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Development of New Bexarotene-loaded Mesoporous Silica Systems for Topical Pharmaceutical Formulations.

Abstract
The present study reports the first time use of MCM-41 mesoporous silica as highly efficient carrier for bexarotene - an antineoplastic agent specific for cutaneous T-cell lymphoma treatment. Bexarotene is highly toxic and poor-water soluble, having low bioavailability in the conventional pharmaceutical forms. Comparative uptake of bexarotene on amino-functionalized silica host at various functionalization degrees is discussed in details taking into account all structural features, of matrix as well as properties of the drug molecules. The obtained results proved a successful bexarotene loading on amino-functionalized MCM-41 silica. The bexarotene molecules are adsorbed on the active centers in non-crystalline state proving the major role of the silica amino-functionalization for the drug solubility and bioavailability enhancing. In vitro dissolution tests showed a prolonged release of bexarotene during 12 h, reaching 50% release of loaded active molecules. The prolonged release has been demonstrated to be a result of the presence of aminopropyl groups on the silica pore walls.
AuthorsAurelia Vasile, Maria Ignat, Mirela Fernanda Zaltariov, Liviu Sacarescu, Iulian Stoleriu, Dan Draganescu, Mihai Dumitras, Lacramioara Ochiuz
JournalActa chimica Slovenica (Acta Chim Slov) Vol. 65 Issue 1 Pg. 97-107 (Mar 2018) ISSN: 1318-0207 [Print] Slovenia
PMID29562115 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • MCM-41
  • Water
  • Silicon Dioxide
  • Bexarotene
Topics
  • Adsorption
  • Antineoplastic Agents (chemistry, pharmacology)
  • Bexarotene (chemistry, pharmacology)
  • Biological Availability
  • Delayed-Action Preparations (chemistry)
  • Drug Carriers (chemistry)
  • Drug Compounding (methods)
  • Drug Liberation
  • Nanoparticles (chemistry)
  • Particle Size
  • Porosity
  • Silicon Dioxide (chemistry)
  • Solubility
  • Surface Properties
  • Water

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