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Liposomes, Exosomes, and Virosomes: From Modeling Complex
Membrane Processes to Medical Diagnostics and Drug Delivery
Poster Abstracts
106
36-POS
Board 18
Newly Synthesized Liposomal Antituberculotic Compounds and Effects on In Vitro Model
Systems
Nikoletta Kósa
1
, Kata Horváti
2
, Barnabás Bocskei-Antal
1
, Szilvia Bosze
2
, Levente Herényi
1
,
István Voszka
1
.
2
MTA− ELTE, Budapest, Hungary.
1
Semmelweis University, Budapest, Hungary,
Introduction
. Liposomes are widely investigated nanocarriers, which are capable for
incorporation of both lipid-soluble and water-soluble drugs. WHO aimed to eradicate TB
disease, which is caused by Mycobacterium tuberculosis bacteria.
Aim.
Preparation and encapsulation of newly synthesized antituberculotic compound into
liposomes. To enhance the encapsulation efficiency and to target intracellular bacteria in the
macrophages.
Methods
.We have prepared two types of liposomes.
Type I. consists of dipalmitoyl phosphatidylcholine (DPPC).
Type II. consists of: dioleoylphosphatidylethanolamine (DOPE), cholesteryl hemisuccinate
(CHEMS) and pegylated distearoyl phosphatidylethanolamine (DSPE-PEG).
We used thin lipid film technology to prepare multilamellar vesicles (MLV) and henceforward
both types were treated with extrusion technique to get small unilamellar vesicles (SUV). The
size distribution of liposomes was determined/measured with dynamic light scattering (DLS).
The change of diameter of vesicles shows the rate of aggregation. The used antituberculotic
compounds were: TB 501, TB 504, TB 505 and TB 515 (chemical structure not published yet).
Encapsulation efficiency was determined by measuring absorbance after size exclusion
chromatography (SEC). Cellular uptake of liposomal compounds and non-encapsulated drugs
was measured by flow cytometry on MonoMac6 human monocytic cell line. Intracellular
fluorescence intensity and forward-scattered light (FSC) of MonoMac6 cells was monitored (488
nm (Coherent Sapphire, 22 mW) laser, which is proportional to the cellular uptake.
Results.
The extrusion method resulted rather uniform and stable vesicles. Encapsulation
efficiency was influenced by the physico-chemical properties of antituberculotic compounds.
The in vitro activity of liposomal antituberculotic compounds was determined on M. tuberculosis
H37Rv culture. Considering that M. tuberculosis is an intracellular pathogen the effect of the
compounds was studied on M. tuberculosis H37Rv infected MonoMac6 human monocytes.
This work was supported by Hungarian Research Fund 104275.