Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release

作者：Trombino Sonia; Cassano Roberta^*; Mellace Silvia; Picci Nevio; Loizzo Monica R; Menichini Francesco; Tundis Rosa

来源：Journal of Pharmacy and Pharmacology, 2016, 68(2): 275-281.

DOI：10.1111/jphp.12509

• gemcitabine
• lung cancer
• microspheres
• release
• triterpene saponins

ObjectivesThis study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine.
MethodsTriterpene saponins were derivatized with acrylic acid. The obtained polymerizable product was characterized by Fourier transform infrared to confirm the ester linkage. Then, spherical microparticles were prepared by suspension radical copolymerization and impregnated with gemcitabine.
Key findingsMicrospheres exhibited a mean diameter of 2.7 . The swelling studies showed that particles swell most at pH 6.2, typical of the tumour pathology, than at pH 7.4, miming physiological conditions. The microspheres were loaded with gemcitabine (LE 72.2%). Their release profile showed an initial dot of around 24% and a further release for 24 h.
ConclusionsThis carrier could be potentially release the drug in the lung, as a function of different pHs between tumour cells and healthy, reducing the systemic drug toxicity, allowing the reduction of the doses number, increasing the drug half-life and eliminating the problems related to the fast clearance of gemcitabine administration.

• 出版日期2016-2