4.6 Article

Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties

Journal

ARCHIVES OF PHARMACAL RESEARCH
Volume 36, Issue 12, Pages 1480-1486

Publisher

PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-013-0175-6

Keywords

Docetaxel-loaded thermosensitive liquid suppository; Poloxamer; Gel strength; Gelation temperature; Gelation time; Mucoadhesive force

Funding

  1. Hanyang University [HY-2013-N]

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The main purpose of this work was to optimize the rheological properties of docetaxel (DCT)-loaded thermosensitive liquid suppositories for rectal administration. DCT-loaded liquid suppositories were prepared by a cold method and characterized in terms of physicochemical and viscoelastic properties. Major formulation parameters including poloxamer (P407) and Tween 80 were optimized to adjust the thermogelling and mucoadhesive properties for rectal administration. Notably, the gel strength and mucoadhesive force significantly increased with the increase in these variables. Furthermore, DCT incorporation did not alter the viscoelastic behavior, and the mean particle size of nanomicelles in it was approximately 16 nm with a distinct spherical shape. The formulation existed as liquid at room temperature and transformed into gel at physiological temperature through the reverse gelation phenomenon. Thus, DCT-loaded thermosensitive liquid suppositories [DCT/P407/P188/Tween 80 (0.25/11/15/10 %)] with optimal gel properties were easy to prepare and administer rectally, and might enable the gel to stay in the rectum without getting out from rectum.

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