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Evaluation of epirubicin in thermogelling and bioadhesive liquid and solid suppository formulations for rectal administration.
Int J Mol Sci. 2013 Dec 31; 15(1):342-60.IJ

Abstract

Temperature sensitive Pluronic (Plu) and pH-sensitive polyacrylic acid (PAA) were successfully mixed in different ratios to form in situ gelling formulations for colon cancer therapy. The major formulations were prepared as the liquid and solid suppository dosage forms. Epirubicin (Epi) was chosen as a model anticancer drug. In vitro characterization and in vivo pharmacokinetics and therapeutic efficacy of Epi in six Plu/PAA formulations were evaluated. Our in vitro data indicate that Epi in Plu 14%/PAA 0.75% of both solid and liquid suppositories possess significant cytotoxicity, strong bioadhesive force, long-term appropriate suppository base, sustained release, and high accumulation of Epi in rat rectums. These solid and liquid suppositories were retained in the upper rectum of Sprague-Dawley (SD) rats for at least 12 h. An in vivo pharmacokinetic study using SD rats showed that after rectal administration of solid and liquid suppositories, Epi had greater area under the curve and higher relative bioavailability than in a rectal solution. These solid and liquid suppositories exhibited remarkable inhibition on the tumor growth of CT26 bearing Balb/c mice in vivo. Our findings suggest that in situ thermogelling and mucoadhesive suppositories demonstrate a great potential as colon anticancer delivery systems for protracted release of chemotherapeutic agents.

Authors+Show Affiliations

Department of Biological Sciences and Technology, National University of Tainan, Tainan 700, Taiwan. yulilo@mail.nutn.edu.tw.Department of Biological Sciences and Technology, National University of Tainan, Tainan 700, Taiwan. lohograce@gmail.com.Department of Biological Sciences and Technology, National University of Tainan, Tainan 700, Taiwan. hrlin@stust.edu.tw.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24384838

Citation

Lo, Yu-Li, et al. "Evaluation of Epirubicin in Thermogelling and Bioadhesive Liquid and Solid Suppository Formulations for Rectal Administration." International Journal of Molecular Sciences, vol. 15, no. 1, 2013, pp. 342-60.
Lo YL, Lin Y, Lin HR. Evaluation of epirubicin in thermogelling and bioadhesive liquid and solid suppository formulations for rectal administration. Int J Mol Sci. 2013;15(1):342-60.
Lo, Y. L., Lin, Y., & Lin, H. R. (2013). Evaluation of epirubicin in thermogelling and bioadhesive liquid and solid suppository formulations for rectal administration. International Journal of Molecular Sciences, 15(1), 342-60. https://doi.org/10.3390/ijms15010342
Lo YL, Lin Y, Lin HR. Evaluation of Epirubicin in Thermogelling and Bioadhesive Liquid and Solid Suppository Formulations for Rectal Administration. Int J Mol Sci. 2013 Dec 31;15(1):342-60. PubMed PMID: 24384838.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of epirubicin in thermogelling and bioadhesive liquid and solid suppository formulations for rectal administration. AU - Lo,Yu-Li, AU - Lin,Yijun, AU - Lin,Hong-Ru, Y1 - 2013/12/31/ PY - 2013/08/18/received PY - 2013/12/16/revised PY - 2013/12/16/accepted PY - 2014/1/4/entrez PY - 2014/1/5/pubmed PY - 2014/12/19/medline SP - 342 EP - 60 JF - International journal of molecular sciences JO - Int J Mol Sci VL - 15 IS - 1 N2 - Temperature sensitive Pluronic (Plu) and pH-sensitive polyacrylic acid (PAA) were successfully mixed in different ratios to form in situ gelling formulations for colon cancer therapy. The major formulations were prepared as the liquid and solid suppository dosage forms. Epirubicin (Epi) was chosen as a model anticancer drug. In vitro characterization and in vivo pharmacokinetics and therapeutic efficacy of Epi in six Plu/PAA formulations were evaluated. Our in vitro data indicate that Epi in Plu 14%/PAA 0.75% of both solid and liquid suppositories possess significant cytotoxicity, strong bioadhesive force, long-term appropriate suppository base, sustained release, and high accumulation of Epi in rat rectums. These solid and liquid suppositories were retained in the upper rectum of Sprague-Dawley (SD) rats for at least 12 h. An in vivo pharmacokinetic study using SD rats showed that after rectal administration of solid and liquid suppositories, Epi had greater area under the curve and higher relative bioavailability than in a rectal solution. These solid and liquid suppositories exhibited remarkable inhibition on the tumor growth of CT26 bearing Balb/c mice in vivo. Our findings suggest that in situ thermogelling and mucoadhesive suppositories demonstrate a great potential as colon anticancer delivery systems for protracted release of chemotherapeutic agents. SN - 1422-0067 UR - https://www.unboundmedicine.com/medline/citation/24384838/Evaluation_of_epirubicin_in_thermogelling_and_bioadhesive_liquid_and_solid_suppository_formulations_for_rectal_administration_ L2 - https://www.mdpi.com/resolver?pii=ijms15010342 DB - PRIME DP - Unbound Medicine ER -