Premium
Synthesis of Mannose‐Cholesterol Conjugates for Targeted Liposomal Drug Delivery
Author(s) -
Nguyen Huong,
Katavic Peter,
Bashah Nur Atikah Halim,
Ferro Vito
Publication year - 2016
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201600007
Subject(s) - conjugate , mannose , combinatorial chemistry , chemistry , click chemistry , drug delivery , liposome , cationic polymerization , azide , cycloaddition , bifunctional , targeted drug delivery , peg ratio , organic chemistry , biochemistry , mathematics , mathematical analysis , catalysis , finance , economics
Several novel, mannose‐cholesterol conjugates for use in targeted liposomal drug delivery were synthesized via a modular strategy utilizing the Cu(I)‐catalysed Huisgen azide‐alkyne cycloaddition (“Click”) reaction. The conjugates, which were fully characterized, comprised either a single mannose unit or a trivalent mannose cluster joined to cholesterol via bifunctional PEG‐based linkers of different lengths. The neutral conjugates offer advantages over a previously reported cationic conjugate and the modular strategy employed can be readily adapted for the preparation of conjugates with alternative targeting groups.