TY - JOUR
T1 - G5 PAMAM dendrimer versus liposome
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
AU - van Dongen, Mallory A.
AU - He, Bing
AU - Wang, Siling
AU - Liu, George
AU - Banaszak Holl, Mark M.
AU - Zhang, Qiang
PY - 2015/1/1
Y1 - 2015/1/1
N2 - 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.
AB - 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.
KW - G5-NH<inf>2</inf> PAMAM dendrimer
KW - Liposome
KW - Oral bioavailability
KW - Simvastatin
KW - Transepithelial transport
UR - http://www.scopus.com/inward/record.url?scp=84930193127&partnerID=8YFLogxK
U2 - 10.1016/j.nano.2015.02.011
DO - 10.1016/j.nano.2015.02.011
M3 - Article
C2 - 25791813
AN - SCOPUS:84930193127
SN - 1549-9634
VL - 11
SP - 1141
EP - 1151
JO - Nanomedicine: Nanotechnology, Biology and Medicine
JF - Nanomedicine: Nanotechnology, Biology and Medicine
IS - 5
ER -