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

Aurelia Vasile,Mihai Dumitras,Mirela Fernanda Zaltariov,Iulian Stoleriu,Maria Ignat,Liviu Sacarescu,Lacramioara Ochiuz,Dan Draganescu

doi:10.17344/acsi.2017.3641

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.

Highlights

If a drug provides high therapeutic efficacy, diminished side effects and does not induce unacceptable toxicity levels, it is used in disease treatment
X-ray diffraction (XRD) is an ideal method to identify the material structure, the nanoparticles are of particular case exhibiting drawbacks as shifting of the diffraction peaks resulting in network parameters modification and peak widening as a result of occasional presence of disordered crystallographic phase
For the structural analysis of the studied samples we considered Small-Angle X-ray Scattering (SAXS) (Small Angle X-ray Scattering) technique which is sensitive to the inhomogeneous electronic density

Summary

Introduction

If a drug provides high therapeutic efficacy, diminished side effects and does not induce unacceptable toxicity levels, it is used in disease treatment. These requirements can be accomplished, in the case of the existing medication, by using new administration possibility as transport and controlled delivery systems. Nowadays, due to their advantages as the ability to incorporate lipophilic and hydrophilic substances, low toxicity, extended persistence into the blood stream, the gradual and controlled drug release and safe administration (produces no local inflammatory reaction), as well as the allowance to be used in adequate doses and to target the drug, controlled Drug.

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