title: Sulfated polysaccharide heparin used as carrier to load hydrophobic lappaconitine.
abstract: One-step self-assembly was used to prepare pH-sensitive lappaconitine-loaded low-molecular-weight heparin (LMWH-LA) and to demonstrate that the sulfur group promotes dissolution and has synergistic effect on the analgesic property of lappaconitine (LA). The LMWH-LA was characterized in terms of releasing behavior, pH-sensitivity, analgesic activity and anticoagulation property. The drug loading level of LA in low-molecular-weight heparin (LMWH) reached 24.3% (w/w). The LA, self-assembled in LMWH, released faster in an acidic environment than that in neutral or alkaline environments. Analgesic experiments showed that the LMWH-LA had earlier onset time and longer duration than the LA. Compared with LMWH, the LMWH-LA can reduce clotting time more effectively. These results suggest that the LMWH is a good template and has great potential to achieve synergistic effect of LA. In addition, similar macromolecular structure can be used as a new natural polymeric carrier for loading hydrophobic alkaloids.
authors.affiliation: College of Food Science and Engineering, Inner Mongolia Agricultural University, Hohhot 010018, China; Department of Agricultural, Food and Nutritional Science (AFNS), University of Alberta, T6G 2P5 Edmonton, AB, Canada; College of Life Sciences, Northwest Normal University, Lanzhou 730070, China. Electronic address: wenxiu_sun@imau.edu.cn.
authors.forename: Wenxiu
authors.initials: W
authors.lastname: Sun
authors.affiliation: Department of Agricultural, Food and Nutritional Science (AFNS), University of Alberta, T6G 2P5 Edmonton, AB, Canada.
authors.forename: Marleny D A
authors.initials: MD
authors.lastname: Saldaña
authors.affiliation: College of Food Science and Engineering, Inner Mongolia Agricultural University, Hohhot 010018, China.
authors.forename: Liyan
authors.initials: L
authors.lastname: Fan
authors.affiliation: Department of Agricultural, Food and Nutritional Science (AFNS), University of Alberta, T6G 2P5 Edmonton, AB, Canada.
authors.forename: Yujia
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: College of Food Science and Engineering, Inner Mongolia Agricultural University, Hohhot 010018, China.
authors.forename: Tungalag
authors.initials: T
authors.lastname: Dong
authors.affiliation: College of Food Science and Engineering, Inner Mongolia Agricultural University, Hohhot 010018, China.
authors.forename: Ye
authors.initials: Y
authors.lastname: Jin
authors.affiliation: College of Life Sciences, Northwest Normal University, Lanzhou 730070, China.
authors.forename: Ji
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000157:Aconitine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage*; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D006493:Heparin / Q000008:administration & dosage / Q000737:chemistry*; D006495:Heparin, Low-Molecular-Weight / Q000008:administration & dosage / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D051379:Mice; D011108:Polymers / Q000737:chemistry; D011134:Polysaccharides / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013431:Sulfates / Q000737:chemistry*
chemical_list: D018712:Analgesics, Non-Narcotic; D000925:Anticoagulants; D004337:Drug Carriers; D006495:Heparin, Low-Molecular-Weight; D011108:Polymers; D011134:Polysaccharides; D013431:Sulfates; D006493:Heparin; D000157:Aconitine; C022150:lappaconitine
keywords: Lappaconitine; Low-molecular-weight heparin; Self-assembly