Shape-Memory Terpolymer Rods with 17-β-estradiol for the Treatment of Neurodegenerative Diseases: an In Vitro and In Vivo Study

Purpose Estradiol (E2)-loaded poly(L-lactide-co-glycolide-trimethylenecarbonate) (P(L-LA:GA:TMC)) rods with shape-memory were developed for the treatment of neurodegenerative diseases. Usefulness of the extrusion method in the obtaining process was also considered. The influence of structural and su...

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Veröffentlicht in:Pharmaceutical research 2016-12, Vol.33 (12), p.2967-2978
Hauptverfasser: Turek, Artur, Olakowska, Edyta, Borecka, Aleksandra, Janeczek, Henryk, Sobota, Michał, Jaworska, Joanna, Kaczmarczyk, Bożena, Jarząbek, Bożena, Gruchlik, Arkadiusz, Libera, Marcin, Liśkiewicz, Arkadiusz, Jędrzejowska-Szypułka, Halina, Kasperczyk, Janusz
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Sprache:eng
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Zusammenfassung:Purpose Estradiol (E2)-loaded poly(L-lactide-co-glycolide-trimethylenecarbonate) (P(L-LA:GA:TMC)) rods with shape-memory were developed for the treatment of neurodegenerative diseases. Usefulness of the extrusion method in the obtaining process was also considered. The influence of structural and surface properties during hydrolytic degradation was developed. The possible therapeutic aspect of rods with E2 was determined. Methods The extruded rods were incubated in a PBS solution (pH 7.4, 37°C, 240 rpm). The amount of released E2 in vitro conditions was estimated by UV-VIS method. The following methods in the degradation of rods were applied: NMR, DSC, FTIR, GPC, SEM, and optical microscopy. Changes in water uptake and weight loss were also determined. In vivo study was performed on rats. Measurements of E2 level were performed before and after ovariectomy of rats using ELISA method. A sample of tissue adjacent to the site of the rod implantation was analysed under an optical microscope. Results A stable and steady degradation process ensured zero-order release of E2. The in vivo study indicated a significant increase in the E2 level in serum after ovariectomy. Moreover, structural and surface features indicated that the extrusion method was appropriate for obtaining E2-loaded rods. Conclusions Shape-memory P(L-LA:GA:TMC) rods with E2 are an adequate proposal for further research in the field of neurological disorders.
ISSN:0724-8741
1573-904X
DOI:10.1007/s11095-016-2019-9