The past decade may be considered as revolutionary in the research field focused on the physiological function of macrophages. Unknown subtypes of these cells involved in pathological mechanisms were described recently, and they are considered as potential drug delivery targets. The innate ability to internalize foreign bodies exhibited by macrophages can be employed as a therapeutic strategy. The efficiency of this uptake depends on the size, shape and surface physiochemical properties of the phagocyted objects. Here, we propose a method of preparation and preliminary evaluation of drug-polymer conjugate-based microspheres for macrophage targeted drug delivery. The aim of the study was to identify crucial uptake-enhancing parameters for solid, surface modified particles. A model drug molecule-lamivudine-was conjugated with poly-ε-caprolactone via ring opening polymerization. The conjugate was utilized in a solvent evaporation method technique to form solid particles. Interactions between particles and a model rat alveolar cell line were evaluated by flow cytometry. The polymerization product was characterized by a molecular weight of 3.8 kDa. The surface of the obtained solid drug-loaded cores of a hydrodynamic diameter equal to 2.4 µm was modified with biocompatible polyelectrolytes via a layer-by-layer assembly method. Differences in the internalization efficiency of four particle batches by the model RAW 264.7 cell line suggest that particle diameter and surface hydrophobicity are the most influential parameters in terms of phagocytic uptake.

• MeSH
• fagocytóza MeSH
• fixní kombinace léků MeSH
• kapronáty aplikace a dávkování   chemie   MeSH
• laktony aplikace a dávkování   chemie   MeSH
• lamivudin aplikace a dávkování   chemie   MeSH
• látky proti HIV aplikace a dávkování   chemie   MeSH
• lékové transportní systémy * MeSH
• magnetická rezonanční spektroskopie MeSH
• makrofágy imunologie   metabolismus   MeSH
• mikrosféry MeSH
• myši MeSH
• nosiče léků chemie   MeSH
• polymery metabolismus   MeSH
• RAW 264.7 buňky MeSH
• spektrální analýza MeSH
• viabilita buněk účinky léků   MeSH
• zvířata MeSH
• Check Tag
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

PURPOSE: Series of N,N-dimethylamino acid esters was synthesized to study their transdermal permeation-enhancing potency, biodegradability and reversibility of action. Effects of chirality, linking chain length and polyfluorination were investigated.

• MeSH
• adenin analogy a deriváty   metabolismus   MeSH
• alanin analogy a deriváty   aplikace a dávkování   farmakologie   chemická syntéza   MeSH
• aplikace kožní MeSH
• časové faktory MeSH
• elektrická impedance MeSH
• esterasy metabolismus   MeSH
• farmaceutická chemie MeSH
• financování organizované MeSH
• halogenace MeSH
• hydrokortison metabolismus   MeSH
• hydrolýza MeSH
• indomethacin metabolismus   MeSH
• isomerie MeSH
• kapronáty aplikace a dávkování   farmakologie   chemická syntéza   MeSH
• kožní absorpce účinky léků   MeSH
• kůže metabolismus   účinky léků   MeSH
• methylaminy aplikace a dávkování   farmakologie   chemická syntéza   MeSH
• molekulární struktura MeSH
• nosiče léků MeSH
• organofosfonáty metabolismus   MeSH
• prasata MeSH
• příprava léků MeSH
• stabilita léku MeSH
• theofylin metabolismus   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH