Gemcitabine hydrochloride microspheres used for intravesical treatment of superficial bladder cancer: a comprehensive in vitro/ex vivo/in vivo evaluation

Drug Design, Development and Therapy
Sinem Yaprak KaravanaEsra Baloğlu

Abstract

Bladder cancer is responsible for more than 130,000 deaths annually worldwide. Intravesical delivery of chemotherapeutic agents provides effective drug localization to the target area to reduce toxicity and increase efficacy. This study aimed to develop an intravesical delivery system of gemcitabine HCl (Gem-HCl) to provide a sustained-release profile, to prolong residence time, and to enhance its efficiency in the treatment of bladder cancer. For this purpose, bioadhesive microspheres were successfully prepared with average particle size, encapsulation efficiency, and loading capacity of 98.4 µm, 82.657%±5.817%, and 12.501±0.881 mg, respectively. For intravesical administration, bioadhesive microspheres were dispersed in mucoadhesive chitosan or in situ poloxamer gels and characterized in terms of gelation temperature, viscosity, mechanical, syringeability, and bioadhesive and rheological properties. The cytotoxic effects of Gem-HCl solution, Gem-HCl microspheres, and Gem-HCl microsphere-loaded gel formulations were evaluated in two different bladder cancer cell lines: T24 (ATCC HTB4TM) and RT4 (ATCC HTB2TM). According to cell-culture studies, Gem-HCl microsphere-loaded poloxamer gel was more cytotoxic than Gem-HCl microsphere...Continue Reading

Citations

Aug 15, 2020·Expert Opinion on Drug Delivery·Ho Yub YoonYoung Wook Choi
Nov 7, 2019·Pharmaceutics·Kamalika SamantaSubhash C Chauhan
Oct 1, 2019·Current Opinion in Urology·Francesca PisanoJ Palou
Aug 25, 2019·Medical Hypotheses·Ersoy Öksüz, Muhammet Serdar Buğday

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Methods Mentioned

BETA
scanning electron microscopy
light microscopy
rheology
light-microscopy

Software Mentioned

GraphPad Prism

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