Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles.
Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability. This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA. Transmission electron microscopy and freeze-fracture replication transmission election microscopy showed that the HSYA nanoparticles have an irregular shape and a narrow size distribution. Zonula occludens 1 protein (ZO-1) labeling showed that the nanoparticles with different dilutions produced an opening in the tight junctions of Caco-2 cells without inducing cytotoxicity to the cells. Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.
Department of Pharmacy, Zhejiang Provincial People's Hospital, Hangzhou, People's Republic of China.
Liang-Zhong
LZ
Lv
Chen-Qi
CQ
Tong
Jia
J
Yu
Min
M
Han
Jian-Qing
JQ
Gao
D000042:Absorption / Q000187:drug effects*; D061605:Administration, Intravenous; D000284:Administration, Oral; D000704:Analysis of Variance; D000818:Animals; D001682:Biological Availability; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004705:Endocytosis / Q000187:drug effects; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D011809:Quinones / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D062826:Zonula Occludens-1 Protein / Q000378:metabolism
D011809:Quinones; D062826:Zonula Occludens-1 Protein; C085278:hydroxysafflor yellow A; D002599:Chalcone
Caco-2 cells; absorption; bioavailability; hydroxysafflor yellow A; nanoparticles