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Thailandepsin A-loaded and octreotide-functionalized unimolecular micelles for targeted neuroendocrine cancer therapy.
Jaskula-Sztul, Renata; Xu, Wenjin; Chen, Guojun; Harrison, April; Dammalapati, Ajitha; Nair, Renu; Cheng, Yiqiang; Gong, Shaoqin; Chen, Herbert.
Afiliación
  • Jaskula-Sztul R; Department of Surgery, University of Wisconsin, Madison, WI, 53705, USA.
  • Xu W; Department of Biomedical Engineering and Wisconsin Institutes for Discovery, University of Wisconsin-Madison, 1550 Engineering Drive, 3144 Engineering Centers Building, Madison, WI, 53715, USA.
  • Chen G; Department of Biomedical Engineering and Wisconsin Institutes for Discovery, University of Wisconsin-Madison, 1550 Engineering Drive, 3144 Engineering Centers Building, Madison, WI, 53715, USA; Department of Materials Science and Engineering, University of Wisconsin-Madison, Madison, WI, 53715, USA.
  • Harrison A; Department of Surgery, University of Wisconsin, Madison, WI, 53705, USA.
  • Dammalapati A; Department of Surgery, University of Wisconsin, Madison, WI, 53705, USA.
  • Nair R; Department of Surgery, University of Wisconsin, Madison, WI, 53705, USA.
  • Cheng Y; University of Texas Health Sciences Center San Anto-Division, 3500 Camp Bowie Blvd, Fort Worth, TX, 76107, USA.
  • Gong S; Department of Biomedical Engineering and Wisconsin Institutes for Discovery, University of Wisconsin-Madison, 1550 Engineering Drive, 3144 Engineering Centers Building, Madison, WI, 53715, USA; Department of Materials Science and Engineering, University of Wisconsin-Madison, Madison, WI, 53715, USA.
  • Chen H; Department of Surgery, University of Alabama - Birmingham, Birmingham, 1808 7th Avenue South / Suite 502, 35233, AL, USA. Electronic address: herbchen@uab.edu.
Biomaterials ; 91: 1-10, 2016 Jun.
Article en En | MEDLINE | ID: mdl-26994874
Due to the overexpression of somatostatin receptors in neuroendocrine (NE) cancers, drug nanocarriers conjugated with somatostatin analogs, such as octreotide (OCT), for targeted NE cancer therapy may offer increased therapeutic efficacies and decreased adverse effects. In this study, OCT-functionalized unimolecular micelles were prepared using individual hyperbranched polymer molecules consisting of a hyperbranched polymer core (Boltorn(®) H40) and approximately 25 amphiphilic polylactide-poly(ethlyene glycol) (PLA-PEG) block copolymer arms (H40-PLA-PEG-OCH3/OCT). The resulting micelles, exhibiting a uniform core-shell shape and an average hydrodynamic diameter size of 66 nm, were loaded with thailandepsin-A (TDP-A), a relatively new naturally produced histone deacetylase (HDAC) inhibitor. In vitro studies using flow cytometry and confocal laser scanning microscopy (CLSM) demonstrated that OCT conjugation enhanced the cellular uptake of the unimolecular micelles. Consequently, TDP-A-loaded and OCT-conjugated micelles exhibited the highest cytotoxicity and caused the highest reduction of NE tumor markers. Finally, the in vivo studies on NE cancer bearing nude mice demonstrated that TDP-A-loaded and OCT-conjugated micelles possessed superior anticancer activity in comparison with other TDP-A formulations or drug alone, while showing no detectable systemic toxicity. Thus, these TDP-A-loaded and OCT-conjugated micelles offer a promising approach for targeted NE cancer therapy.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Polietilenglicoles / Portadores de Fármacos / Octreótido / Carcinoma Neuroendocrino / Antineoplásicos Hormonales / Depsipéptidos / Inhibidores de Histona Desacetilasas / Lactatos Límite: Animals / Humans / Male Idioma: En Revista: Biomaterials Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Polietilenglicoles / Portadores de Fármacos / Octreótido / Carcinoma Neuroendocrino / Antineoplásicos Hormonales / Depsipéptidos / Inhibidores de Histona Desacetilasas / Lactatos Límite: Animals / Humans / Male Idioma: En Revista: Biomaterials Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Países Bajos