Enhanced anti-tumor activity and alleviated hepatotoxicity of clotrimazole-loaded suppository using poloxamer-propylene glycol gel
- Authors
- Yong, Chul Soon; Xuan, Jing Ji; Paek, Seung-Hwan; Oh, Yu-Kyoung; Woo, Jong-Soo; Lee, Mann Hyung; Kim, Jung-Ae; Choi, Han-Gon
- Issue Date
- Sep-2006
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- clotrimazole; poloxamer 188; suppository; melting point; anti-tumor activity; hepatotoxicity
- Citation
- INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.321, no.1-2, pp.56 - 61
- Indexed
- SCIE
SCOPUS
- Journal Title
- INTERNATIONAL JOURNAL OF PHARMACEUTICS
- Volume
- 321
- Number
- 1-2
- Start Page
- 56
- End Page
- 61
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/44682
- DOI
- 10.1016/j.ijpharm.2006.05.023
- ISSN
- 0378-5173
- Abstract
- To develop a novel clotrimazole-loaded poloxamer-based suppository with enhanced anti-tumor activity and alleviated hepatotoxicity, the melting point of various formulations composed of P 188 and propylene glycol were investigated. The dissolution and anti-tumor activity of clotrimazole delivered by the poloxamer-based suppository was performed. Furthermore, the hepatotoxicity of clotrimazole was carried out after its rectal administration compared to oral administration in mice. The poloxamer mixtures composed of P 188 and propylene glycol were homogeneous phases. P 188 greatly affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 188/propylene glycol (70%/30%)] with the melting point of about 32 degrees C was a solid form at room temperature and instantly melted at physiological temperature. The ratio of P 188/propylene glycol greatly affected the dissolution rates of clotrimazole from poloxamer-based suppository. Dissolution mechanism analysis showed the dissolution rate of clotrimazole from poloxamer-based suppositories was independent of the time. The clotrimazole-loaded suppository with P 188 and propylene glycol could not irritate or damage the rectal tissues of rats and gave the improved anti-tumor activity in a dose-dependent manner at mouse. Furthermore, its rectal administration decreased the hepatotoxicity compared to oral administration. Thus, the poloxamer-based solid suppository system with clotrimazole/P 188/propylene glycol was an effective rectal dosage form for the treatment of tumors with alleviated adverse effects. (c) 2006 Elsevier B.V. All rights reserved.
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