Preparation, characterization, and drug release behavior of nitrendipine encapsulated grafted copolymer microspheres

Abstract

The major global cause for human premature death is hypertension. It leads to cardiac attack, cardiac failure, kidney failure, and cognitive decline. The statistical research data issued by the Fourth National Family health survey of India revealed that 20% of the adults in India suffered from high blood pressure. In this study, three different amounts of acrylamide were grafted with the same amount of sodium alginate. The grafting parameters such as grafting percentage were evaluated for the three samples and observed that the ratio 1:4 shows the higher grafting percentage which is considered for further study. The microsphere of grafted copolymers with and without drug was prepared by a free radical mechanism. Characterization was done to know the chemical interactions and the morphological effects of microsphere formation without and with a drug. Drug release behavior of the insoluble antihypertensive drug, Nitrendipine was done with the help of in-vitro drug release studies. Sustained slow drug discharge in both stomach and intestinal media was identified. The amount of polymer, their viscosity, and a cross-linking agent was mainly responsible for controlled release. The API release from the grafted copolymer follows the non-fickian diffusion mechanism. The bioavailability of the drug is improved by the usage of microsphere-based controlled delivery systems. Usage of Hydrophilic polymers, acrylamide along sodium alginate improve the active pharmaceutical ingredient (API) release and the side effects were reduced. From these results, we concluded that sodium alginate grafted acrylamide would be a good drug matrix for the controlled drug release.