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Molecules 2016, 21(6), 712;

A Hydrogel-Based Epirubicin Delivery System for Intravesical Chemotherapy

School of Pharmacy, Kaohsiung Medical University, No.100, Shih-Chuan 1st Road, Sanmin District, Kaohsiung 807, Taiwan
Department of Pathology, E-Da Hospital, I-Shou University, No.1, Yida Road, Yanchao District, Kaohsiung 824, Taiwan
Department of Urology, E-Da Hospital, I-Shou University, No.1, Yida Road, Yanchao District, Kaohsiung 824, Taiwan
Department of Medical Imaging and Radiological Sciences, Chung Shan Medical University, No.110, Sec. 1, Jianguo North Rd., South District., Taichung 402, Taiwan
Department of Occupational Therapy, I-Shou University, No.8, Yida Road, Yanchao District, Kaohsiung 824, Taiwan
Department of Pharmacy, E-Da Hospital, I-Shou University, No.1, Yida Road, Yanchao District, Kaohsiung 824, Taiwan
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 20 March 2016 / Revised: 15 May 2016 / Accepted: 26 May 2016 / Published: 1 June 2016
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [8593 KB, uploaded 1 June 2016]   |  


This study aimed to examine the efficacy of epirubicin-loaded gelatin hydrogel (EPI-H) in the treatment of superficial urothelium carcinoma. Hydrogel was prepared by Schiff base-crosslinking of gelatin with glutaraldehyde. EPI-H exhibited high entrapment efficiency (59.87% ± 0.51%). EPI-H also increased epirubicin accumulation in AY-27 cells when compared with the effect of aqueous solutions of epirubicin (EPI-AQ); respective epirubicin-positive cell counts were 69.0% ± 7.6% and 38.3% ± 5.8%. EPI-H also exhibited greater cytotoxicity against AY-27 cells than that of EPI-AQ; IC50 values were 13.1 ± 1.1 and 7.5 ± 0.3 μg/mL, respectively. Cystometrograms showed that EPI-H reduced peak micturition, threshold pressures, and micturition duration, and that it increased bladder compliance more so than EPI-AQ. EPI-H enhanced epirubicin penetration into basal cells of urothelium in vivo, whereas EPI-AQ did so only to the umbrella cells. EPI-H inhibited tumor growth upon intravesical instillation to tumor-bearing bladder of F344 rats, inducing higher levels of caspase-3 expression than that observed with EPI-AQ treatment; the number of caspase-3 positive cells in treated urothelium carcinoma was 13.9% ± 4.0% (EPI-AQ) and 34.1% ± 1.0%, (EPI-H). EPI-H has value as an improved means to administer epirubicin in intravesical instillation treatments for bladder cancer. View Full-Text
Keywords: epirubicin; hydrogel; intravesical; bladder cancer epirubicin; hydrogel; intravesical; bladder cancer

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Liu, C.-W.; Wu, Y.-T.; Lin, K.-J.; Yu, T.-J.; Kuo, Y.-L.; Chang, L.-C. A Hydrogel-Based Epirubicin Delivery System for Intravesical Chemotherapy. Molecules 2016, 21, 712.

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