Faculty Collaboration Database

Performance evaluation of PAMAM dendrimer based simvastatin formulations. Int J Pharm 2011 Feb 28;405(1-2):203-9

Date

12/15/2010

Pubmed ID

21145960

DOI

10.1016/j.ijpharm.2010.12.002

Scopus ID

2-s2.0-79151485330 (requires institutional sign-in at Scopus site)   91 Citations

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.

Author List

Kulhari H, Pooja D, Prajapati SK, Chauhan AS

Author

Abhay Chauhan PhD Associate Professor in the School of Pharmacy Administration department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Anticholesteremic Agents
Chemistry, Pharmaceutical
Dendrimers
Drug Carriers
Drug Stability
Hydrogen-Ion Concentration
Molecular Structure
Polymers
Simvastatin
Solubility