YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Effect of Liposome Encapsulation on Intestinal Absorption of Rhodamine 123

리포솜 봉입이 로다민 123의 소장 흡수에 미치는 영향

  • Hong, Soon-Sun (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Lee, Hae-Ree (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Li, Hong (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Chung, Suk-Jae (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Kim, Dae-Duk (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Shim, Chang-Koo (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University)
  • 홍순선 (서울대학교 약학대학 종합약학연구소) ;
  • 이해리 (서울대학교 약학대학 종합약학연구소) ;
  • 이홍 (서울대학교 약학대학 종합약학연구소) ;
  • 정석재 (서울대학교 약학대학 종합약학연구소) ;
  • 김대덕 (서울대학교 약학대학 종합약학연구소) ;
  • 심창구 (서울대학교 약학대학 종합약학연구소)
  • Published : 2005.01.01
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Abstract

The absorption of a P-gp substrate, rhodamine 123, from a liposomal dosage form was investigated across Caco-2 cell monolayers, rat intestines and rat intestinal Peyer's patches in Ussing chamber, Rhodamine 123 was incorporated into liposomes according to the standard evaporation method, which led to a production of liposomes with a mean diameter of 71.3 nm. The permeability (Papp of rhodamine 123 from a water solution across the monolayer was $2.45{\times}10^{-6}$ cm/s for $A{\leftrightarrow}B$ (apical to basal) and $14.0{\times}10^{-6}$ cm/s for $B{\leftrightarrow}A$ (basal to apical) directions, consistent with the fact that rhodamine 123 is one of the P-gp substrates. The transport of rhodamine 123 from the liposomal dosage form was much lower for both directions compared to the solution of rhodamine 123. The transport of rhodamine 123 across the rat intestine was also significantly decreased for both directions, I.e., influx and efflux, by the liposomal incorporation of the compound. The transport of rhodamine 123 across the Peyer's patch was substantially reduced by liposomal incorporation. No difference was found in the transport between the Peyer's patch and non-Peyer's patch. These observations suggest that the contribution of transport via Peyer's patches in the uptake of liposomes may be minimal, especially for rapidly absorbed compounds like rhodamine 123. Therefore, the increased absorption of P-gp substrates does not appear to be feasible by incorporating the compounds in liposomes, due to negligible involvement of Peyer's patches in the uptake of particulate dosage forms like liposomes. Liposomes may rather represent a sustained release dosage form of incorporated compounds.

Keywords

References

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