04. Evaluation of slow release system of antitumor bioactive organic compounds from Poly (βamino ester)
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Abstract
The present work is a trail to evaluate the synthesized slow release system of composed of poly poly(β-amino ester) (PAE) containing drugs as antitumor for sustained time period. The network structures from poly(β-amino ester) were synthesized via a simplified addition polymerization method to carry drug for applying as drug delivery matrix. It can hold the active organic compounds (drugs) that had an effect as antitumor activity in order to control their release. The active organic compounds that loaded into the prepared polymer matrix, are a new series of heterocyclic derivatives prepared from pyrimidine and naphthyridine namely: 7-(2-methoxy phenyl)-3-methyl-5-thioxo-5,6-dihydro[1,2,4] triazolo [4,3-c] pyrimidine-8-carbonitrile (D1), 7-(2-methoxy phenyl)-3-oxo-5-thioxo-2,3,5, 6-tetrahydro[1,2,4] triazolo [4,3-c] pyrimidine-8-carbonitrile (D2) and (E)-2-((furan-2-yl)methylene)-1-(2,7-dimethyl-1,8-naphthyridin-5-yl)hydrazine (D3).
The resulting polymer structures and the surface morphology of the PAE capsules before and after encapsulation with the active drugs were characterized by SEM. The SEM studies illustrate good dispersion and holding properties of the drug into the network structure of the prepared polymer. In vitro, the release results of the drug from the PAE capsules indicated that the capsules able to give sustained release of drug in DMF up to 15 days at 25°C. The polymer carried active compounds was tested for drug delivery through subjecting to release drug in aqueous media for different time periods and examined as anti-proliferative agents against human liver (HEPG2) cancer cell line.
Results showed that Compound (D2) gave the highest growth inhibition activity followed by compound (D1) while compound (D3) indicated the lowest activity against human liver (HEPG2) cancer cell line. The promising results were obtained from the reveal data resulted for the human liver cancer cell line.
Keywords: Poly(β-amino ester), addition polymerization, drug delivery, swelling, degradation, in vitro release