Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect

Title
Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect
Author(s)
김종오서윤기김동욱[김동욱]최한곤[최한곤]티르거네쉬라마사미김정환마라시니니르말용철순김진기[김진기]오유경[오유경]김대환
Keywords
IN-VIVO EVALUATION; ORAL BIOAVAILABILITY; PHYSICOCHEMICAL CHARACTERIZATION; MICROEMULSIFYING FORMULATION; INTESTINAL-ABSORPTION; VITRO EVALUATION; NANOPARTICLES; RATS; OPTIMIZATION; MICELLES
Issue Date
201308
Publisher
ELSEVIER SCIENCE BV
Citation
INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.452, no.1-2, pp.412 - 420
Abstract
The main purpose of this study was to investigate the potential of self-nano-emulsifying drug delivery system (SNEDDS) in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect. The DCT-loaded SNEDDS was prepared by employing rational blends of capryol 90, labrasol, and transcutol HP using ternary phase diagram. The liquid nano-emulsion was spray-dried into solid SNEDDS (D-SNEDDS) using an inert porous carrier, colloidal silica. The optimized formulation was characterized in terms of physico-chemical and pharmacokinetic parameters. Furthermore, anti-tumor efficacy of D-SNEDDS was compared with commercial marketed product, Taxotere (R). The various compositions of SNEDDS were screened and found optimal at a volume ratio of 10/75/15 for capryol 90, labrasol, and transcutol HP, respectively. We observed a high oral bioavailability of 17% DCT for D-SNEDDS than compared to only 2.6% for pure DCT solution. Notably, D-SNEDDS exhibited an augmented anti-tumor efficacy with a reduced toxicity profile when compared with intravenously administered Taxotere (R), the commercialized formulation of DCT. Taken together, D-SNEDDS could be a potential candidate for an oral dosage form of DCT with enhanced antitumor activity and reduced toxicity. (C) 2013 Elsevier B. V. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/29264http://dx.doi.org/10.1016/j.ijpharm.2013.05.034
ISSN
0378-5173
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약학대학 > 약학부 > Articles
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