As the incidence of diabetes continues to increase in the western world, the prevalence of chronic wounds related to this condition continues to be a major focus of wound care research. Additionally, over 50% of chronic wounds exhibit signs and symptoms that are consistent with localized bacterial biofilms underlying severe infections that contribute to tissue destruction, delayed wound-healing and other serious complications. Most current biomedical approaches for advanced wound care aim at providing antimicrobial protection to the open wound together with a matrix scaffold (often collagen-based) to boost reestablishment of the skin tissue. Therefore, the present review is focused on the efforts that have been made over the past years to find peptides possessing wound-healing properties, towards the development of new and effective wound care treatments for diabetic foot ulcers and other skin and soft tissue infections.

Most drugs currently entering the clinical pipeline for severe malaria therapeutics are of lipophilic nature, with a relatively poor solubility in plasma and large biodistribution volumes. Low amounts of these compounds do consequently accumulate in circulating Plasmodium-infected red blood cells, exhibiting limited antiparasitic activity. These drawbacks can in principle be satisfactorily dealt with by stably encapsulating drugs in targeted nanocarriers. Here this approach has been adapted for its use in immunocompetent mice infected by the Plasmodium yoelii 17XL lethal strain, selected as a model for human blood infections by Plasmodium falciparum. Using immunoliposomes targeted against a surface protein characteristic of the murine erythroid lineage, the protocol has been applied to two novel antimalarial lipophilic drug candidates, an aminoquinoline and an aminoalcohol. Large encapsulation yields of >90% were obtained using a citrate-buffered pH gradient method and the resulting immunoliposomes reached in vivo erythrocyte targeting and retention efficacies of >80%. In P. yoelii-infected mice, the immunoliposomized aminoquinoline succeeded in decreasing blood parasitemia from severe to uncomplicated malaria parasite densities (i.e. from ≥25% to ca. 5%), whereas the same amount of drug encapsulated in non-targeted liposomes had no significant effect on parasite growth. Pharmacokinetic analysis indicated that this good performance was obtained with a rapid clearance of immunoliposomes from the circulation (blood half-life of ca. 2 h), suggesting a potential for improvement of the proposed model.

Ionic liquids derived from active pharmaceutical ingredients may open new perspectives towards low-cost rescuing of classical drugs. Thus, we have synthesized novel ionic liquids derived from the antimalarial drug primaquine, and evaluated them in vitro against three stages of malaria parasites. Results from this unprecedented approach open a new chapter in the history of antimalarial drugs.

Novel 9-aminoacridine derivatives were synthesized by linking the heteroaromatic core to different cinnamic acids through an aminobutyl chain. The test compounds demonstrated mid-nanomolar in vitro activity against erythrocytic stages of the chloroquine-resistant W2 strain of the human malaria parasite Plasmodium falciparum. Two of the most active derivatives also showed in vitro activity against liver-stage Plasmodium berghei, with activity greater than that of the reference liver-stage antimalarial primaquine. The compounds were not toxic to human hepatoma cells at concentrations up to 5 μM. Hence, 9-(N-cinnamoylbutyl)aminoacridines are a new class of leads for prevention and treatment of malaria.

Background/Objectives: Peptides from protein ingredients exhibit key biological activities, including antimicrobial, antihypertensive, antioxidant, anti-inflammatory, analgesic, and immunomodulatory effects. Aligning with the One Health approach, there is growing investment in promoting pet health and well-being. As a result, sustainable functional ingredients are increasingly essential for pet food development. In this work, peptides derived from lactoferrins of different mammalian species were synthesized and their antioxidant, anti-inflammatory, and antihypertensive activities were investigated. Methods: This study examined the antioxidant, anti-inflammatory, antihypertensive activities, and cytotoxicity of bioactive peptides derived from lactoferrins of various mammalian species through spectroscopical methods. The peptides were produced via chemical synthesis (bottom-up approach). Results: Peptides derived from bovine lactoferrin showed the most promising antioxidant and anti-inflammatory activities, whereas those derived from human lactoferrin showed the highest antihypertensive effects and the lowest cytotoxicity. In short, milk-derived peptides with antioxidant, anti-inflammatory, and antihypertensive activity were identified. Conclusions: This motivates further studies to better characterize these peptides, including their properties and pharmacokinetics in vivo, to assess their true potential as nutraceutical agents.