G5 PAMAM dendrimer versus liposome: A comparison study on the in vitro transepithelial transport and in vivo oral absorption of simvastatin

Rong Qi, Heran Zhang, Lu Xu, Wenwen Shen, Cong Chen, Chao Wang, Yini Cao, Yunan Wang, Mallory A. van Dongen, Bing He, Siling Wang, George Liu, Mark M. Banaszak Holl, Qiang Zhang

Research output: Contribution to journalArticleResearchpeer-review

Abstract

This study compared formulation effects of a dendrimer and a liposome preparation on the water solubility, transepithelial transport, and oral bioavailability of simvastatin (SMV). Amine-terminated G5 PAMAM dendrimer (G5-NH2) was chosen to form SMV/G5-NH2 molecular complexes, and SMV-liposomes were prepared by using a thin film dispersion method. The effects of these preparations on the transepithelial transport were investigated in vitro using Caco-2 cell monolayers. Results indicated that the solubility and transepithelial transport of SMV were significantly improved by both formulations. Pharmacokinetic studies in rats also revealed that both the SMV/G5-NH2 molecular complexes and the SMV-liposomes significantly improved the oral bioavailability of SMV with the liposomes being more effective than the G5-NH2. The overall better oral absorption of SMV-liposomes as compared to SMV/G5-NH2 molecular complexes appeared to arise from better liposomal solubilization and encapsulation of SMV and more efficient intracellular SMV delivery. From the Clinical Editor: Various carrier systems have been designed to enhance drug delivery via the oral route. In this study, the authors compared G5 PAMAM dendrimers to liposome preparations in terms of solubility, transepithelial transport, and oral bioavailability of this poorly water-soluble drug. This understanding has improved our knowledge in the further development of drug carrier systems.

Original languageEnglish
Pages (from-to)1141-1151
Number of pages11
JournalNanomedicine: Nanotechnology, Biology, and Medicine
Volume11
Issue number5
DOIs
Publication statusPublished - 1 Jan 2015
Externally publishedYes

Keywords

  • G5-NH<inf>2</inf> PAMAM dendrimer
  • Liposome
  • Oral bioavailability
  • Simvastatin
  • Transepithelial transport

Cite this

Qi, Rong ; Zhang, Heran ; Xu, Lu ; Shen, Wenwen ; Chen, Cong ; Wang, Chao ; Cao, Yini ; Wang, Yunan ; van Dongen, Mallory A. ; He, Bing ; Wang, Siling ; Liu, George ; Banaszak Holl, Mark M. ; Zhang, Qiang. / G5 PAMAM dendrimer versus liposome : A comparison study on the in vitro transepithelial transport and in vivo oral absorption of simvastatin. In: Nanomedicine: Nanotechnology, Biology, and Medicine. 2015 ; Vol. 11, No. 5. pp. 1141-1151.
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G5 PAMAM dendrimer versus liposome : A comparison study on the in vitro transepithelial transport and in vivo oral absorption of simvastatin. / Qi, Rong; Zhang, Heran; Xu, Lu; Shen, Wenwen; Chen, Cong; Wang, Chao; Cao, Yini; Wang, Yunan; van Dongen, Mallory A.; He, Bing; Wang, Siling; Liu, George; Banaszak Holl, Mark M.; Zhang, Qiang.

In: Nanomedicine: Nanotechnology, Biology, and Medicine, Vol. 11, No. 5, 01.01.2015, p. 1141-1151.

Research output: Contribution to journalArticleResearchpeer-review

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T2 - A comparison study on the in vitro transepithelial transport and in vivo oral absorption of simvastatin

AU - Qi, Rong

AU - Zhang, Heran

AU - Xu, Lu

AU - Shen, Wenwen

AU - Chen, Cong

AU - Wang, Chao

AU - Cao, Yini

AU - Wang, Yunan

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AU - He, Bing

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AU - Liu, George

AU - Banaszak Holl, Mark M.

AU - Zhang, Qiang

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