Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release
| Autor: | Rosa Tundis, Sonia Trombino, Francesco Menichini, Monica Rosa Loizzo, Silvia Mellace, Nevio Picci, Roberta Cassano |
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| Rok vydání: | 2016 |
| Předmět: |
Drug
Antimetabolites Antineoplastic Surface Properties Drug Compounding media_common.quotation_subject Pharmaceutical Science 02 engineering and technology Pharmacology Deoxycytidine Plant Roots Microsphere 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Triterpene Spectroscopy Fourier Transform Infrared Medicine media_common Acrylic acid chemistry.chemical_classification Drug Carriers Chromatography Apiaceae biology business.industry Physospermum Hydrogen-Ion Concentration Saponins 021001 nanoscience & nanotechnology biology.organism_classification Gemcitabine Microspheres Triterpenes Drug Liberation chemistry 030220 oncology & carcinogenesis Swelling medicine.symptom 0210 nano-technology business medicine.drug |
| Zdroj: | Journal of Pharmacy and Pharmacology. 68:275-281 |
| ISSN: | 2042-7158 0022-3573 |
| DOI: | 10.1111/jphp.12509 |
| Popis: | Objectives This 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. Methods Triterpene 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 findings Microspheres exhibited a mean diameter of 2.7 μ. 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. Conclusions This 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. |
| Databáze: | OpenAIRE |
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