Preparation and evaluation of tacrolimus-loaded nanoparticles for lymphatic delivery

Title
Preparation and evaluation of tacrolimus-loaded nanoparticles for lymphatic delivery
Author(s)
최한곤이용복[이용복]신새벽[신새벽]김대덕[김대덕]조혜영[조혜영]
Keywords
DRUG-DELIVERY; IN-VITRO; GENETIC POLYMORPHISMS; LIPID NANOPARTICLES; PLGA NANOPARTICLES; MASS-SPECTROMETRY; PHARMACOKINETICS; SYSTEM; TRANSPLANTATION; CYCLOSPORINE
Issue Date
201002
Publisher
ELSEVIER SCIENCE BV
Citation
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, v.74, no.2, pp.164 - 171
Abstract
In an effort to improve lymphatic targeting efficiency and reduce the toxicity of tacrolimus, the emulsification-diffusion method was used to load the drug into nanoparticles (NP). Poly(lactide-co-glycolide) (PLGA) and PLGA surface-modified with poly(ethylene glycol) (PEG) were used as polymers. Mean particle size and drug encapsulation efficiency of PLGA were 218 +/- 51 nm and 60.0 +/- 1.2% and for PEG-PLGA NP were 220 +/- 33 nm and 60.3 +/- 2.0%. NP were characterized by thermal analyzer and X-ray diffractometry (XRD), and their shapes were observed by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). In vitro release profiles were affected by the pH of dissolution media. The prepared NP and commercial product of tacrolimus (Prograf (R) inj.) were intravenously administered to rats to compare their pharmacokinetic characteristics and lymphatic targeting efficiency. The area under the whole blood concentration-time curve (AUC), mean residence time (MRT), and total clearance (CL(t)) of PEG-PLGA NP were significantly different (P < 0.05) compared with those of Prograf (R) inj., and lymphatic targeting efficiencies of both NP formulations at the mesenteric lymph node significantly increased (P < 0.05). These results showed that the prepared tacrolimus-loaded NP are good possible candidates as a lymphatic delivery system of tacrolimus. (C) 2009 Elsevier B.V. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/22937http://dx.doi.org/10.1016/j.ejpb.2009.08.006
ISSN
0939-6411
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약학대학 > 약학부 > Articles
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