The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

Title
The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
Author(s)
김종오김동욱[김동욱]티르거네쉬라마사미최주연김정환용철순최한곤[최한곤]
Keywords
SELF-ASSEMBLED NANOPARTICLES; DRUG-DELIVERY SYSTEM; IN-VITRO EVALUATION; LIQUID SUPPOSITORY; BIOAVAILABILITY; RATS; POLOXAMER; MICELLES
Issue Date
201408
Publisher
DOVE MEDICAL PRESS LTD
Citation
INTERNATIONAL JOURNAL OF NANOMEDICINE, v.9, pp.3815 - 3824
Abstract
The primary aim of this work was to investigate the potential of bile salt, sodium taurocholate (NaTC), in improving the bioavailability and anti-tumor efficacy of docetaxel (DCT) upon rectal administration. Poloxamer-based nanomicelles with thermosensitive and mucoadhesive properties were prepared using the cold method. The optimized nanomicellar formulation was evaluated in terms of physicochemical and viscoelastic parameters. Nanomicelles containing bile salt maintained sufficient gelation strength (234x10(2) mPa.s) and mucoadhesive force (17.3x10(2) dyne/cm(2)) to be retained in the upper part of the rectum. They significantly enhanced the DCT internalization across the rectal mucosa and showed a high plasma level during the first 4 hours of the study period, compared to nanomicelles with no bile salt. As a result, a slightly higher rectal bioavailability of similar to 33% was observed in nanomicelles containing bile salt, compared to similar to 28% from the latter system. The higher pharmacokinetic parameters for rectally administered DCT/P407/P188/Tween 80/NaTC (0.25%/11%/15%/10%/0.1% by weight, respectively) resulted in significant anti-tumor efficacy. However, the tumor regression rate for the NaTC group was not statistically different from that for nanomicelles without NaTC. Therefore, overall results suggest that thermosensitive nanomicelles could be a potential dosage form for improvement of the bioavailability and chemotherapeutic profile of DCT.
URI
http://hdl.handle.net/YU.REPOSITORY/31332http://dx.doi.org/10.2147/IJN.S64794
ISSN
1178-2013
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약학대학 > 약학부 > Articles
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