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Joshua Chou,* Tomoko Ito, Makoto Otsuka, Besim Ben-Nissan, and Bruce Milthorpe
DOI: 10.1002/adhm.201200342
Simvastatin, a cholesterol treatment drug, has been shown
to stimulate bone regeneration. As such, there has been an
increase interest in the development of suitable materials and
systems for the delivery of simvastatin. Like many pharmaceu-
tical drugs, the prescribed methodology for delivering simvas-
tatin is by injection
[1,2]
and oral intake.
[3]
This can sometimes
result in low dosage of the drug being delivered and in most
cases, insufficient amounts to exhibit any significant thera-
peutic effects.
[4]
In the case of simvastatin, studies have shown
that high concentrations of the drug can result in adverse side
effects including liver failure, kidney disease, and rhabdomy-
olysis.
[5]
However, the most common side effects of statins
are skeletal muscle complaints, including clinically important
myositis and rhabdomyolysis.
[6]
Rhabdomyolysis is a clinical
syndrome in which skeletal muscle damage and necrosis leads
to the release of intracellular contents of muscle. The risk of
rhabdomyolysis and other adverse effects of statin use can be
exacerbated by several factors, including compromised hepatic
and renal function, hypothyroidism, diabetes, and concomitant
medications.
[6]
This creates additional challenges in the devel-
opment of a suitable carrier, as the potential system must be
one that possesses controlled release of the drug to reduce or
inhibit the rise of any side effects. The design should allow the
system to function to induce and promote key processes in
regeneration. To date, the most appropriate concentration of
simvastatin to induce bone formation is yet to be determined
but studies conducted by other groups have looked at effects
at various loadings: 2.2 mg,
[7]
0.5 mg;
[8,9]
0.1, 0.5, 1.0, 1.5, and
2.2 mg.
[10]
Furthermore, the development of various carriers
for the delivery of simvastatin has also been investigated: meth-
ylcellulose gel,
[7,9]
collagen bovine matrix,
[8]
gelatin sponge,
[9,10]
polylactic acid/polyglycolic acid copolymer,
[11]
and calcium sul-
phate.
[12,13]
However, with potential serious side effects associ-
ated with its use, the development of a suitable controlled drug
release system is evermore crucial.
A biomimicry approach to regenerative medicine is a newly
emerging field of research. It will enable the production of
better, more effective designs for scaffolds and templates that
can be used to store pharmaceutical drugs and deliver them in
therapeutic amounts. Fossilized coral exoskeleton (calcium car-
bonate; CaCO
3
) possesses unique architectural structures with
interconnected and uniform pore distribution which can poten-
tially assist in more predictable drug loading. Furthermore,
these exoskeleton structures can be hydrothermally converted
into biocompatible calcium phosphate derivatives
[14]
thereby
providing a more predictable dissolution profile depending on
the intended application. As part of the degradation of the mate-
rial, the breakdown of calcium and phosphate ions can provide
the additional supplement for fostering bone formation. With
these factors in mind, the purpose of the present work was to
prepare and evaluate implanted controlled release drug delivery
system of simvastatin using hydrothermally converted beta-
tricalcium phosphate ( β-TCP) to treat osteoporotic mice.
The conversion to β-TCP was confirmed by powder x-ray dif-
fraction analysis ( Figure 1a) with matching peaks compared
with JCPDS database. Scanning electron microscopy images
show a uniform spherical coating around the β-TCP macro-
sphere and this process can be easily reproduced (Figure 1d).
To control the release of simvastatin, an outer apatite layer was
coated on the material (Figure 1c) to slow the release of the drug
( Figure 2a). For the first 96 h there was no significant change in
the release pattern between the coated and uncoated samples.
A reduction in the release of simvastatin was only observed for
the apatite coated samples after 96 h. The similarity with the
initial release is likely due to the release of the drug from the
micropores being filled with the buffer solution. It is anticipated
that only after the initial release of simvastatin do we begin to
observe the slower release of the drug from the delivery system
as observed at 120 and 144 h. A longer duration release study is
needed to study the long term release profile and to determine
Simvastatin-Loaded β-TCP Drug Delivery System Induces
Bone Formation and Prevents Rhabdomyolysis
in OVX Mice
Dr. J. Chou
University of Technology Sydney
School of Medical and Molecular Sciences
Ultimo, Sydney, NSW, 2007, Australia
E-mail: Joshua.chou@uts.edu.au
Dr. T. Ito
Research Institute of Pharmaceutical Science
Faculty of Pharmacy
Musashino University
1–1-20, Shinmachi, Nishi-Tokyo 202–8585 Japan
Prof. M. Otsuka
Research Institute of Pharmaceutical Science
Faculty of Pharmacy
Musashino University
1–1-20, Shinmachi, Nishi-Tokyo 202–8585 Japan
Prof. B. Ben-Nissan
University of Technology Sydney
School of Chemistry and Forensic Sciences
Ultimo, Sydney, NSW, 2007, Australia
Prof. B. Milthorpe
University of Technology Sydney
Faculty of Science (CB04.04.48H)
Ultimo, Sydney, NSW, 2007, Australia
Adv. Healthcare Mater. 2013, 2, 678–681