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Controlled release and anti-proliferative effect of imatinib mesylate loaded sporopollenin microcapsules extracted from pollens of Betula pendula

Sargin, Idris, Akyuz, Lalehan, Kaya, Murat, Tan, Gamze, Ceter, Talip, Yildirim, Kevser, Ertosun, Seymanur, Aydin, Gozde Hatun, Topal, Muge
International journal of biological macromolecules 2017
Betula pendula, buffers, colorectal neoplasms, drugs, encapsulation, humans, hydrochloric acid, neoplasm cells, pH, pollen, sporopollenin
Sporopollenin is a promising material for drug encapsulation due to its excellent properties; uniformity in size, non-toxicity, chemically and thermally resilient nature. Herein, morphologically intact sporopollenin microcapsules were extracted from Betula pendula pollens. Cancer therapeutic agent (imatinib mesylate) was loaded into the microcapsules. The encapsulation efficiency by passive loading technique was found to be 21.46%. Release behaviour of the drug from microcapsules was found to be biphasic, with an initial fast release followed by a slower rate of release. Imatinib mesylate release from the drug itself (control) was faster than from imatinib mesylate-loaded sporopollenin microcapsules. The release profiles for both free and entrapped drug samples were significantly slower and more controlled in PBS buffer (pH 7.4) than in HCl (pH 1.2) buffer. Cumulative drug release from IM-MES-loaded sporopollenin microcapsules was found to be 65% within 24h for PBS, whereas release from the control was completed within 1h. Also, a complete dissolution of control in HCl buffer was observed within first 30min. MTT assay revealed that drug-loaded microcapsules were effective on WiDr human colon carcinoma cell line. B. pendula sporopollenin can be suggested as an effective carrier for oral delivery of imatinib mesylate.