All

What are you looking for?

All
Projects
Results
Organizations

Quick search

  • Projects supported by TA ČR
  • Excellent projects
  • Projects with the highest public support
  • Current projects

Smart search

  • That is how I find a specific +word
  • That is how I leave the -word out of the results
  • “That is how I can find the whole phrase”

Effects of Membrane PEGylation on Entry and Location of Antifungal Drug Itraconazole and Their Pharmacological Implications

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11110%2F17%3A10362240" target="_blank" >RIV/00216208:11110/17:10362240 - isvavai.cz</a>

  • Result on the web

    <a href="http://dx.doi.org/10.1021/acs.molpharmaceut6b00969" target="_blank" >http://dx.doi.org/10.1021/acs.molpharmaceut6b00969</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1021/acs.molpharmaceut6b00969" target="_blank" >10.1021/acs.molpharmaceut6b00969</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Effects of Membrane PEGylation on Entry and Location of Antifungal Drug Itraconazole and Their Pharmacological Implications

  • Original language description

    Itraconazole (ITZ) is arr antifungal agent used clinically to treat mycotic infections. However, its therapeutic effects are limited by low solubility in aqueous media. Liposome-based delivery systems (LDS) have been proposed as a delivery Mechanism for ITZ to :alleviate this problem. Furthermore, PEGylation, the inclusion in the formulation of a protective &quot;stealth sheath&quot; of poly(ethylene glycol) around carrier particles, is widely used to increase circulation time in the bloodstream and hence efficacy. Together; these themes highlight the importance of mechanistic and structural understanding of incorporation info liposomes both with and without PEGylation because it can provide a potential foundation for the rational design of LDS-based systems for delivery of ITZ, using alternate protective polymers or formulations. Here we have combined atomistic simulations, cryo-TEM, Langmuir film balance, and fluorescence quenching experiments to explore how ITZ interacts with both pristine and PEGylated liposomes. We found that the drug can be incorporated into conventional and PEGylated liposomes for drug, concentrations up to 15 mol % without phase separation. We observed that, in addition to its protective properties, PEGylation significantly increases the stability of liposomes that host ITZ. In a 1-palmitoyl2-oleoyl-sn-glycero-3-phosphocholine (POPC) bilayer without PEGylation, ITZ was found to reside inside the lipid bilayer between the glycerol and the double-bond regions-of POPC, adopting a largely parallel orientation along the membrane surface: In a PEGylated liposome; ITZ partitions mainly to the PEG layer. The results provide a solid basis for further development of liposome-based delivery systems.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10600 - Biological sciences

Result continuities

  • Project

    <a href="/en/project/GBP302%2F12%2FG157" target="_blank" >GBP302/12/G157: Dynamics and Organization of Chromosomes in the Cell Cycle and during Differentiation under Normal and Pathological Conditions</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2017

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Molecular Pharmaceutics

  • ISSN

    1543-8384

  • e-ISSN

  • Volume of the periodical

    14

  • Issue of the periodical within the volume

    4

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    14

  • Pages from-to

    1057-1070

  • UT code for WoS article

    000398426100009

  • EID of the result in the Scopus database

    2-s2.0-85019028641