Pharmaceutical Lipid Formulations of Amphotericin B for the Treatment of Human Leishmaniasis

The first description of a skin lesion, “Delhi button” dates back to Cunningham (1885) who reported the presence, on tissue sections, of bodies of 12.6 μm x 8.8 μm, presumably parasitic macrophages, containing "nucleoid bodies" which he believed to be spores belonging to Mycetozoa. But the first to describe the Leishmania parasite was, in 1898, a young man Russian military surgeon, named Borowsky. He investigated the cause of the "Sart button" at the military hospital in Tashkent. This paper, through the analysis of the studies carried out over the years proposes a description of the different therapeutic strategies for the treatment of leishmaniasis (advantages and criticalities of the same) and in particular an analysis detailed description of Amphotericin B, its mechanisms of action and pharmaceutical formulations, especially liposomal ones

Phytotherapeutic Strategy as a Powerful Approach for the Prevention and Therapy of Alzheimer's Disease

According to the World Health Organization and Alzheimer's Disease International there were about 35.6 million people suffering from dementia in 2010 with an estimated double increase in 2030, triple in 2050, with 7.7 million new cases. per year (1 every 4 seconds) and with an average survival, after diagnosis, of 4-8 years. Alzheimer's disease is generally associated with the elderly and with aging, which is why the symptoms of this disease are often ignored. In reality, Alzheimer's seems to affect people between the ages of 65 and 70, while more precocious and severe cases occur before the age of 65 and aging and stress can only worsen the symptoms. The sex most affected is female. It has been noted that dementia in industrialized countries affects about 8% of people over 65 and rises to over 20% after the age of eighty. This suggests that, very often, different factors such as lifestyle, stress and nutrition influence the speed and onset of this disease. To date, it is now known that the affected organ is the brain, such a complex and fascinating organ, but above all difficult to study and treat due to its complicated structure and organization. In fact, the treatment is based on pharmacological therapies, but although numerous research studies are underway to identify effective therapies in the treatment of dementia, the available interventions have not given definitive solutions to treat 6 this pathology. The therapeutic strategies available for dementias in addition to those of a pharmacological type are: psychosocial and integrated management for continuity of care and also psychotherapeutic support for families. In recent decades, however, we have focused on another aspect of this disease: how to prevent it? And this is where the use of medicinal plants comes into play to prevent and mitigate the onset of this disease. This type of approach is based on the use of medicinal plants; in particular the phytocomplex, contained in them, owes its activity to the synergy between its components. Plants produce secondary metabolites, organic compounds, which unlike the primary ones such as carbohydrates, proteins and fats, do not participate in the normal development and growth of the plant, but are developed by the plant to mediate the relationship with the external environment, carrying out important activities such as facilitate reproduction and therefore attract pollinating insects or act as a deterrent to the external environment. These compounds have very complex chemical structures that can be used as guiding compounds for the discovery of new drugs or for the development of nutraceutical or cosmeceutical remedies. In phytotherapy, medicinal plants that can be used for preventive purposes or as adjuvants in the treatment of Alzheimer's, are identified essentially starting from their antioxidant, anticholinesterase and anti-inflammatory properties, or as very often happens from all three. This paper reviews the plant species used in the prevention of Alzheimer's disease and as adjuvants in the treatment of Alzheimer's

Novel Penicillin-Type Analogues Bearing a Variable Substituted 2-Azetidinone Ring at Position 6: Synthesis and Biological Evaluation

The synthesis and the biological activity of novel semi-synthetic β-lactam compounds containing an azetidinone moiety joined to the amino-nitrogen of the (+)-6-aminopenicillanic acid (6-APA) as new antibacterial agents is reported. The synthesized compounds were screened for their in vitro antimicrobial activity against a panel of Gram positive and Gram negative pathogens and environmental bacteria. Tested compounds displayed good antimicrobial activity against all tested Gram positive bacteria and for Staphylococcus aureus and Staphylococcus epidermidis antimicrobial activity resulted higher than that of the reference antibiotic. Additionally, in vitro cytotoxic screening was also carried out indicating that the compounds do not cause a cell vitality reduction effective at concentration next to and above those shown to be antimicrobial

Metabolic Syndrome and Inflammatory Cytokines in Psoriasis.

Obesity negatively affects the pathological states of chronic inflammation, such as Psoriasis and Psoriatic Arthritis. The inflammatory cytokines released by the adipose tissue determine, in addition to inflammation, a condition of insulin resistance, which is also a comorbidity of psoriasis. The state of chronic inflammation unites both psoriasis and obesity. The first is an autoimmune skin disease, where very thick skin layers are evident due to an abnormal proliferation of keratinocytes; obesity, on the other hand, represents one of the possible comorbidities of psoriasis the simultaneous presence in the same subject of two or more diseases

Carbazoles: Role and Functions in Fighting Diabetes

Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing to their role in the pathogenesis and development of diabetes. Several studies have demonstrated the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation, prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we summarize the latest advances in the synthetic and natural carbazole-containing compounds involved in diabetes pathways

Synthesis of sericin-based conjugates by click chemistry: enhancement of sunitinib bioavailability and cell membrane permeation

Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw material for polypeptide-based drug delivery systems (DDSs). In this paper, it has been employed as pharmaceutical biopolymer for the production of sunitinib–polypeptide conjugate. The synthesis has been carried out by simple click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide as a free radical grafting initiator. The bioconjugate molecular weight (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic characteristics have been studied in order to reveal the presence of grafted sunitinib. In both FT-IR and UV/Vis spectra, signals corresponding to sunitinib functional groups have been identified. Since sunitinib is an anticancer drug characterized by low bioavailability and low permeability, the bioconjugation aimed at their enhancement. In vitro studies demonstrated that bioavailability has been increased to almost 74%, compared with commercial formulation. Also cell membrane permeability has been augmented in in vitro tests, in which membrane models have been used to determine the lipid membrane/physiological fluid partition coefficient (Kp). The log(Kp) value of the bioconjugate was increased to over 4. This effect resulted in a three-fold decrease of IC50 value against MCF-7 cells