Home » Key Scientific Articles » Comparative anti-inflammatory activity of poly(amidoamine) (PAMAM) dendrimer-dexamethasone conjugates with dexamethasone-liposomes.

Comparative anti-inflammatory activity of poly(amidoamine) (PAMAM) dendrimer-dexamethasone conjugates with dexamethasone-liposomes.

Choksi A, Sarojini KV, Vadnal P, Dias C, Suresh PK, Khandare J.

Int J Pharm. 2013 Jun 5;449(1-2):28-36.

 

School of Biosciences & Technology, VIT University, Vellore, Vellore Dt., 632014, India.

 

Abstract

 

Lipophilicity vs hydrophicility physicochemical traits are extremely important variables that are active considerations for optimizing drug delivery systems. The comparative anti-inflammatory delivery potential of dexamethasone (dex) in an encapsulation-based (liposome-lipophilic) and poly(amidoamine) (PAMAM) dendrimer prodrug conjugation-based delivery systems (hydrophilic) was performed in this work. Dendrimer prodrugconjugates were characterized by (1)H NMR. The drug encapsulation efficiency for drug in liposomes was observed to be 14.02% and this was correlated with a dose-dependent tumor necrosis factor (TNF)-{Alpha} inhibition (39-57% inhibition). The biological evaluation of nanocarriers for drug was demonstrated in a standard, conventionally used in vitro cell-based system for TNF-{Alpha} inhibition. This served as a comparative tool to demonstrate a quantitatively higher TNF-{Alpha} inhibition (67-71.48%) produced by the dendrimer-dex drug conjugate. The structure activity relationship (dose-for-dose) was inferred by relatively lesser inhibition of TNF-{Alpha} by variants of PAMAM G4 (NH2) dendrimer-dex conjugates and was compared with liposomes carrying dex. In vitro results suggest that the prodrug conjugates of PAMAM dendrimer deliver dex to be more efficient in comparison with liposome-based dex in terms of higher TNF-{Alpha} inhibition. This study has implications in designing efficient prodrug nanocarrier systems for delivering dex.

Copyright © 2013 Elsevier B.V. All rights reserved.

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