Encapsulation of honokiol into self-assembled pectin nanoparticles for drug delivery to HepG2 cells.
Self-assembled pectin nanoparticles was prepared and evaluated for delivering the hydrophobic drug, honokiol (HK), to HepG2 cells. These hydrophobic drug-loaded nanoparticles were developed without using any surfactant and organic solvent. Hydroxypropyl-β-cyclodextrin (HCD) was used to fabricate an inclusion complex with HK (HKHCD) to increase the solubility of the drug and thus facilitate its encapsulation and dispersion in the pectin nanoparticles. Investigation of the in vitro release indicated that the drug-loaded nanoparticles exhibited a higher drug release rate than free honokiol and an effective sustained-release. Cytotoxicity, cell apoptosis and cellular uptake studies further confirmed that the pectin nanoparticles with galactose residues generated higher cytotoxicity than free honokiol on HepG2 cells which highly expressed asialoglycoprotein receptors (ASGR). Nevertheless, these findings were not observed in ASGR-negative A549 cells under similar condition. Therefore, pectin nanoparticles demonstrated a specific active targeting ability to ASGR-positive HepG2 cells and could be used as a potential drug carrier for treatment of liver-related tumors.
Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, Medicine Engineering Research Center, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Yuxia
Y
Zhang
School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, PR China.
Tong
T
Chen
Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, Medicine Engineering Research Center, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Pei
P
Yuan
The Experimental Teaching Centre, Chongqing Medical University, Chongqing 400016, PR China.
Rui
R
Tian
Chongqingshi Shapingba District People's Hospital, Chongqing 400030, PR China.
Wenjing
W
Hu
Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, Medicine Engineering Research Center, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Yalan
Y
Tang
Department of Pharmacy, Children's Hospital of Chongqing Medical University, Chongqing 400010, PR China.
Yuntao
Y
Jia
Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, Medicine Engineering Research Center, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China. Electronic address: zlkdyx@126.com.
Liangke
L
Zhang
D017209:Apoptosis / Q000187:drug effects; D001667:Binding, Competitive; D001692:Biological Transport; D001713:Biphenyl Compounds / Q000737:chemistry*; D002214:Capsules; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D065546:Drug Liberation; D056945:Hep G2 Cells; D006801:Humans; D017705:Lignans / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010368:Pectins / Q000737:chemistry*; D000498:Allyl Compounds; D010636:Phenols
D001713:Biphenyl Compounds; D002214:Capsules; D004337:Drug Carriers; D017705:Lignans; D010368:Pectins; C005499:honokiol; D000498:Allyl Compounds; D010636:Phenols
HepG2; Honokiol; Hydroxypropyl-β-cyclodextrin; Nanoparticle; Pectin