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Expert Opin Drug Deliv. 2013 Oct;10(10):1319-34. doi: 10.1517/17425247.2013.801957. Epub 2013 Jun 22.

New surface hydroxylated and internally quaternised poly(propylene imine) dendrimers as efficient biocompatible drug carriers of norfloxacin.

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1
1University of Madras, Department of Physical Chemistry, School of Chemical Sciences, Maraimalai Campus, Guindy, Chennai , 600025, Tamil Nadu , India emurugan_68@yahoo.co.in.

Abstract

OBJECTIVES:

This study intended to describe the development of two novel, biocompatible and potential surface hydroxylated quaternary ammonium chloride based poly(propylene imine) (PPI) dendrimers for effective delivery of the drug Norfloxacin (NFN).

METHODS:

The synthetic pathway involved the hydroxylation and methylation of generation 2 and 3 PPI dendrimers and thus produced surface hydroxylated and internally quaternised PPI dendrimers viz., QPPI-OH (G2) and QPPI-OH (G3), respectively. The potential of these dendrimers were examined as drug carrier for NFN, by carrying out solubility, in vitro release, cytotoxicity and anti-bacterial studies.

RESULTS:

It was observed that the QPPI-OH (G2)/QPPI-OH (G3) dendrimers have excellent solubilising potential/drug loading abilities of NFN in aqueous medium and can also sustain delivery of NFN. The effective complexation of NFN with QPPI-OH (G2) and QPPI-OH (G3) increased the solubility of NFN and thus elevates the NFN drug from Class 4 to Class 3 (according to BCS). These dendrimers increase the biocompatibility and increase the tolerance concentration during drug-dendrimer formulations. Anti-bacterial studies showed that the efficacy of the drug was increased in the presence of dendrimer carriers.

CONCLUSIONS:

These results indicate that the QPPI-OH (G2) and QPPI-OH (G3) dendrimers might be considered as potential biocompatible drug carriers of fluoroquinolines under suitable conditions.

PMID:
23789895
DOI:
10.1517/17425247.2013.801957
[Indexed for MEDLINE]
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