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2018 ; 8
(1
): 3929
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Development of an Injectable Slow-Release Metformin Formulation and Evaluation of
Its Potential Antitumor Effects
#MMPMID29500390
Baldassari S
; Solari A
; Zuccari G
; Drava G
; Pastorino S
; Fucile C
; Marini V
; Daga A
; Pattarozzi A
; Ratto A
; Ferrari A
; Mattioli F
; Barbieri F
; Caviglioli G
; Florio T
Sci Rep
2018[Mar]; 8
(1
): 3929
PMID29500390
show ga
Metformin is an antidiabetic drug which possesses antiproliferative activity in
cancer cells when administered at high doses, due to its unfavorable
pharmacokinetics. The aim of this work was to develop a pharmacological tool for
the release of metformin in proximity of the tumor, allowing high local
concentrations, and to demonstrate the in vivo antitumor efficacy after a
prolonged metformin exposition. A 1.2% w/w metformin thermoresponsive parenteral
formulation based on poloxamers P407 and P124, injectable at room temperature and
undergoing a sol-gel transition at body temperature, has been developed and
optimized for rheological, thermal and release control properties; the
formulation is easily scalable, and proved to be stable during a 1-month storage
at 5?°C. Using NOD/SCID mice pseudo-orthotopically grafted with MDA-MB-231/luc(+)
human breast cancer cells, we report that multiple administrations of 100?mg of
the optimized metformin formulation close to the tumor site cause tissue
accumulation of the drug at levels significantly higher than those observed in
plasma, and enough to exert antiproliferative and pro-apoptotic activities. Our
results demonstrate that this formulation is endowed with good stability,
tolerability, thermal and rheological properties, representing a novel tool to be
pursued in further investigations for adjuvant cancer treatment.
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