Formulation and optimization of drug-loaded mesoporous silica nanoparticle-based tablets to improve the dissolution rate of the poorly water-soluble drug silymarin

A1 Originalartikel i en vetenskaplig tidskrift (referentgranskad)

Interna författare/redaktörer

Publikationens författare: Ahmed H. Ibrahim, Jan-Henrik Smått, N. Prakirth Govardhanam, Harry M. Ibrahim, Hatem R. Ismael, Mohsen I. Afouna, Ahmed M. Samy, Jessica M. Rosenholm.
Förläggare: Elsevier
Publiceringsår: 2020
Tidskrift: European Journal of Pharmaceutical Sciences
Volym: 142
Artikelns första sida, sidnummer: 1
Artikelns sista sida, sidnummer: 11
ISSN: 0928-0987


Porous carriers have been put forward as a promising alternative for
stabilizing the amorphous state of loaded drugs, and thus significantly
improving the dissolution rate of poorly soluble compounds. The purpose
of this study was to enhance the saturation solubility, dissolution rate
and drug loading of the poorly water-soluble drug silymarin via
incorporation into mesoporous silica nanospheres within a lyophilized
tablet to obtain a unique formulation. 32 full factorial
design was applied to study the effect of both independent variables,
polyvinyl alcohol (PVA) as stabilizer and binder and sucrose as
cryoprotectant and disintegrant; and on the dependent variables that
included the mean particle size (Y1), disintegration time (Y2), tablet strength (Y3) and % of drug release after 2 min, R2min,Y4.
The drug-loaded mesoporous silica nanospheres and the optimized formula
was evaluated by different characterization methods: scanning electron
microscopy, transmission electron microscopy, differential scanning
calorimetry, X-ray diffractometry and Fourier transform infrared
spectroscopy; as well as drug content, saturation solubility and
moisture content. The evaluation demonstrated that the loaded mesoporous
silica nanospheres and the optimized formula are in amorphous state
without any chemical interaction with the silica matrix or the
stabilizer. Moreover, the drug was stably maintained in nanosize range
with narrow particle size distribution. Furthermore, the optimized
lyophilized tablets had highly porous structure, low friability (less
than 1%), fast disintegration (less than 30 s), high tablet strength,
low moisture content (less than 1%), remarkably increased dissolution
rate and noticeable improvement in saturation solubility.


Dissolution, Dissolution kinetics, Dissolution profile, factorial design, mesoporous materials, Mesoporous silica, Micro-Mesoporous material, Poorly soluble drug, Poorly soluble drugs, Poorly water-soluble drugs

Senast uppdaterad 2020-01-10 vid 02:52