Cardiovascular disease (CVD) is the leading cause of mortality and disability worldwide, with 17.9 million annual deaths, including myocardial infarction caused by atherosclerosis [1]. Atherosclerosis is a complicated cardiovascular disease caused by multiple factors, including aging, inflammation, coronary artery blockage, oxidative stress, and plaque rupture, which causes myocardial ischemia (MI) and damages the heart muscle [2]. Current clinical strategies face limitations such as a lack of regeneration of damaged muscle and residual heart failure progression (e.g., pharmacological treatments and reperfusion therapies), leading to death [3]. Targeted drug delivery systems, including nanomedicine, nanoparticles and microsphere therapies, are being investigated to improve cardiomyocyte renewal. In this study, we designed a cardiomyocyte-loaded Gelatin-Alginate (GA) microsphere conjugated with LA (lipoic acid) and CMP (WLSEAGPVVTVRALRGTGSW) peptide to treat damaged heart tissue by using the electrostatic spray drying technique. We determined the chemical groups and morphological analyses of the microsphere using FT-IR, 1H NMR, and EDS-SEM. Dose-dependent cytotoxicity of drug and peptide conjugation on cell-loaded microspheres was obtained on days 4, 8, and 12 of incubation using the CCK-8 assay and live-dead assay. The cytotoxicity results showed the cell viability increased from 72% to 100% on day 12, indicating that drug and peptide conjugation increased cell regeneration. Thus, this treatment method may be part of a promising next-generation cellular therapy in the future.