Hepatic-targeting microcapsules construction by self-assembly of bioactive galactose-branched polyelectrolyte for controlled drug release system.
We describe the construction of hepatic-targeting microcapsules by self-assembly of chemo-enzymatic synthesized poly(vinyl galactose ester-co-methacryloxyethyl trimethylammonium chloride) (PGEDMC) containing galactose branches, which can be specifically recognized by membrane bound galactose receptors (ASGPR), for acyclovir (ACV) controlled release system. Alternate deposition of PGEDMC and poly(sodium 4-styrenesulfonate) (PSS) was carried out on ACV microcrystals. It was revealed that the drug release rate decreases with the increase of coated layer number and a microcapsule-drying treatment would enhance the sustained release effect probably because of a multilayer shrink and tightness during the process. The complete release of ACV yielded a hollow PGEDMC/PSS multilayered network with favorable integrity and nano-thickness by TEM and SEM. The potential targetability of the system was proved in vitro by PNA lectin recognition. Lectin hardly adsorbed on the film where the outmost layer was a polyanion or a polycation without galactose component. Whilst the galactose-containing layer (PGEDMC) was the outmost layer, a significant lectin combination was observed. This technique could provide a promising way to encapsulate and deliver various target substances in biological and pharmaceutical applications.
Zhang
Fu
F
Department of Chemistry, Zhejiang University, Hangzhou 310027, People's Republic of China.
Wu
Qi
Q
Chen
Zhi-Chun
ZC
Zhang
Ming
M
Lin
Xian-Fu
XF
D000212:Acyclovir / Q000008:administration & dosage / Q000378:metabolism; D000818:Animals; D001672:Biocompatible Materials / Q000737:chemistry; D002214:Capsules; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D004573:Electrolytes / Q000737:chemistry; D005690:Galactose / Q000737:chemistry; D006801:Humans; D037102:Lectins; D008099:Liver / Q000187:drug effects* / Q000378:metabolism*; D011956:Receptors, Cell Surface / Q000378:metabolism
D001672:Biocompatible Materials; D002214:Capsules; D003692:Delayed-Action Preparations; D004573:Electrolytes; D037102:Lectins; D011956:Receptors, Cell Surface; C039707:galactose receptor; D005690:Galactose; D000212:Acyclovir