Performance evaluation of PAMAM dendrimer based simvastatin formulations.

Abstract:

:The purpose of this investigation was to evaluate the performance of poly (amidoamine) (PAMAM) dendrimers, with three different surface groups, to be used as drug carriers. Drug-dendrimers complexes were investigated for solubility studies, dissolution studies, in vitro drug release studies, and for stability studies. The solubility enhancement was found maximum with PEGylated dendrimers (33 times) followed by amine (23 times) and hydroxyl (17.5 times) dendrimers. The solubility profile of simvastatin-dendrimer complex showed a linear correlation (Higuchi A(L)-type diagram) between solubility and dendrimers concentration. The formation of the complexes between drug molecules and dendrimers were characterized by the FTIR spectra of these complexes, showing the appearance of the bond formed between the functional groups of the drug (OH and COOH) and dendrimers (NH(2) and OH). The drug-dendrimer complexes displayed the controlled release action during in vitro release studies. Pure simvastatin (SMV) was released in 5h whereas the PEGylated dendrimers-SMV complexes released the drug up to 5 days. The non-PEGylated formulations released the drug up to 24h. Formulations with amine and PEGylated dendrimers were subjected to accelerated stability studies. Formulations with amine dendrimers were found to be most stable in dark, low temperature (0°C) whereas the dark, RT was most suitable storage conditions for formulation with PEGylated dendrimers.

journal_name

Int J Pharm

authors

Kulhari H,Pooja D,Prajapati SK,Chauhan AS

doi

10.1016/j.ijpharm.2010.12.002

subject

Has Abstract

pub_date

2011-02-28 00:00:00

pages

203-9

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(10)00922-1

journal_volume

405

pub_type

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