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Development of mannosylated liposomes using synthesized N-octadecyl-D-mannopyranosylamine to enhance gastrointestinal permeability for protein delivery.利用合成的 N-十八烷基-D-甘露吡喃胺制备甘露糖化脂质体，以增强蛋白质的胃肠道通透性。
AAPS PharmSciTech. 2012 Jun;13(2):699-706. doi: 10.1208/s12249-012-9788-1. Epub 2012 May 5.
2
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Formulation, Pharmacokinetic, and Efficacy Studies of Mannosylated Self-Emulsifying Solid Dispersions of Noscapine.那可丁甘露糖化自乳化固体分散体的处方、药代动力学及药效学研究
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本文引用的文献

1
Characterization and in vitro evaluation of intestinal absorption of liposomes encapsulating zanamivir.载有扎那米韦的脂质体的特性鉴定及其肠吸收的体外评价。
Curr Drug Deliv. 2011 Jul;8(4):392-297. doi: 10.2174/156720111795767915.
2
Influence of microenvironment and liposomal formulation on secondary structure and bilayer interaction of lysozyme.溶菌酶的微环境和脂质体配方对其二级结构和双层相互作用的影响。
Colloids Surf B Biointerfaces. 2010 Feb 1;75(2):501-9. doi: 10.1016/j.colsurfb.2009.09.027. Epub 2009 Sep 26.
3
Probing insulin's secondary structure after entrapment into alginate/chitosan nanoparticles.胰岛素包封于海藻酸盐/壳聚糖纳米颗粒后的二级结构探究
Eur J Pharm Biopharm. 2007 Jan;65(1):10-7. doi: 10.1016/j.ejpb.2006.09.005. Epub 2006 Sep 24.
4
Effect of mannose density on mannose receptor-mediated cellular uptake of mannosylated O/W emulsions by macrophages.
J Control Release. 2006 Aug 28;114(2):193-201. doi: 10.1016/j.jconrel.2006.04.010. Epub 2006 May 9.
5
Effectiveness of submicron-sized, chitosan-coated liposomes in oral administration of peptide drugs.亚微米级壳聚糖包衣脂质体用于口服肽类药物的有效性
Int J Pharm. 2005 Oct 13;303(1-2):160-70. doi: 10.1016/j.ijpharm.2005.06.028.
6
Enhanced intestinal absorption of salmon calcitonin (sCT) from proliposomes containing bile salts.从含有胆盐的前体脂质体中增强鲑鱼降钙素（sCT）的肠道吸收。
J Control Release. 2005 Sep 2;106(3):298-308. doi: 10.1016/j.jconrel.2005.05.016.
7
The lectin-cell interaction and its implications to intestinal lectin-mediated drug delivery.凝集素-细胞相互作用及其对肠道凝集素介导的药物递送的影响。
Adv Drug Deliv Rev. 2004 Mar 3;56(4):459-80. doi: 10.1016/j.addr.2003.10.015.
8
Potentiality of double liposomes containing salmon calcitonin as an oral dosage form.
J Control Release. 2003 May 20;89(3):429-36. doi: 10.1016/s0168-3659(03)00160-3.
9
Differential expression of the murine mannose-binding lectins A and C in lymphoid and nonlymphoid organs and tissues.小鼠甘露糖结合凝集素A和C在淋巴及非淋巴器官和组织中的差异表达。
J Immunol. 2003 Feb 1;170(3):1462-5. doi: 10.4049/jimmunol.170.3.1462.
10
L-MBP is expressed in epithelial cells of mouse small intestine.L-髓鞘碱性蛋白在小鼠小肠的上皮细胞中表达。
J Immunol. 2002 Dec 15;169(12):6945-50. doi: 10.4049/jimmunol.169.12.6945.

利用合成的 N-十八烷基-D-甘露吡喃胺制备甘露糖化脂质体，以增强蛋白质的胃肠道通透性。

Development of mannosylated liposomes using synthesized N-octadecyl-D-mannopyranosylamine to enhance gastrointestinal permeability for protein delivery.

机构信息

Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudhya Road, Bangkok, 10400, Thailand.

出版信息

AAPS PharmSciTech. 2012 Jun;13(2):699-706. doi: 10.1208/s12249-012-9788-1. Epub 2012 May 5.

DOI:10.1208/s12249-012-9788-1
PMID:22562613
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3364374/
Abstract

The lysozyme (LZ)-entrapped mannosylated liposomes were prepared in this study by the use of N-octadecyl-D-mannopyranosylamine (SAMAN), which had been synthesized in-house and confirmed by characterization with FTIR and NMR. The reactant residues of synthesized SAMAN were found to be less than 1%. The mean sizes, zeta potentials, drug entrapment efficiencies, and loading capacities of all liposomal formulations were in the ranges of 234.7 to 431.0 nm, -10.97 to -25.80 mV, 7.52 to 14.10%, and 1.44 to 2.77%, respectively. The permeability of mannosylated LZ liposomes across Caco-2 cell monolayers was significantly enhanced to about 2.5- and 7-folds over those of conventional liposomes and solution, respectively, which might be due to the role of mannose receptor or mannose-binding protein on the intestinal enterocytes.

摘要

本研究通过使用 N-十八烷基-D-甘露吡喃胺（SAMAN）制备了溶菌酶（LZ）包封的甘露糖化脂质体，SAMAN 是在内部合成的，并通过傅里叶变换红外光谱和核磁共振进行了表征确认。合成的 SAMAN 的反应物残留量被发现小于 1%。所有脂质体制剂的平均粒径、ζ电位、药物包封效率和载药量分别在 234.7 至 431.0nm、-10.97 至-25.80mV、7.52 至 14.10%和 1.44 至 2.77%之间。甘露糖化 LZ 脂质体穿过 Caco-2 细胞单层的通透性显著提高，相对于普通脂质体和溶液分别提高了约 2.5 倍和 7 倍，这可能是由于肠上皮细胞上甘露糖受体或甘露糖结合蛋白的作用。