Lin Tingsheng, Wu Jinhui, Zhao Xiaozhi, Lian Huibo, Yuan Ahu, Tang Xiaolei, Zhao Sai, Guo Hongqian, Hu Yiqiao
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, 210093, China; The Department of Urology, Nanjing Drum Tower Hospital, The Affiliated Hospital of Nanjing University Medical School, Nanjing, 210093, China; Medical School of Nanjing University, Nanjing, 210093, China.
J Pharm Sci. 2014 Mar;103(3):927-36. doi: 10.1002/jps.23854. Epub 2014 Jan 21.
Drug solution is commonly used in conventional intravesical instillation. However, most of them would be easily eliminated by voiding, which significantly limit their efficacy. Recent advances in intravesical drug delivery are to use hydrogels as drug reservoir to extend the drug residence time in bladder. However, because of the high viscosity of hydrogel, urinary obstruction is usually existed during the intravesical instillation. To overcome these, we developed a floating hydrogel for the delivery of Adriamycin (ADR). The floating hydrogel was made of ADR, thermosensitive polymer (Poloxamer 407) and NaHCO₃, which was liquid at low temperature, whereas formed gel at high temperature. In the presence of H⁺, NaHCO₃ decomposed and produced CO₂ that attached on the surface of hydrogel and helped the hydrogel float on the urine. Hence, the urinary tract will not be blocked. Meanwhile, the encapsulated ADR released in a controlled manner. These results suggest that the floating gel may have promising applications in intravesical therapy for bladder cancer.
药物溶液常用于传统的膀胱内灌注。然而,它们中的大多数会因排尿而容易被排出,这显著限制了它们的疗效。膀胱内给药的最新进展是使用水凝胶作为药物储库,以延长药物在膀胱中的停留时间。然而,由于水凝胶的高粘度,膀胱内灌注期间通常会存在尿路梗阻。为了克服这些问题,我们开发了一种用于递送阿霉素(ADR)的漂浮水凝胶。该漂浮水凝胶由ADR、热敏聚合物(泊洛沙姆407)和NaHCO₃制成,其在低温下为液体,而在高温下形成凝胶。在H⁺存在的情况下,NaHCO₃分解并产生CO₂,CO₂附着在水凝胶表面并帮助水凝胶漂浮在尿液上。因此,尿路不会被阻塞。同时,包封的ADR以可控方式释放。这些结果表明,漂浮凝胶在膀胱癌的膀胱内治疗中可能具有广阔的应用前景。