Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties

Title
Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties
Author(s)
김종오여우현티르거네쉬라마사미김동욱[김동욱]조혁준김용일조관형용철순최한곤[최한곤]
Keywords
IN-VITRO EVALUATION; P-GLYCOPROTEIN; INCREASED BIOAVAILABILITY; ORAL BIOAVAILABILITY; RATS; POLOXAMER; VIVO; BIODISTRIBUTION; IBUPROFEN; MICELLES
Issue Date
201312
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.36, no.12, pp.1480 - 1486
Abstract
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.
URI
http://hdl.handle.net/YU.REPOSITORY/28303http://dx.doi.org/10.1007/s12272-013-0175-6
ISSN
0253-6269
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약학대학 > 약학부 > Articles
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