDOI
TL;DR: The main goal of this article is to explore the role of microparticles in ulcerative colitis for the appropriate targeting of drugs to colon and find microparticulate systems seem to be a promising approach for controlled and sustained drug release after oral administration.
Abstract: Ulcerative colitis is the chronic relapsing multifactorial gastrointestinal inflammatory bowel disease, which is characterized by bloody or mucus diarrhea, tenesmus, bowel dystension, anemia. The annual incidence of ulcerative colitis in Asia, North America and Europe was found to be 6.3, 19.2 and 24.3 per 100,000 person-years. The major challenge in the treatment of ulcerative colitis is appropriate local targeting and drug related side-effects. To overcome these challenges, microparticulate systems seem to be a promising approach for controlled and sustained drug release after oral administration. The main goal of this article is to explore the role of microparticles in ulcerative colitis for the appropriate targeting of drugs to colon. There are different approaches which have been studied over the last decade, including prodrugs, polymeric approach, time released system, pH sensitive system, which show the site specific drug delivery to colon. Among these approaches, microparticulate drug delivery system has been gaining an immense importance for local targeting of drug to colon at a controlled and sustained rate. Combined approaches such as pH dependent and time dependent system provide the maximum release of drug into colon via oral route. This article embraces briefly about pathophysiology, challenges and polymeric approaches mainly multiparticulate systems for site specific drug delivery to colon in sustained and controlled manner so that drug related side-effects by reducing dosage frequency can be minimized.

109 citations


Journal ArticleDOI
TL;DR: This randomised controlled study provides evidence about favourable impact of a pharmacist led diabetes intervention programme on HbA1c, medication adherence and QoL scores amongst type 2 diabetes patients at UKMMC, Malaysia.
Abstract: Malaysia is situated in Western Pacific region which bears 36.17% of total diabetes mellitus population. Pharmacist led diabetes interventions have been shown to improve the clinical outcomes amongst diabetes patients in various parts of the world. Despite high prevalence of disease in this region there is a lack of reported intervention outcomes from this region. The aim of this study was to evaluate the impact of a pharmacist led intervention on HbA1c, medication adherence, quality of life and other secondary outcomes amongst type 2 diabetes patients. Method: Type 2 diabetes mellitus patients (n = 73) attending endocrine clinic at Universiti Kebangsaan Malaysia Medical Centre (UKMMC) were randomised to either control (n = 36) or intervention group (n = 37) after screening. Patients in the intervention group received an intervention from a pharmacist during the enrolment, after three and six months of the enrolment. Outcome measures such as HbA1c, BMI, lipid profile, Morisky scores and quality of life (QoL) scores were assessed at the enrolment and after 6 months of the study in both groups. Patients in the control group did not undergo intervention or educational module other than the standard care at UKMMC. Results: HbA1c values reduced significantly from 9.66% to 8.47% (P = 0.001) in the intervention group. However, no significant changes were noted in the control group (9.64–9.26%, P = 0.14). BMI values showed significant reduction in the intervention group (29.34–28.92 kg/m2; P = 0.03) and lipid profiles were unchanged in both groups. Morisky adherence scores significantly increased from 5.83 to 6.77 (P = 0.02) in the intervention group; however, no significant change was observed in the control group (5.95–5.98, P = 0.85). QoL profiles produced mixed results. Conclusion: This randomised controlled study provides evidence about favourable impact of a pharmacist led diabetes intervention programme on HbA1c, medication adherence and QoL scores amongst type 2 diabetes patients at UKMMC, Malaysia.

Journal ArticleDOI
TL;DR: A high prevalence for pDDIs was found in the Department of Cardiology, most of which were of moderate severity, and older patients, patients with longer hospital stay and with elevated number of prescribed drugs were at higher risk of p DDIs.
Abstract: Drug-drug interactions (DDIs) may result in the alteration of therapeutic response. Sometimes they may increase the untoward effects of many drugs. Hospitalized cardiac patients need more attention regarding drug-drug interactions due to complexity of their disease and therapeutic regimen. This research was performed to find out types, prevalence and association between various predictors of potential drug-drug interactions (pDDIs) in the Department of Cardiology and to report common interactions. This study was performed in the hospitalized cardiac patients at Ayub Teaching Hospital, Abbottabad, Pakistan. Patient charts of 2342 patients were assessed for pDDIs using Micromedex® Drug Information. Logistic regression was applied to find predictors of pDDIs. The main outcome measure in the study was the association of the potential drug-drug interactions with various factors such as age, gender, polypharmacy, and hospital stay of the patients. We identified 53 interacting-combinations that were present in total 5109 pDDIs with median number of 02 pDDIs per patient. Overall, 91.6% patients had at least one pDDI; 86.3% were having at least one major pDDI, and 84.5% patients had at least one moderate pDDI. Among 5109 identified pDDIs, most were of moderate (55%) or major severity (45%); established (24.2%), theoretical (18.8%) or probable (57%) type of scientific evidence. Top 10 common pDDIs included 3 major and 7 moderate interactions. Results obtained by multivariate logistic regression revealed a significant association of the occurrence of pDDIs in patient with age of 60 years or more (p < 0.001), hospital stay of 7 days or longer (p < 0.001) and taking 7 or more drugs (p < 0.001). We found a high prevalence for pDDIs in the Department of Cardiology, most of which were of moderate severity. Older patients, patients with longer hospital stay and with elevated number of prescribed drugs were at higher risk of pDDIs.

Journal ArticleDOI
TL;DR: A background into phosphorus homoeostasis is provided and some of the most important reasons for failure to control hyperphosphatemia are covered with emphasis on the effect of the gastric pH on phosphate binders efficiency.
Abstract: Hyperphosphatemia in chronic kidney disease (CKD) patients is a potentially life altering condition that can lead to cardiovascular calcification, metabolic bone disease (renal osteodystrophy) and the development of secondary hyperparathyroidism (SHPT). It is also associated with increased prevalence of cardiovascular diseases and mortality rates. To effectively manage hyperphosphatemia in CKD patients it is important to not only consider pharmacological and nonpharmacological treatment options but also to understand the underlying physiologic pathways involved in phosphorus homoeostasis. This review will therefore provide both a background into phosphorus homoeostasis and the management of hyperphosphatemia in CKD patients. In addition, it will cover some of the most important reasons for failure to control hyperphosphatemia with emphasis on the effect of the gastric pH on phosphate binders efficiency.

Journal ArticleDOI
TL;DR: Three substituted-imidazolidine derivatives possess promising anti-inflammatory and analgesic actions and displayed superior GI safety profile with respect to the positive control, Indomethacin.
Abstract: The aim of this study was to design and synthesize pharmaceutical agents containing imidazolidine heterocyclic ring in the hope of developing potent, safe and orally active anti-inflammatory agents. A number of substituted-imidazolidine derivatives (3a–k) were synthesized starting from ethylene diamine and aromatic aldehydes. The imidazolidine derivatives (3a–k) were investigated for their anticipated anti-inflammatory, and analgesic activity in Wistar albino rats and Swiss albino mice, respectively. Bioactivity score, molecular and pharmacokinetic properties of the imidazolidine derivatives were calculated by online computer software programs viz. Molinspiration and Osiris property explorer. The results of biological testing indicated that among the synthesized compounds only three imidazolidine derivatives namely 4-[1,3-Bis(2,6-dichlorobenzyl)-2-imidazolidinyl]phenyl-diethylamine (3g), 4-[1,3-Bis(3-hydroxy-4-methoxybenzyl)-2-imidazolidinyl]phenyl-diethylamine (3i) and 4-(1,3-Bis(4-methoxybenzyl)-4-methylimidazolidin-2-yl)-phenyl-diethylamine (3j) possess promising anti-inflammatory and analgesic actions. Additionally these derivatives displayed superior GI safety profile (low severity index) with respect to the positive control, Indomethacin. All synthesized compounds showed promising bioactivity score for drug targets by Molinspiration software. Almost all the compounds were predicted to have very low toxicity risk by Osiris online software. Compound number (3i) emerged as a potential candidate for further research as it obeyed Lipinski’s rule of five for drug likeness, exhibited promising biological activity in-vivo and showed no risk of toxicity in computer aided screening.

Journal ArticleDOI
TL;DR: A review on some exemplary and progressing research studies with either scalability as their objective or upscaling as their future scope may smoothen the future upscaled attempts in this field of nanocrystal technology.
Abstract: Drug nanocrystals comprise unique drug delivery platforms playing a significantly important and distinctive role in drug delivery and as such, the industry and academia are spending a lot of their time and money in developing the nanocrystal products. The current research works in this field depict a vivid shift from lab scale optimization studies to scale up focused studies. In this emerging scenario of nanocrystal technology, a review on some exemplary and progressing research studies with either scalability as their objective or upscaling as their future scope may smoothen the future upscaling attempts in this field. Hence, this paper reviews the efforts of such research works as case studies since an analysis of such research studies may input certain beneficial knowledge to carry out more scale up based research works on nanocrystals.

Journal ArticleDOI
TL;DR: In this paper, groups of multifunctional polymers used in drug dosage form technology were classified and evaluated, and special emphasis was placed on the advantages of using them when designing new drug.
Abstract: In the article, groups of multifunctional polymers used in drug dosage form technology were classified and evaluated. These compounds, in addition to their basic function as excipients, may have additional properties, e.g. stimuli sensitivity, enzyme inhibition, intestinal epithelium penetration enhancement, efflux pump inhibition, taste-masking, pharmacological activity and the ability to interact with enzymes responsible for drug metabolism. While classifying specific groups of multifunctional polymers, special emphasis was placed on the advantages of using them when designing new drug. Such advantages include, i.a., increasing substance bioavailability, improving substance stability during formulation and the possibility of obtaining forms of controlled or localized release to a specific site in the organism.

Journal ArticleDOI
TL;DR: Evidence based pharmaceutical care is a natural and logical emerging concept in the modern pharmacy practice to achieve high quality and more effective pharmaceutical care but still more efforts and resources are needed to promote new attitude toward more professional career.
Abstract: Introduction Pharmacy is a very dynamic profession and the role of the pharmacist is improving with the expansion of the scope of services and the introduction of new subspecialties over time. Moving from being medication dispensers to outcome-oriented and patient-focused care providers; pharmacists will carry more responsibility and commitment to improve their knowledge and practice. Being updated and evidence-based is a key tool to achieve effective pharmaceutical care services. The primary purpose of this article is to highlight the concept of “evidence based pharmaceutical care” as professional practice to improve the quality of pharmaceutical care. Methods Literature for relevant evidence was searched by Medline (through PubMed), Cochrane library using the keywords: pharmaceutical care, evidence-based and pharmacy practice. Also a manual search through major journals for articles referenced in those located through PubMed was done. Results and discussion There is strong data showing that pharmaceutical care lead to improvement in health outcomes and cost-effective therapy. More efforts, policies and qualified staff are needed to establish the “evidence-based pharmaceutical care” as new daily professional practice. Evidence to support pharmacists in their emerging role as care providers is available to improve the efficacy and quality of pharmaceutical care. Education and specialized training practicing evidence based approach are vital to prepare pharmacists to provide high quality pharmaceutical care. Conclusion As care providers, pharmacists are effective in providing high quality patient care and being members in multidisciplinary clinical teams is needed to give them the opportunity. Evidence based pharmaceutical care is a natural and logical emerging concept in the modern pharmacy practice to achieve high quality and more effective pharmaceutical care but still more efforts and resources are needed to promote new attitude toward more professional career.

Journal ArticleDOI
TL;DR: This review concerns about different types of plants that retain the immune stimulating and anti-tumor properties of Allium sativum, Echinacea, Curcuma longa, Arctium lappa, Camellia sinensis, Panax ginseng and Flax seed.
Abstract: For centuries, herbs and plants have been used for medicinal purposes and as food as well. This review concerns about different types of plants that retain the immune stimulating and anti-tumor properties. Large variety of active phytochemicals such as carotenoids, flavonoids, ligands, polyphenolics, terpenoids, sulfides, lignans and plant sterols has been identified in different types of herbs. These phytochemicals have different mechanisms of action. They either stimulate the protective enzyme like glutathione transferase or prevent the cell proliferation. This review has centered on the biochemical properties of Allium sativum, Echinacea, Curcuma longa, Arctium lappa, Camellia sinensis, Panax ginseng and Flax seed. Extracts and juices of Withania somnifera, Amoora rohituka, Dysoxylum binectariferum and Vaccinium macrocarpon, respectively also used as anti-breast cancer. The volatile oils and extracts of these herbs and plants inhibit the synthesis of mevalonate that lessen the tumor growth and cholesterol synthesis.

Journal ArticleDOI
TL;DR: The study has demonstrated the potential of blended hydrophilic polymers in the design and optimization of extended release matrix tablets for soluble and poorly soluble drugs by direct compression.
Abstract: The study was aimed at developing extended release matrix tablets of poorly water-soluble diclofenac sodium and highly water-soluble metformin hydrochloride by direct compression using cashew gum, xanthan gum and hydroxypropylmethylcellulose (HPMC) as release retardants. The suitability of light grade cashew gum as a direct compression excipient was studied using the SeDeM Diagram Expert System. Thirteen tablet formulations of diclofenac sodium (∼100 mg) and metformin hydrochloride (∼200 mg) were prepared with varying amounts of cashew gum, xanthan gum and HPMC by direct compression. The flow properties of blended powders and the uniformity of weight, crushing strength, friability, swelling index and drug content of compressed tablets were determined. In vitro drug release studies of the matrix tablets were conducted in phosphate buffer (diclofenac: pH 7.4; metformin: pH 6.8) and the kinetics of drug release was determined by fitting the release data to five kinetic models. Cashew gum was found to be suitable for direct compression, having a good compressibility index (ICG) value of 5.173. The diclofenac and metformin matrix tablets produced generally possessed fairly good physical properties. Tablet swelling and drug release in aqueous medium were dependent on the type and amount of release retarding polymer and the solubility of drug used. Extended release of diclofenac (∼24 h) and metformin (∼8-12 h) from the matrix tablets in aqueous medium was achieved using various blends of the polymers. Drug release from diclofenac tablets fitted zero order, first order or Higuchi model while release from metformin tablets followed Higuchi or Hixson-Crowell model. The mechanism of release of the two drugs was mostly through Fickian diffusion and anomalous non-Fickian diffusion. The study has demonstrated the potential of blended hydrophilic polymers in the design and optimization of extended release matrix tablets for soluble and poorly soluble drugs by direct compression.

Journal ArticleDOI
TL;DR: MTT assay and measurement of LDH release suggest that necrosis is the form of cellular death predominates in H9c2 cells exposed to high doses of DOX, while for weak doses apoptosis could be the predominate form.
Abstract: The use of doxorubicin (DOX) is limited by its dose-dependent cardiotoxicity Entrapped DOX in liposome has been shown to reduce cardiotoxicity Results showed that about 92% of the total drug was encapsulated in liposome The release experiments showed a weak DOX leakage in both culture medium and in PBS, more than 98% and 90% of the encapsulated DOX respectively was still retained in liposomes after 24 h of incubation When the release experiments were carried out in phosphate buffer pH53, the leakage of DOX from liposomes reached 37% after 24 h of incubation Evaluation of cellular uptake of the liposomal DOX indicated the possible endocytosis of liposomes because the majority of visible fluorescence of DOX was mainly in the cytoplasm, whereas the nuclear compartment showed a weak intensity When using unloaded fluorescent-liposomes, the fluorescence was absent in nuclei suggests that liposomes cannot cross the nuclear membrane MTT assay and measurement of LDH release suggest that necrosis is the form of cellular death predominates in H9c2 cells exposed to high doses of DOX, while for weak doses apoptosis could be the predominate form Entrapped DOX reduced significantly DOX toxicity after 3 and 6 h of incubation, but after 20 h entrapped DOX is more toxic than free one

Journal ArticleDOI
TL;DR: The flux and apparent permeability coefficient in intestine from OLM nanosuspension was higher than the plain drug, thereby suggesting better drug delivery.
Abstract: The purpose of this study was to develop nanosuspension based on combinative technology to enhance the intestinal absorption of Olmesartan medoxomil (OLM), a potent antihypertensive agent with limited oral bioavailability. Two combinative approaches were employed and then characterized. In vitro intestinal absorption of OLM nanosuspension and plain OLM was studied using non-everted rat intestinal sac model. Optimal OLM nanosuspension was prepared by a combination of ball milling and probe sonication using stabilizer, Poloxamer 407. The formula exhibited particle size of 469.9 nm and zeta potential of −19.1 mV, which was subjected to ex vivo studies. The flux and apparent permeability coefficient in intestine from OLM nanosuspension was higher than the plain drug, thereby suggesting better drug delivery.

Journal ArticleDOI
TL;DR: There is a need to develop a high quality assessment tool which can meticulously establish suitable diagnostic criteria for ADRs with universal acceptance to improvise the fundamental aspect of drug safety and evade the impendingADRs with the motive to convert Pharmacovigilance into a state of art.
Abstract: Importance: Basic essence of Pharmacovigilance is prevention of ADRs and its precise diagnosis is crucially a primary step, which still remains a challenge among clinicians. Objective: This study is undertaken with the objective to scrutinize and offer a notion of commonly used as well as recently developed methods of causality assessment tools for the diagnosis of adverse drug reactions and discuss their pros and cons. Evidence review: Overall 49 studies were recognized for all assessment methods with five major decisive factors of causality evaluation, all the information regarding reasons allocating causality, the advantages and limitations of the appraisal methods were extracted and scrutinized. Findings: From epidemiological information a past prospect is designed and subsequent possibility merged this background information with a clue in the individual case to crop up with an approximation of causation. Expert judgment is typically based on the decisive factor on which algorithms are based, nevertheless in imprecise manner. The probabilistic methods use the similar principle; however connect probabilities to each measure. Such approaches are quite skeptical and liable to generate cloudy causation results. Causation is quite intricate to ascertain than correlation in Pharmacovigilance due to numerous inherent shortcomings in causality assessment tools. Conclusions and relevance: We suggest that there is a need to develop a high quality assessment tool which can meticulously establish suitable diagnostic criteria for ADRs with universal acceptance to improvise the fundamental aspect of drug safety and evade the impending ADRs with the motive to convert Pharmacovigilance into a state of art.

Journal ArticleDOI
TL;DR: The analgesic activity and antimicrobial screening of the test compounds 2a–x, 4a–c and 5 revealed moderate activity in comparison to reference drugs and the LD50 of compounds 2e and 2v was determined.
Abstract: In continuation to our previous work, thiazolopyrimidines 2a-x were synthesized through intramolecular cyclization of 2-phenacylthio-dihydropyrimidine hydrobromides 1a-x using polyphosphoric acid. On the other hand, thiazolo[3,2-a]pyrimidine-3-one 3 was coupled with aryldiazonium salts or condensed with isatin to afford compounds 4a-c or 5, respectively. Chemical structure of the target compounds was substantiated by IR, FT-IR, (1)H-, (13)C and DEPT-(13)C NMR, MS as well as microanalyses. Moreover, the lipophilicity of the target compounds is expressed as Clog P. The antimicrobial screening of the test compounds 2a-x, 4a-c and 5 revealed moderate activity in comparison to reference drugs. Compounds 2a-c, 2e, 2o and 2v showed a gradual increase in their anti-inflammatory activity reaching its maximum at 5 h compared to indomethacin. Furthermore, the analgesic activity of compounds 2a-c, 2e, 2o and 2v revealed a maximum activity after 5 h of injection compared to aspirin and the LD50 of compounds 2e and 2v was determined.

Journal ArticleDOI
TL;DR: Strategic and interventions are desirable to promote RUM and minimize the consequences of poly-pharmacy in main government hospitals in four emirates in UAE.
Abstract: Rational: Studies conducted showed that there were gaps regarding the rational use of medicines (RUM). Aims and objectives: Evaluate RUM in main government hospitals in four emirates in UAE, using WHO prescribing indicators. Method: Multicenter prospective cross-sectional comparative study was conducted in 4 hospitals in 4 different Emirates in UAE. Using consecutive random sampling method, a total of 1100 prescriptions (2741 prescribed drugs) were collected and analyzed from surveyed hospitals from April to October 2012. Index of Rational Drug Prescribing (IRDP) was used as an indicator of RUM. Results: The main finding of this study was that, the mean values of prescribing indicators of RUM in the surveyed hospitals were estimated to be within the WHO optimal values for generics (100.0 vs. 100.0), antibiotics (9.8 ± 4.8 vs. ⩽30), injections (3.14 ± 1.7 vs. ⩽10) and formulary (EML) prescribing (100.0 vs. 100.0). However, the only discrepancy was reported regarding the number of drugs per prescription which was found to be more than the WHO optimal value (2.49 ± 0.9 vs. ⩽2); respectively. The mean IRDP was 4.55 which was less than the WHO optimal value of 5. Conclusions: Strategies and interventions are desirable to promote RUM and minimize the consequences of poly-pharmacy.

Journal ArticleDOI
TL;DR: Various aspects of oral midazolam, ketamine and their combinations in conscious sedation including, advantages of oral route of sedation, pharmacokinetics, range of oral doses, and antagonists for clinical dental treatment procedures are discussed.
Abstract: For fearful and uncooperative children behavioral management techniques are used. In order to control the pain and anxiety in pedodontic patients, pharmacologic sedation, anesthesia and analgesia are commonly used. Midazolam is commonly used as an oral sedation agent in children; it has several features such as safety of use, quick onset and certain degree of amnesia that makes it a desirable sedation agent in children. This review paper discusses various aspects of oral midazolam, ketamine and their combinations in conscious sedation including, advantages of oral route of sedation, pharmacokinetics, range of oral doses, and antagonists for clinical dental treatment procedures.

Journal ArticleDOI
TL;DR: The roles of community pharmacists in Abu Dhabi Emirate, United Arab Emirates are reviewed in an attempt to adapt to the changes occurring and to the growing needs of patients and to maximize the utilization ofcommunity pharmacists’ unique structured strategies are needed.
Abstract: Background: The pharmaceutical care and ‘extended’ roles are still not practiced optimally by community pharmacists. Several studies have discussed the practice of community pharmacy in the UAE and have shown that most community pharmacists only counsel patients. However, UAE, has taken initiatives to allow and prepare community pharmacists to practice ‘extended’ roles. Aim of the review: The aim was to review the current roles of community pharmacists in Abu Dhabi Emirate, United Arab Emirates (UAE). Objective: The objective was to encourage community pharmacists toward extending their practice roles. Methods: In 2010, Health Authority Abu Dhabi (HAAD) surveyed community pharmacists, using an online questionnaire, on their preferences toward extending their counseling roles and their opinion of the greatest challenge facing the extension of their counseling roles. Results: Following this survey, several programs have been developed to prepare community pharmacists to undertake these extended counseling roles. In addition to that, HAAD redefined the scope of pharmacist roles to include some extended/enhanced roles. Abu Dhabi Health Services (SEHA) mission is to ensure reliable excellence in healthcare. It has put clear plans to achieve this; these include increasing focus on public health matters, developing and monitoring evidence-based clinical policies, training health professionals to comply with international standards to deliver world-class quality care, among others. Prior to making further plans to extend community pharmacists’ roles, and to ensure the success of these plans, it is imperative to establish the views of community pharmacists in Abu Dhabi on practicing extended roles and to gain understanding and information on what pharmacists see as preferred change strategies or facilitators to change. Conclusions: In an attempt to adapt to the changes occurring and to the growing needs of patients and to maximize the utilization of community pharmacists’ unique structured strategies are needed to be introduced to the community pharmacy profession.

Journal ArticleDOI
TL;DR: It was established that no association was found between adherence to warfarin therapy and INR control groups, and the demographic background influences adherence and InR control, but no link was found with adherence and anticoagulation control.
Abstract: Warfarin is a commonly prescribed oral anticoagulant in Saudi Arabia and yet patient adherence to warfarin therapy and its impact on anticoagulation control have not been well researched here. A cross-sectional survey was conducted over 6 weeks at the outpatient anticoagulant clinic on patients who were receiving warfarin. Adherence was assessed using the translated Arabic version of the Morisky Medication Adherence Scale (MMAS-8). Levels of adherence were classed as low (score ⩽ 7), or high (score = 8) based on the scores. Good anticoagulation control was defined as percent Time INR in Therapeutic Range (TTR) ⩾ 75% using the Rosendaal method. A total of 192 patients completed a questionnaire with a response rate of 68.1%. It was established that no association was found between adherence to warfarin therapy and INR control groups. Among the 89 (46.4%) patients who had high adherence, only 34 (38.2%) had an acceptable INR control. This was versus 103 (53.6%) patients who had low adherence but also 34 (33.0%) had good INR control. Multivariate logistic regression (MLR) analysis showed that when studying females and occupational status of unemployment, they were independently associated with poor INR control with an OR 2.31, 95% CI 1.10–4.92, and OR 2.71, 95% CI 1.12–6.61 respectively. MLR analysis also showed that age <50 years alongside no formal education was independently associated with low adherence to warfarin therapy with an OR 2.67, 95% CI 1.29–5.52 and OR 2.63, 95% CI 1.01–6.93 respectively. The demographic background influences adherence and INR control, but no association was found between adherence and anticoagulation control.

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TL;DR: This review summarized multidisciplinary application of biomedical microelectromechanical systems in drug delivery and its potential in analytical procedures.
Abstract: Advancement in microelectromechanical system has facilitated the microfabrication of polymeric substrates and the development of the novel class of controlled drug delivery devices. These vehicles have specifically tailored three dimensional physical and chemical features which together, provide the capacity to target cell, stimulate unidirectional controlled release of therapeutics and augment permeation across the barriers. Apart from drug delivery devices microfabrication technology's offer exciting prospects to generate biomimetic gastrointestinal tract models. BioMEMS are capable of analysing biochemical liquid sample like solution of metabolites, macromolecules, proteins, nucleic acid, cells and viruses. This review summarized multidisciplinary application of biomedical microelectromechanical systems in drug delivery and its potential in analytical procedures.

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TL;DR: The drug safety concept has earned a lot of attention during the past decade due to the fact it plays a major role in patients’ health and recent laws stress this concept should be included in the process of new medications’ approval and continued conduct of post-marketing drug evaluations.
Abstract: Background Drug safety is one of the hottest topics in daily medical practice, particularly with regard to approving new medication or questioning the possibility of withdrawing a drug from the market.

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TL;DR: It is shown that sun awareness and protection are generally inadequate in the Saudi population and suggests the need for health education programs.
Abstract: Background: Many international studies have been conducted to assess the knowledge, attitudes and practices (KAP) of the public toward sun exposure and sun-protection measures. However, there are scarce data on these factors from the Middle East. Objectives: This study aimed to explore the KAP of the public toward sun exposure and sun-protection measures among Saudis. Methods: A cross-sectional survey using a specially designed questionnaire was conducted on a stratified random sample of the general population in the five geographical regions of Saudi Arabia (central, eastern, northern, southern, and western). Data were collected between October 2010 and March 2011. Multiple logistic regressions were applied to relate the use of sunscreen and skin cancer awareness with various socio-demographic variables. Results: The questionnaire was distributed to 2900 Saudis. A total of 2622 questionnaires were completed, returned, and included in the data analysis, corresponding to a response rate of 90.4%. The mean (SD) age of respondents was 27.8 ± 9.7 years. Fifty percent (1301/1601) of the respondents were males. Fifty-five percent (1406/2544) were aware of the association between sun exposure and skin cancer. Female, young and student respondents were more likely to be aware of the connection between sun exposure and skin cancer (p < 0.001). Likewise, respondents from the middle social class and those with higher education levels were more likely to be informed (p < 0.02). The prevalence of regular sunscreen use among study participants was only 23.7%, and female and employed respondents were more likely to use sunscreen (p < 0.001). Protective clothes were the most commonly used sun protection measure as reported by more than 90% of our participants. Conclusion: This study has shown that sun awareness and protection are generally inadequate in the Saudi population and suggests the need for health education programs.