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Cardiomyocyte-targeted and 17?-estradiol-loaded acoustic nanoprobes as a theranostic platform for cardiac hypertrophy.


ABSTRACT: Theranostic perfluorocarbon nanoprobes have recently attracted attention due to their fascinating versatility in integrating diagnostics and therapeutics into a single system. Furthermore, although 17?-estradiol (E2) is a potential anti-hypertrophic drug, it has severe non-specific adverse effects in various organs. Therefore, we have developed cardiomyocyte-targeted theranostic nanoprobes to achieve concurrent targeted imaging and treatment of cardiac hypertrophy.We had successfully synthesized E2-loaded, primary cardiomyocyte (PCM) specific peptide-conjugated nanoprobes with perfluorocarbon (PFP) as a core (PCM-E2/PFPs) and demonstrated their stability and homogeneity. In vitro and in vivo studies confirmed that when exposed to low-intensity focused ultrasound (LIFU), these versatile PCM-E2/PFPs can be used as an amplifiable imaging contrast agent. Furthermore, the significantly accelerated release of E2 enhanced the therapeutic efficacy of the drug and prevented systemic side effects. PCM-E2/PFPs?+?LIFU treatment also significantly increased cardiac targeting and circulation time. Further therapeutic evaluations showed that PCM-E2/PFPs?+?LIFU suppressed cardiac hypertrophy to a greater extent compared to other treatments, revealing high efficiency in cardiac-targeted delivery and effective cardioprotection.Our novel theranostic nanoplatform could serve as a potential theranostic vector for cardiac diseases.

SUBMITTER: Zhao X 

PROVIDER: S-EPMC5877324 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature

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Cardiomyocyte-targeted and 17β-estradiol-loaded acoustic nanoprobes as a theranostic platform for cardiac hypertrophy.

Zhao Xueli X   Luo Wen W   Hu Jing J   Zuo Lei L   Wang Jing J   Hu Rui R   Wang Bo B   Xu Lei L   Li Jing J   Wu Meng M   Li Pan P   Liu Liwen L  

Journal of nanobiotechnology 20180330 1


<h4>Background</h4>Theranostic perfluorocarbon nanoprobes have recently attracted attention due to their fascinating versatility in integrating diagnostics and therapeutics into a single system. Furthermore, although 17β-estradiol (E2) is a potential anti-hypertrophic drug, it has severe non-specific adverse effects in various organs. Therefore, we have developed cardiomyocyte-targeted theranostic nanoprobes to achieve concurrent targeted imaging and treatment of cardiac hypertrophy.<h4>Results<  ...[more]

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