NDLI: Development and In Vitro Characterization of Galactosylated Low Molecular Weight Chitosan Nanoparticles Bearing Doxorubicin

Content Provider	Springer Nature Link
Author	Jain, Nitin K. Jain, Sanjay K.
Copyright Year	2010
Abstract	The aim of the present research was to evaluate the potential of galactosylated low molecular weight chitosan (Gal-LMWC) nanoparticles bearing positively charged anticancer, doxorubicin (DOX) for hepatocyte targeting. The chitosan from crab shell was depolymerized, and the lactobionic acid was coupled with LMWC using carbodiimide chemistry. The depolymerized and galactosylated polymers were characterized. Two types of Gal-LMWC(s) with variable degree of substitution were employed to prepare the nanoparticles using ionotropic gelation with pentasodium tripolyphosphate anions. Factors affecting nanoparticles formation were discussed. The nanoparticles were characterized by transmission electron microscopy and photon correlation spectroscopy and found to be spherical in the size range 106–320 nm. Relatively higher percent DOX entrapment was obtained for Gal-LMWC(s) nanoparticles than for LMWC nanoparticles. A further increase in drug entrapment was found with nanoparticles prepared by Gal-LMWC with higher degree of substitution. A hypothesis which correlates the ionic concentration of DOX in nanoparticles preparation medium and percent DOX entrapment in cationic polymer has been proposed to explain the enhanced DOX entrapment. In-vitro drug release study demonstrated an initial burst release followed by a sustained release. The targeting potential of the prepared nanoparticles was assessed by in vitro cytotoxicity study using the human hepatocellular carcinoma cell line (HepG$_{2}$) expressing the ASGP receptors on their surfaces. The enthusiastic results showed the feasibility of Gal-LMWC(s) to entrap the cationic DOX and targeting potential of developed Gal-LMWC(s) nanoparticles to HepG$_{2}$ cell line.
Starting Page	686
Ending Page	697
Page Count	12
File Format	PDF
Journal	AAPS PharmSciTech
Volume Number	11
Issue Number	2
e-ISSN	15309932
Language	English
Publisher	Springer US
Publisher Date	2010-04-23
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	doxorubicin HCC targeting low molecular weight chitosan nanoparticles Pharmacy Biochemistry Biotechnology Pharmacology/Toxicology
Content Type	Text
Resource Type	Article

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