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Comparative Study
. 2003 Aug 11;261(1-2):21-6.
doi: 10.1016/s0378-5173(03)00274-6.

The absorption behavior of cyclosporin A lecithin vesicles in rat intestinal tissue

Ying Chen  1 , Qineng Ping, Jianxin Guo, Wenli Lv, Jing Gao
Affiliations
Comparative Study

The absorption behavior of cyclosporin A lecithin vesicles in rat intestinal tissue

Ying Chen et al. Int J Pharm. .

Abstract

The purpose of the study was to investigate the absorption behavior of lecithin vesicles of cyclosporin A (CsA-VES), prepared by the rotary evaporation method and treated further with sonication. The everted gut sac technique and in situ circulation method were used to examine: (1) relationship between the CsA-VES absorption velocity and the CsA-VES content; (2) the influence of the intestinal mucus, blank vesicles, concentration of Na(+), energy inhibitor and P-gp inhibitor on the absorption of CsA-VES; and (3) the respective accumulated content of CsA in the incubating medium and the sacs after incubation with Sandimmum Neoral((R))(CsA-NEO) and CsA-VES. Our results showed there was a saturated absorption of CsA. Most CsA-VES accumulated in the mucus before it reached the intestinal tissue. There was no significant difference in the accumulated absorption content in the incubating medium and the sacs of CsA-NEO and CsA-VES. The addition of blank vesicles and concentration of Na(+) had no significant influence on the accumulated absorption of CsA (P>0.05). The energy inhibitor and P-gp inhibitor influenced the accumulated absorption of CsA significantly (P<0.05). CsA-VES may be transported by phagocytosis. Mucus was a barrier blocking the diffusion of CsA-VES. CsA-NEO and CsA-VES showed equal absorption levels in the intestine.

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