Mesoporous silica materials: From physico-chemical properties to enhanced dissolution of poorly water-soluble drugs

A2 Review article, Literature review, Systematic review

Internal Authors/Editors

Publication Details

List of Authors: Maleki A, Kettiger H, Schoubben A, Rosenholm JM, Ambrogi V, Hamidi M
Publisher: Elsevier
Publication year: 2017
Journal: Journal of Controlled Release
Volume number: 262
Start page: 329
End page: 347
ISSN: 0168-3659


New approaches in pharmaceutical
chemistry have resulted in more complex drug molecules in the quest to
achieve higher affinity to their targets. However, these ‘highly active’
drugs can also suffer from poor water solubility. Hence, poorly water
soluble drugs became a major challenge in drug formulation,
and this problem is increasing, as currently about 40 of the marketed
drugs and 90% of drug candidates are classified as poorly water soluble.
Various approaches exist to circumvent poor water solubility and poor dissolution rate in aqueous environment, however, each having disadvantages and certain limitations.

Recently, mesoporous silica
materials (MSMs) have been proposed to be used as matrices for
enhancing the apparent solubility and dissolution rate of different drug
molecules. MSMs are ideal candidates for this purpose, as silica is a
“generally regarded as safe” (GRAS) material, is biodegradable, and can
be readily surface-modified in order to optimize drug loading and
subsequent release in the human body. The major advantage of mesoporous silica as drug delivery
systems (DDSs) for poorly water soluble drugs lies in their pore size,
pore morphology, and versatility in alteration of the surface groups,
which can result in optimized interactions between a drug candidate and
MSM carrier by modifying the pore surfaces. Furthermore, the drug of
interest can be loaded into these pores in a preferably amorphous state,
which can increase the drug dissolution properties dramatically.

highlights of this review include a critical discussion about the
modification of the physico-chemical properties of MSMs and how these
physico-chemical modifications influence the drug loading and the
subsequent dissolution of poorly water soluble drugs. It aims to further
promote the use of MSMs as alternative strategy to common methods like
solubility enhancement by cyclodextrins, micronization, or microemulsion techniques. This review can provide guidance on how to tailor MSMs to achieve optimized drug loading and drug dissolution.


Drug delivery, Mesoporous silica

Last updated on 2019-19-04 at 02:06