|
KMID : 0369820070370010015
|
|
Jorunal of Korean Pharmaceutical Sciences
2007 Volume.37 No. 1 p.15 ~ p.22
|
|
|
Preparation of Cyclosporin A-loaded Nanoparticles Containing Ethyl Myristate or Chitosan and Pharmacokinetics in Rats
|
|
Nam Dae-Sik
Lee Woo-Kyoung
|
|
|
Abstract
|
|
|
|
An oil-in-water solvent evaporation method was used to prepare the cyclosporin A (CyA)-loaded nano- particles varying in poly(D,L-lactide-co-glycolide) (PLGA) polymer (RG 502H, RG 503H) and the amount of additive ethyl myristate (EM) or chitosan (CS). The particles were characterized for drug loading and entrapment efficiency by HPLC, sur- face morphology by scanning electron microscopy, particle size by dynamic light scattering and surface charge by Zeta- potential. The results showed drug loadings ranging from 10.9% to 15.8% with high encapsulation efficiency (82.0-97.8%). SEM and DLS studies showed discrete and spherical particles with smooth surfaces and mean size ranging 257.6-721.7 nm. The additive EM or CS did not change the mean sizes of the nanoparticles, whereas by the coating effect of CS, the Zeta- potential values of the CS-added nanoparticles were moved to the more positive direction as the amount of CS was increased. From the pharmacokinetic analysis, the nanoparticles formulations showed the higher bioavailability and MRT than Neoral®. While little adding effect of EM or CS was detected in pharmacokinetic profile when RG 503H was used as polymer carrier, more noticeable different pharmacokinetic behaviors could be observed in case of RG 502H. EM incor- poration was found to elevate the Kel, whereas CS coating resulted in the decrease of F and K디, which seems to be due to the function of CS as a barrier and a mucoadhesive coating.
|
|
|
KEYWORD
|
|
|
Nanoparticles, Cyclosporin A, Oral, Neoral
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|
|