Enhanced solubility and oral absorption of sirolimus using D-α-tocopheryl polyethylene glycol succinate micelles

Min Soo Kim, Jung Soo Kim, Won Kyung Cho, Sung Joo Hwang

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

The objective of this study was to develop an oral formulation that would improve the solubility and oral absorption of sirolimus using a TPGS micellar solution. The effect of TPGS on the solubility and stability of sirolimus was evaluated. The sirolimus-loaded TPGS micelles were prepared using the thin-film hydration method. The average size of the sirolimus-loaded TPGS micelles was 11 nm. The concentration of sirolimus in a 50 mg/mL TPGS micellar solution was 0.97 ± 0.12 mg/mL, which demonstrates an enhancement of approximately 400-fold from the solubility of sirolimus in water. Furthermore, pharmacokinetic studies in rats indicated that the TPGS micellar solution significantly improved the oral absorption of sirolimus. Therefore, the preliminary results from this study suggest that a TPGS micellar solution has great potential for clinical applications.

Original languageEnglish
Pages (from-to)85-91
Number of pages7
JournalArtificial Cells, Nanomedicine and Biotechnology
Volume41
Issue number2
DOIs
Publication statusPublished - 2013 Apr 1

Fingerprint

Micelles
Sirolimus
Solubility
Polyethylene glycols
Pharmacokinetics
Hydration
Rats
Thin films
alpha-tocopheryl polyethylene glycol succinate
poly(ethylene succinate)
Water

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Medicine (miscellaneous)
  • Biomedical Engineering
  • Pharmaceutical Science

Cite this

@article{fc91797295194be0838562c473ad64ef,
title = "Enhanced solubility and oral absorption of sirolimus using D-α-tocopheryl polyethylene glycol succinate micelles",
abstract = "The objective of this study was to develop an oral formulation that would improve the solubility and oral absorption of sirolimus using a TPGS micellar solution. The effect of TPGS on the solubility and stability of sirolimus was evaluated. The sirolimus-loaded TPGS micelles were prepared using the thin-film hydration method. The average size of the sirolimus-loaded TPGS micelles was 11 nm. The concentration of sirolimus in a 50 mg/mL TPGS micellar solution was 0.97 ± 0.12 mg/mL, which demonstrates an enhancement of approximately 400-fold from the solubility of sirolimus in water. Furthermore, pharmacokinetic studies in rats indicated that the TPGS micellar solution significantly improved the oral absorption of sirolimus. Therefore, the preliminary results from this study suggest that a TPGS micellar solution has great potential for clinical applications.",
author = "Kim, {Min Soo} and Kim, {Jung Soo} and Cho, {Won Kyung} and Hwang, {Sung Joo}",
year = "2013",
month = "4",
day = "1",
doi = "10.3109/21691401.2012.742100",
language = "English",
volume = "41",
pages = "85--91",
journal = "Artificial Cells, Nanomedicine and Biotechnology",
issn = "2169-1401",
publisher = "Informa Healthcare",
number = "2",

}

Enhanced solubility and oral absorption of sirolimus using D-α-tocopheryl polyethylene glycol succinate micelles. / Kim, Min Soo; Kim, Jung Soo; Cho, Won Kyung; Hwang, Sung Joo.

In: Artificial Cells, Nanomedicine and Biotechnology, Vol. 41, No. 2, 01.04.2013, p. 85-91.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Enhanced solubility and oral absorption of sirolimus using D-α-tocopheryl polyethylene glycol succinate micelles

AU - Kim, Min Soo

AU - Kim, Jung Soo

AU - Cho, Won Kyung

AU - Hwang, Sung Joo

PY - 2013/4/1

Y1 - 2013/4/1

N2 - The objective of this study was to develop an oral formulation that would improve the solubility and oral absorption of sirolimus using a TPGS micellar solution. The effect of TPGS on the solubility and stability of sirolimus was evaluated. The sirolimus-loaded TPGS micelles were prepared using the thin-film hydration method. The average size of the sirolimus-loaded TPGS micelles was 11 nm. The concentration of sirolimus in a 50 mg/mL TPGS micellar solution was 0.97 ± 0.12 mg/mL, which demonstrates an enhancement of approximately 400-fold from the solubility of sirolimus in water. Furthermore, pharmacokinetic studies in rats indicated that the TPGS micellar solution significantly improved the oral absorption of sirolimus. Therefore, the preliminary results from this study suggest that a TPGS micellar solution has great potential for clinical applications.

AB - The objective of this study was to develop an oral formulation that would improve the solubility and oral absorption of sirolimus using a TPGS micellar solution. The effect of TPGS on the solubility and stability of sirolimus was evaluated. The sirolimus-loaded TPGS micelles were prepared using the thin-film hydration method. The average size of the sirolimus-loaded TPGS micelles was 11 nm. The concentration of sirolimus in a 50 mg/mL TPGS micellar solution was 0.97 ± 0.12 mg/mL, which demonstrates an enhancement of approximately 400-fold from the solubility of sirolimus in water. Furthermore, pharmacokinetic studies in rats indicated that the TPGS micellar solution significantly improved the oral absorption of sirolimus. Therefore, the preliminary results from this study suggest that a TPGS micellar solution has great potential for clinical applications.

UR - http://www.scopus.com/inward/record.url?scp=84879581427&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84879581427&partnerID=8YFLogxK

U2 - 10.3109/21691401.2012.742100

DO - 10.3109/21691401.2012.742100

M3 - Article

C2 - 23305536

AN - SCOPUS:84879581427

VL - 41

SP - 85

EP - 91

JO - Artificial Cells, Nanomedicine and Biotechnology

JF - Artificial Cells, Nanomedicine and Biotechnology

SN - 2169-1401

IS - 2

ER -