Dendrimers are nanoscopic compounds, which are monodispersed, and they are generally considered as homogeneous. PAMAM (polyamidoamine) was introduced in 1985, by Donald A. Tomalia, as a new class of polymers, named ‘starburst polymers’. This important contribution of Professor Tomalia opened a new research field involving nanotechnological approaches. From then on, many groups have been using PAMAM for diverse applications in many areas, including biomedical applications. The possibility of either linking drugs and bioactive compounds, or entrapping them into the dendrimer frame can improve many relevant biological properties, such as bioavailability, solubility, and selectivity. Directing groups to reach selective delivery in a specific organ is one of the advanced applications of PAMAM. In this review, structural and safety aspects of PAMAM and its derivatives are discussed, and some relevant applications are briefly presented. Emphasis has been given to gene delivery and targeting drugs, as advanced delivery systems using PAMAM and an incentive for its use on neglected diseases are briefly mentioned.
Malaria and tuberculosis are no longer considered to be neglected diseases by the World Health Organization. However, both are huge challenges and public health problems in the world, which affect poor people, today referred to as neglected populations. In addition, malaria and tuberculosis present the same difficulties regarding the treatment, such as toxicity and the microbial resistance. The increase of Plasmodium resistance to the available drugs along with the insurgence of multidrug-and particularly tuberculosis drug-resistant strains are enough to justify efforts towards the development of novel medicines for both diseases. This literature review provides an overview of the state of the art of antimalarial and antituberculosis chemotherapies, emphasising novel drugs introduced in the pharmaceutical market and the advances in research of new candidates for these diseases, and including some aspects of their mechanism/sites of action.
AbstractBackgroundTuberculosis is a worldwide health concern and isoniazid is considered one of the most used and effective drug for the treatment. Moreover, the “quality” concept must be incorporated into the final pharmaceutical product, according to Quality by Design (QbD) definition. Therefore, the determination of the analytical test conditions is extremely important, and the design of experiments (DoE) becomes a very useful tool.ObjectiveThis paper used the concept of QbD to assist the analytical conditions developments of the isoniazid and its respective prodrug, applying High Performance Liquid Chromatography (HPLC).MethodsHPLC analytical methodologies were developed for isoniazid and its succinoylated derivative. The experimental design was carried out using three analytical parameters at three levels. Four chromatographic responses were studied. The impact of analytical parameters on chromatographic responses was assessed by Pareto chart. Regression models were obtained using multiple regression analysis. DoE analysis was conducted by Minitab® program and the experiments were performed sequentially, varying the factors.ResultsWe identify three main risk parameters: mobile phase (high); flow rate (moderate); and pH of buffer (moderate). The ratio of mobile phase buffer (X2) and mobile phase pH (X3) had a major influence on the peaks resolutions (Y3). The capacity factor for iso-suc (Y1) and isoniazid (Y2) peaks should be from 3-9 and 4-10, respectively. The peaks resolutions between iso-suc and isoniazid (Y3) should be above 2.ConclusionWe designed 27 experiments, obtaining 1.0 mL/min flow rate, 95% of buffer in mobile phase, and pH 7.0 as the best analytical condition.
:The Zika virus (ZIKV) infection is a major public health concern in Brazil and worldwide, being a rapidly
spreading disease with possible severe complications for pregnant women and neonates. There is currently no preventative
therapy or specific treatment available. Within this context, drug repositioning is a very promising approach for the
discovery of new treatment compounds, since old drugs may become new ones. Therefore, this paper aims to perform a
literature mini-review to identify promising compounds to combat this virus. The mechanism of action at the molecular
level and, when possible, the structure-activity relationship of prototypes are discussed. Among the candidates identified,
we highlight sofosbuvir, chloroquine and suramine, which present a higher quantity of experimental data to draw on for
our discussion. The current treatment is palliative, therefore, this study is of paramount importance in identifying drug
candidates useful for combating ZIKV.
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