Fucoidan-Coated Liposomes: A Target System to Deliver the Antimicrobial Drug Usnic Acid to Macrophages Infected with Mycobacterium tuberculosis.

The present study describes the use of fucoidan, a negative sulfated polysaccharide, as a coating material for the development of liposomes targeted to macrophages infected with Mycobacterium tuberculosis. First, fucoidan was chemically modified to obtain a hydrophobized-fucoidan derivative (cholesteryl-fucoidan) using a two-step microwave-assisted (µW) method. The total reaction time was decreased from 14 hours to 1 hour while maintaining the overall yield. Cholesterylfucoidan was then used to prepare surface-modified liposomes containing usnic acid (UA-LipoFuc), an antimicrobial lichen derivative. UA-LipoFuc was evaluated for mean particle size, polydispersity index (PDI), surface charge (ζ), and UA encapsulation efficiency. In addition, a cytotoxicity study, competition assay and an evaluation of antimycobacterial activity against macrophages infected with M. tuberculosis (H37Ra) were performed. When the amount of fucoidan was increased (from 5 to 20 mg), vesicle size increased (from 168 ± 2.82 nm to 1.18 ± 0.01 µm). Changes in from +20 ± 0.41 mV for uncoated liposomes to -5.41 ± 0.23 mV for UA-LipoFuc suggested that the fucoidan was placed on the surface of the liposomes. UA-LipoFuc exhibited a lower IC50 (8.26 ± 1.11 µM) than uncoated liposomes (18.37 ± 3.34 µM), probably due to its higher uptake. UA-LipoFuc5 was internalized through the C-type carbohydrate recognition domain of the cell membrane. Finally, usnic acid, both in its free form and encapsulated in fucoidan-coated liposomes (UA-LipoFuc5), was effective against infected macrophages. Hence, this preliminary investigation suggests that encapsulated usnic acid will aid in further studies related to infected macrophages and may be a potential option for tuberculosis treatment.

Nanocarriers in the Delivery of Hydroxychloroquine to the Respiratory System: An Alternative to COVID-19.

In response to the global outbreak caused by SARS-CoV-2, this article aims to propose the development of nanosystems for the delivery of hydroxychloroquine in the respiratory system to the treatment of COVID-19. A descriptive literature review was conducted, using the descriptors "COVID-19", "Nanotechnology", "Respiratory Syndrome" and "Hydroxychloroquine", in the PubMed, ScienceDirect and SciElo databases. After analyzing the articles according to the inclusion and exclusion criteria, they were divided into 3 sessions: Coronavirus: definitions, classifications and epidemiology, pharmacological aspects of hydroxychloroquine and pharmaceutical nanotechnology in targeting of drugs. We used 131 articles published until July 18, 2020. Hydroxychloroquine seems to promote a reduction in viral load, in vivo studies, preventing the entry of SARS-CoV-2 into lung cells, and the safety of its administration is questioned due to the toxic effects that it can develop, such as retinopathy, hypoglycemia and even cardiotoxicity. Nanosystems for the delivery of drugs in the respiratory system may be a viable alternative for the administration of hydroxychloroquine, which may enhance the therapeutic effect of the drug with a consequent decrease in its toxicity, providing greater safety for implementation in the clinic in the treatment of COVID-19.