Josef Jampilek1*, Michal Oravec2, Martin Kunes3, Sarka Pospisilova1,4, Alois Cizek4

 

1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 83232 Bratislava, Slovakia
2
Global Change Research Institute CAS, Belidla 986/4a, 60300 Brno, Czech Republic
3Department of Biology, Faculty of Science, University of Hradec Kralove, Jana Koziny 1237, 50003 Hradec Kralove, Czech Republic
4Department of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences, Palackeho 1, 61242 Brno, Czech Republic

 

Human fungal infections generally receive less attention than bacterial and viral diseases, since the incidence of systemic fungal infections is considerably lower than that of superficial infections, however, mortality rates from invasive fungal infections are very high, often exceeding 50%. The increase in the number of fungal infections and the occurrence of new fungal opportunistic species are caused by general immunosuppression of patients. Deep mycoses involving the lungs, abdominal viscera, bones and central nervous system are extremely serious diseases. In general, treatment of various illnesses of brain meets with the problem of impenetrability of the blood–brain barrier, which prevents the passage of many drugs that target the central nervous system1,2.

The rapid development of various nanosystems employed for nano-based drug delivery systems has great potential to facilitate the movement of drugs across all barriers, and thus these drug carriers have been extensively studied as a strategy of direct drug delivery to the CNS3. This contribution is focused on the preparation of nano-based formulations of amphotericin B, one of the most effective but also most toxic and non-bioavailable antifungal drugs, and evaluation of their permeation using an in vivo model of rat brain perfusion and in vitro antifungal effect.

 

This study was supported by the MSMT CZ National Programme for Sustainability (LO1415), National infrastructure CzeCOS (LM2015061) and by the Slovak Research and Development Agency (APVV-0516-12). This contribution utilizes also research results of the CEBV project (ITMS 26240120034).

 

References

1Jampilek, J. Expert Opin. Drug Dis. 2016, 11, 1-9. Potential of agricultural fungicides for antifungal drug discovery.

2Jampilek, J. Future Med. Chem. 2016, 8, 1393-1397. How can we bolster the antifungal drug discovery pipeline?

3Jampilek, J.; Kralova, K. Nano-antimicrobials: Activity, benefits and weaknesses. In: Nanostructures in Therapeutic Medicine, Vol. 2 – Nanostructures for Antimicrobial Therapy. Ficai, A.; Grumezescu, A.M. (Eds.). Elsevier, 2017, Chapter 2,  pp 23- 54.

 

 

Biographic Details

Name: Josef Jampilek

Title: Professor of Medicinal Chemistry

Affiliation, Country: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Bratislava, Slovakia

Phone: +421 250 117 229; E-mail: josef.jampilek@gmail.com

Research interests: Synthesis and structure-activity relationships of heterocyclic compounds as anti-invasive agents; ADME and drug bioavailability