Key result
CHP-mel@SPIONs (melatonin encapsulation 77.69%) accumulated more in the heart than mel@SPIONs and ameliorated myocardial hypertrophy and fibrosis in an animal model.
Why the study?
Melatonin ameliorates cardiac hypertrophy and fibrosis but has limited clinical appeal orally due to a short-lasting time in hostile microenvironments.
Does CHP-mel@SPIONs improve targeted delivery and ameliorate myocardial hypertrophy and fibrosis in an animal model of pressure overload-induced cardiac hypertrophy?
Does CHP-mel@SPIONs improve targeted delivery and ameliorate myocardial hypertrophy and fibrosis in an animal model of pressure overload-induced cardiac hypertrophy?
A novel dual-targeting nanoagent (CHP-mel@SPIONs) enhances melatonin delivery to the heart and ameliorates cardiac hypertrophy and fibrosis in a preclinical model.
Hypothesis-generating for targeted nanotherapy in hypertrophy; leaves open translation to human pressure-overload disease.
INTRODUCTION: Currently, the unsatisfactory treatment of cardiac hypertrophy is due to the unbridled myocardial fibrosis. Melatonin has been demonstrated to ameliorate cardiac hypertrophy and its accompanied fibrosis in previous studies. But it is not clinically appealing due to its short-lasting time against the hostile microenvironment when administered orally. METHODS: Herein, to address this, poly (lactide) polycarboxybetaine (PLGA-COOH) accompanied by cardiac homing peptide (CHP) and superparamagnetic iron oxide nanoparticles (SPIONs) were used to establish a novel drug delivery and transportation strategy for melatonin via a facile two-step emulsion method. This study characterized these nanoparticles (CHP-mel@SPIONs) and tested their delivery to the hypertrophied heart and their effect on myocardial hypertrophy and fibrosis in an animal model of pressure overload-induced cardiac hypertrophy. RESULTS: The engineered magnetic nanoparticles of CHP-mel@SPIONs were spherical (diameter = 221 ± 13 nm) and had a negative zeta potential of -19.18 ± 3.27 mV. The CHP-mel@SPIONs displayed excellent drug encapsulation capacities of SPIONs (75.27 ± 3.1%) and melatonin (77.69 ± 6.04%) separately, and their magnetic properties were characterized by constructing magnetic hysteresis curves and exhibited no remnant magnetization or coercivity. The animal experiments showed that compared with mel@SPIONs, CHP-mel@SPIONs accumulated more in the heart, especially in the presence of an external magnetic field, with in vivo echocardiography and RT-PCR and histological assessments confirming the amelioration of the myocardial hypertrophy and fibrosis with low drug doses. CONCLUSION: This simple biocompatible dual-targeting nanoagent may be a potential candidate for the guided clinical therapy of heart disease.
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Zhao et al. (2020) studied pressure overload-induced cardiac hypertrophy. CHP-mel@SPIONs vs. mel@SPIONs was evaluated on myocardial hypertrophy and fibrosis. CHP-mel@SPIONs (melatonin encapsulation 77.69%) accumulated more in the heart than mel@SPIONs and ameliorated myocardial hypertrophy and fibrosis in an animal model.
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