Abstract Background Bipolar disorder confers the highest risk of suicide among major psychological disorders. The risk factors associated with bipolar disorder and suicide exist and are relevant to ...clinicians and researchers. Objective The aim of the present study was to conduct a systematic review of articles regarding the suicide risk factors in bipolar disorder. Methods A systematic review of articles on suicide risk factors in bipolar disorder, published from January 1, 2010 to April 05, 2014, on SCOPUS and PUBMED databases was carried out. Search terms were “Suicide” (medical subject headings MeSH), “Risk factors” (MeSH), and “Bipolar” (keyword). Of the 220 retrieved studies, 42 met the eligibility criteria. Results Bipolar disorder is associated with an increased rate death by suicide which contributes to overall mortality rates. Studies covered a wide range of aspects regarding suicide risk factors in bipolar disorder, such as risk factors associated to Sociodemographic conditions, Biological characteristics, Drugs Relationships, Psychological Factors, Genetic Compound, Religious and Spirituals conditions. Recent scientific literature regarding the suicide risk factors in bipolar disorder converge to, directly or indirectly, highlight the negative impacts of risk factors to the affected population quality of life. Conclusion This review demonstrated that Bipolar disorders commonly leads to other psychiatric disorders and co-morbidities involving risk of suicide. Thus the risk factors are relevant to have a better diagnosis and prognosis of BD cases involving risk of suicide.
Borneol is a bicyclic monoterpenoid alcohol commonly used in traditional Chinese and Indian medicine. It is extracted from the essential oil of various medicinal plants. It has antibacterial, ...analgesic, and anti-inflammatory action proven in studies that used oral and intraperitoneal applications of this monoterpene in mice. The current study was designed to develop a topical gel formulation containing the monoterpene borneol using carbopol as gel base and to evaluate its stability. The prepared formulation was subjected to physical characterization and physical-chemistry assessment. The gel was prepared from carbopol and 5% of borneol. The prepared gel was subjected to pharmacotechnical tests such as its pH, viscosity, conductivity, spreadability, centrifugation, and accelerated stability with freezing-thaw cycle. The borneol was successfully incorporated into the carbopol formulation. Borneol gel (BG5) showed good stability after eight months of its development and after 12 days in the freeze-thaw cycle, not showing statistical difference in pH value, conductivity, and viscosity before and after test. Furthermore, the formulation showed a good spreadability. Therefore, it was concluded that the formulation could be very promising alternative for the topical or transdermal treatment of skin diseases.
β-Lapachone is an ortho-naphthoquinone originally isolated from the heartwood of Handroanthus impetiginosus and can be obtained through synthesis from lapachol, naphthoquinones, and other aromatic ...compounds. β-Lapachone is well known to inhibit topoisomerase I and to induce NAD(P)H: quinone oxidoreductase 1. Currently, phase II clinical trials are being conducted for the treatment of pancreatic cancer. In view of ever-increasing scientific interest in this naphthoquinone, herein, the authors present a review of the synthesis, physicochemical properties, biological activities, and toxicity of β-lapachone. This natural compound has shown activity against several types of malignant tumors, such as lung and pancreatic cancers and melanoma. Furthermore, this ortho-naphthoquinone has antifungal and antibacterial activities, underscoring its action against resistant microorganisms and providing anti-inflammatory, antiobesity, antioxidant, neuroprotective, nephroprotective, and wound-healing properties. β-Lapachone presents low toxicity, with no signs of toxicity against alveolar macrophages, dermal fibroblast cells, hepatocytes, or kidney cells.
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•The formation of ROS is the primary mechanism of β-lapachone against cancer cells.•The β-lapachone has shown antiviral, antiparasitic and antimicrobial effects.•Anti-inflammatory activities of β-lapachone may be due to synergistic mechanisms.•β-lapachone has potential therapeutic effects on obesity by the fat-browning effect.•β-Lapachone is able to suppress metastasis in vivo by several mechanisms.
Chagas disease (CD), caused by the flagellate protozoan Trypanosoma cruzi, is one of the major public health problems in developing countries. Benznidazole (BNZ) is the only drug available for CD ...treatment in most countries, however, it presents high toxicity and low bioavailability. To address these problems this study used Zeolitic Imidazolate Framework-8 (ZIF-8), which has garnered considerable attention due to its potential applications, enabling the controlled delivery of drugs. The present work developed and characterized a BNZ@ZIF-8 system, and the modulation of BNZ release from the ZIF-8 framework was evaluated through the in vitro dialysis release method under sink conditions at different pH values. Moreover, the in vitro evaluation of cell viability and cytotoxicity by MTT assay were also performed. The dissolution studies corroborated that a pH sensitive Drug Delivery System capable of vectorizing the release of BNZ was developed, may leading to the improvement in the bioavailability of BNZ. The MTT assay showed that no statistically significant toxic effects occurred in the developed system, nor significant effects on cell viability.
The traditional use of the M. charantia L. plant to treat coughs, fever and expectoration is widely practiced in different cultures, but its effectiveness and safety still require scientific ...investigation. This study sought to perform a chemical analysis and evaluate the antitussive, expectorant and antipyretic effects of the ethanolic extract of M. charantia leaves (EEMc) in rats and mice. The EEMc was subjected to chemical analysis by HPLC-DAD, revealing the presence of the flavonoids astragalin and isoquercetin. Acute oral toxicity in mice did not result in deaths, although changes in liver weight and stool consistency were observed. EEMc demonstrated an antitussive effect at doses of 100 and 300 mg/kg in mice subjected to cough induction by citric acid nebulization. Furthermore, it showed expectorant activity at a dose of 300 mg/kg, assessed based on the elimination of the phenol red marker in bronchoalveolar lavage. In the evaluation of antipyretic activity in rats, fever induced by Saccharomyces cerevisiae was reduced at all doses tested during the first hour after treatment. This innovative study identified the presence of astragalin and isoquercetin in EEMc and indicated that the extract has antitussive, expectorant and antipyretic properties.
Lamellar double hydroxides (LDH) are a class of inorganic materials widely used as pharmaceutical ingredients. However, their use as excipients and mainly as drug carriers lacks specific research in ...pharmaceutical technology, as there are no publications capable of defining the behavior of these materials as components of a formulation in the presence of other pharmaceutical adjuvants already consolidated. The purpose of the study was to evaluate the excipient–excipient compatibility of calcium and aluminum LDH (LDH–CaAl) against other excipients, including colloidal silicon dioxide (aerosil
®
), soluble starch (SS), microcrystalline cellulose 101 (MCC), magnesium stearate (MS), hydroxypropyl-beta-cyclodextrin (HPβCD), lactose monohydrate (LACM), sodium starch glycollate (SSG), PVP-K30 and talc. Initially, absorption spectroscopy in the infrared region with Fourier transform (FTIR) and thermogravimetry and differential thermal analysis (TG/DTA) was performed. When signs of possible interactions were observed, X-ray diffraction (XRD) was performed as a complementary technique. At the end of the study, the FTIR spectra and the TG curves of LDH–CaAl and each of the isolated excipients were compared with the analysis of the binary mixtures, where there is compatibility between LDH–CaAl and all excipients tested. Although the XRD has been used to assess evidence of interactions in mixtures with stearate, lactose, PVP and talc, the joint analysis of the results proved to be satisfactory. All these pioneering results suggest, therefore, the acceptability and suitability of LDH–CaAl as a potentially scalable excipient for the development of safe and rational dosage forms.
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Benznidazole (BNZ), the only commercialized antichagasic drug, and the antifungal compound posaconazole (PCZ) have shown synergistic action in the therapy of Chagas disease, however ...both active pharmaceutical ingredients (APIs) exhibit low aqueous solubility potentially limiting their bioavailability and therapeutic efficacy. In this paper, we report for the first time the formation of a eutectic mixture as well as an amorphous solid solution of PCZ and BNZ (at the same characteristic ratio of 80:20wt%), which provided enhanced solubility and dissolution rate for both APIs. This eutectic system was characterized by DSC and the melting points obtained were used for the construction of a phase diagram. The preservation of the characteristic PXRD patterns and the IR spectra of the parent APIs, and the visualization of a characteristic eutectic lamellar crystalline microstructure using Confocal Raman Microscopy confirm this system as a true eutectic mixture. The PXRD result also confirms the amorphous nature of the prepared solid solution. Theoretical chemical analyses indicate the predominance of π-stacking interactions in the amorphous solid solution, whereas an electrostatic interaction between the APIs is responsible for maintaining the alternating lamellar crystalline microstructure in the eutectic mixture. Both the eutectic mixture and the amorphous solid solution happen to have a characteristic PCZ to BNZ ratio similar to that of their pharmacological doses for treating Chagas disease, thus providing a unique therapeutic combination dose with enhanced apparent solubility and dissolution rate.
Schistosomiasis: Drugs used and treatment strategies Siqueira, Lidiany da Paixão; Fontes, Danilo Augusto Ferreira; Aguilera, Cindy Siqueira Britto ...
Acta tropica,
December 2017, 2017-Dec, 2017-12-00, 20171201, Letnik:
176
Journal Article
Recenzirano
•Public politics must be more effective for the endemic control of schistosomiasis.•The number of drugs used to treat NTDs is very small, because that the investment in R&D for such diseases is ...inadequate.•Currently, some pharmaceutical companies have R&D units with major university centers focusing on the neglected diseases.
Neglected tropical diseases (NTDs) affect millions of people in different geographic regions, especially the poorest and most vulnerable. Currently NTDs are prevalent in 149 countries, seventeen of these neglected tropical parasitic diseases are classified as endemic. One of the most important of these diseases is schistosomiasis, also known as bilharzia, a disease caused by the genus Schistosoma. It presents several species, such as Schistosoma haematobium, Schistosoma japonicum and Schistosoma mansoni, the latter being responsible for parasitosis in Brazil. Contamination occurs through exposure to contaminated water in the endemic region. This parasitosis is characterized by being initially asymptomatic, but it is able to evolve into more severe clinical forms, potentially causing death. Globally, more than 200 million people are infected with one of three Schistosome species, including an estimated 40 million women of reproductive age. In Brazil, about 12 million children require preventive chemotherapy with anthelmintic. However, according to the World Health Organization (WHO), only about 15% of the at-risk children receive regular treatment. The lack of investment by the pharmaceutical industry for the development and/or improvement of new pharmaceutical forms, mainly aimed at the pediatric public, is a great challenge. Currently, the main forms of treatment used for schistosomiasis are praziquantel (PZQ) and oxaminiquine (OXA). PZQ is the drug of choice because it presents as a high-spectrum anthelmintic, used in the treatment of all known species of schistosomiasis and some species of cestodes and trematodes. OXA, however, is not active against the three Schistosome species. This work presents a literature review regarding schistosomiasis. It addresses points such as available treatments, the role of the pharmaceutical industry against neglected diseases, and perspectives for treatment.
Pentavalent antimonials are the primary treatment for leishmaniasis due to their proven efficacy and cost-effectiveness. However, they present poor oral absorption, parenteral administration, and ...serious adverse effects due to prolonged use. Nanostructured Lipid Carriers (NLC) offer a promising solution, providing prolonged release, enhanced intestinal permeability, and oral bioavailability. This study aimed to address these issues by developing Nanostructured Lipid Carrier loaded with meglumine antimoniate (NLC-MA) for oral leishmaniasis treatment. We used design of experiments (DoE) for optimization. The chosen NLC-MA was characterized assessing size, polydispersity index (PdI), zeta potential (ZP), entrapment efficiency (EE), pH, and by analytical techniques such as DSC, FTIR, XRD, and TEM. Stability under simulated gastrointestinal conditions, in vitro release kinetics, cytotoxicity in RAW 264.7 macrophages, and leishmanicidal activity were assessed. NLC-MA presented 41.13 nm, PdI 0.227, ZP −27.9 mV, EE of 62.43%, and pH 5.23. Characterization techniques confirmed drug incorporation and nanoparticles with reduced crystallinity. TEM images showed spherical morphology. NLC remained stable in gastrointestinal pH and under refrigeration storage, while lyophilized formulations retained their initial properties. MA release from NLC followed the Peppas-Sahlin model, an anomalous transport mechanism. Importantly, MA showed no cytotoxicity in macrophages, but the NLCs exhibited cytotoxicity beyond 50 µg/mL. NLC-MA displayed improved efficacy against Leishmania infantum. Overall, these results highlight the potential of utilizing a lipid nanocarrier incorporating meglumine antimoniate as an innovative drug delivery platform for oral treatment against leishmaniasis.
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•The design of experiments provided better lipid formulation for the nanoparticle.•Nanostructured Lipid Carrier containing meglumine antimoniate was developed.•Simulated gastric stability of the nanocarrier was observed.•The nanocarrier promoted in vitro release kinetics longer than 48 h.•In vitro leishmanicidal activity was better in the L. infantum specie.
Layered Double Hydroxides (LDH) have received great attention in the development of drug carrier systems. LDHs have become intelligent excipients of high technological potential for the ...pharmaceutical industry due to their ability to intercalate biomaterials in the interlayer region, adsorb substances on its vast surface area, have flexible structure, swelling properties, high chemical and thermal stability, modulate drug release, have high biocompatibility and be easily synthesized. This article, using typical examples, mainly addresses the systems formed between LDHs and antimicrobial, antineoplastic and anti-inflammatory agents, which constitute the main pharmacological classes of wide interest due to the problems encountered with low solubility, control in administration, stability in body fluids and toxicity, among others. Additionally, the article also reports on the recent development of ternary or quaternary (multicomponent systems) compounds based on LDH, bringing the advantages of targeted therapy, improving the aqueous stability of nanohybrids and the performance of these inorganic carriers.
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