PMID- 32035254 OWN - NLM STAT- MEDLINE DCOM- 20201225 LR - 20201225 IS - 1873-3476 (Electronic) IS - 0378-5173 (Linking) VI - 579 DP - 2020 Apr 15 TI - Bile acid transporter mediated STC/Soluplus self-assembled hybrid nanoparticles for enhancing the oral drug bioavailability. PG - 119120 LID - S0378-5173(20)30104-6 [pii] LID - 10.1016/j.ijpharm.2020.119120 [doi] AB - The nano-particulate system for oral delivery faces a big challenge across the gastrointestinal bio-barriers. The aim was to explore the potential applications of bile acid transporter mediated the self-assembled hybrid nanoparticles (SHNPs) of sodium taurocholate (STC) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) for augmenting the oral delivery of poorly water-soluble drugs. Felodipine (FLDP) was chosen as a model drug. The self-assembly of STC with Soluplus to load FLDP and the microstructure of the SHNPs were confirmed using molecular simulation, STC determination by high performance liquid chromatography (HPLC) and transmission electron microscope. Results showed that STC was integrated with Soluplus on the surface of nanoparticles by hydrophobic interactions. The permeability of FLDP loaded STC/Soluplus SHNPs was STC dependent in the ileum, which was inhibited by the higher concentrations of STC and the inhibitor of apical sodium-dependent bile acid transporter (ASBT). STC/Soluplus (1:9) SHNPs significantly improved the drug loading of FLDP, achieved the highest permeability of FLDP and realized 1.6-fold of the area under the curve (AUC) of Soluplus self-assembled nanoparticles (SNPs). A water-quenching fluorescent probe P4 was loaded into the STC/Soluplus SHNPs, which verified that the SHNPs were transferred intactly across the ileum. In conclusion, STC/Soluplus SHNPs via ASBT are a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs. CI - Copyright (c) 2020 Elsevier B.V. All rights reserved. FAU - Zhang, Shujuan AU - Zhang S AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310032, PR China. FAU - Cui, Dongmei AU - Cui D AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310032, PR China. FAU - Xu, Jiawei AU - Xu J AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310032, PR China. FAU - Wang, Jiandong AU - Wang J AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310032, PR China. FAU - Wei, Qi AU - Wei Q AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310032, PR China. FAU - Xiong, Subin AU - Xiong S AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, 18 Chaowang Road, Hangzhou 310032, PR China; Shanghai Anbison Laboratory Co., Ltd., 889 Yishan Road, Shanghai 200233, PR China. Electronic address: sbxiong@gmail.com. LA - eng PT - Journal Article DEP - 20200205 PL - Netherlands TA - Int J Pharm JT - International journal of pharmaceutics JID - 7804127 RN - 0 (Drug Carriers) RN - 0 (Organic Anion Transporters, Sodium-Dependent) RN - 0 (Polyvinyls) RN - 0 (Symporters) RN - 0 (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer) RN - 145420-23-1 (sodium-bile acid cotransporter) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - 5E090O0G3Z (Taurocholic Acid) RN - OL961R6O2C (Felodipine) SB - IM MH - Administration, Oral MH - Animals MH - Area Under Curve MH - Drug Carriers/*chemistry MH - Drug Compounding/methods MH - Drug Liberation MH - Felodipine/*administration & dosage/pharmacokinetics MH - Hydrophobic and Hydrophilic Interactions MH - Male MH - Mice MH - Nanoparticles/*chemistry MH - Organic Anion Transporters, Sodium-Dependent/*chemistry MH - Permeability MH - Polyethylene Glycols/chemistry MH - Polyvinyls/chemistry MH - Rats MH - Symporters/*chemistry MH - Taurocholic Acid/*chemistry OTO - NOTNLM OT - ASBT OT - Felodipine OT - P4 OT - Self-assembled hybrid nanoparticles OT - Sodium taurocholate OT - Soluplus COIS- Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. EDAT- 2020/02/09 06:00 MHDA- 2020/12/29 06:00 CRDT- 2020/02/09 06:00 PHST- 2019/09/19 00:00 [received] PHST- 2020/02/02 00:00 [revised] PHST- 2020/02/04 00:00 [accepted] PHST- 2020/02/09 06:00 [pubmed] PHST- 2020/12/29 06:00 [medline] PHST- 2020/02/09 06:00 [entrez] AID - S0378-5173(20)30104-6 [pii] AID - 10.1016/j.ijpharm.2020.119120 [doi] PST - ppublish SO - Int J Pharm. 2020 Apr 15;579:119120. doi: 10.1016/j.ijpharm.2020.119120. Epub 2020 Feb 5.