Folated Synperonic-Cholesteryl Hemisuccinate Polymeric Micelles for the Targeted Delivery of Docetaxel in Melanoma

Varshosaz, Jaleh; Taymouri, Somayeh; Hassanzadeh, Farshid; Haghjooy Javanmard, Shaghayegh; Rostami, Mahboobeh
March 2015
BioMed Research International;3/8/2015, Vol. 2015, p1
Academic Journal
The objective of this study was the synthesis of folic acid- (FA-) targeted polymeric micelles of Synperonic PE/F 127-cholesteryl hemisuccinate (PF127-Chol) for specific delivery of docetaxel (DTX). Targeted or nontargeted micelles loaded with DTX were prepared via dialysis method. The effects of processing variables on the physicochemical properties of targeted micelles were evaluated using a full factorial design. After the optimization of the polymer/drug ratio, the organic solvent type used for the preparation of the micelles, and the temperature of dialyzing medium, the in vitro cytotoxicity and cellular uptake of the optimized micelles were studied on B16F10 melanoma cells by flow cytometry and fluorescent microscopy. The anticancer efficacy of DTX-loaded FA-PF127-Chol was evaluated in mice bearing melanoma tumor. Optimized targeted micelles had the particle size of 171.3 nm, zeta potential of −7.8 mV, PDI of 0.325, and a high encapsulation efficiency that released the drug within 144 h. The MTT assay indicated that targeted micelles carrying DTX were significantly more cytotoxic, had higher cellular uptake, and reduced the tumor volume significantly more than the nontargeted micelles and the free drug. FA-PF127-Chol could be, therefore, a promising biomaterial for tumors overexpressing folate receptors.


Related Articles

  • Dynamic Fluctuation of Circulating Tumor Cells during Cancer Progression. Juratli, Mazen A.; Sarimollaoglu, Mustafa; Nedosekin, Dmitry A.; Melerzanov, Alexander V.; Zharov, Vladimir P.; Galanzha, Ekaterina I. // Cancers;Mar2014, Vol. 6 Issue 1, p128 

    Circulating tumor cells (CTCs) are a promising diagnostic and prognostic biomarker for metastatic tumors. We demonstrate that CTCs' diagnostic value might be increased through real-time monitoring of CTC dynamics. Using preclinical animal models of breast cancer and melanoma and in vivo flow...

  • A Novel Pharmacological Method to Study the Chinese Medicinal Formula Hua-Zheng-Hui-Sheng-Dan. Cao, Rui; Zhang, Hong; Guo, Jie; Liu, Xiao-hui; Liu, Chang; Zhu, Cui-hong; Wu, Xiong-zhi // Evidence-based Complementary & Alternative Medicine (eCAM);9/1/2015, Vol. 2015, p1 

    Objectives. Hua-Zheng-Hui-Sheng-Dan (HZHSD) was used as an experimental model to explore research methods of large formulae in traditional Chinese medicine (TCM) using current molecular biology approaches. Materials and Methods. The trypan blue exclusion assay was used to determine cell...

  • In Vivo Osteogenesis and In Vitro Streptococcus mutans Adherence: Porous-Surfaced Cylindrical Implants vs Rough-Surfaced Threaded Implants. Prado, Renata Falchete do; Vasconcellos, Luis Gustavo Oliveira de; Vasconcellos, Luana Marotta Reis de; Cairo, Carlos Alberto Alves; Leite, Daniel de Oliveira; dos Santos, Alessandra; Jorge, Antônio Olavo Cardoso; Romeiro, Rogério de Lima; Balducci, Ivan; Carvalho, Yasmin Rodarte // International Journal of Oral & Maxillofacial Implants;2013, Vol. 28 Issue 6, p1630 

    Purpose: To analyze and compare bone apposition at the interface of commercially available rough-surfaced, threaded implants with porous-surfaced, cylindrical implants after several healing periods in a rabbit model. In addition, the study aimed to elucidate the influence of the implant surface...

  • In-vitro/In-vivo comparison of leuprolide acetate release from an in-situ forming plga system. Mashayekhi, Roya; Mobedi, Hamid; Najafi, Jamal; Enayati, Marjan // DARU;2013, Vol. 21 Issue 7, p57 

    A poly (lactide-co-glycolide) (PLGA) implant was used to control the release profile of leuprolide acetate (LA) drug. The system is an in-situ polymeric precipitation system. And the formulation consisted of PLGA polymer, LA drug and N-methyl-2-pyrrolidon solvent with no additives. First, the...

  • Antiproliferative effect of the jararhagin toxin on B16F10 murine melanoma. Maria, Durvanei Augusto; da Silva, Manuela Garcia Laveli; Junior, Mario Cesar Correia; Garcia Ruiz, Itamar Romano // BMC Complementary & Alternative Medicine;2014, Vol. 14 Issue 1, p1 

    Background Malignant melanoma is a less common but highly dangerous form of skin cancer; it starts in the melanocytes cells found in the outer layer of the skin. Jararhagin toxin, a metalloproteinase isolated from Bothrops jararaca snake venom acts upon several biological processes, as...

  • Sonic hedgehog antagonists induce cell death in acute myeloid leukemia cells with the presence of lipopolysaccharides, tumor necrosis factor-α, or interferons. Lu, Frank; Yu, Ching-Chia; Chiu, Huei-Hsuan; Liu, Hsingjin; Chen, Shao-Yin; Lin, Shufan; Goh, Ting-Yi; Hsu, Hsin-Chih; Chien, Chih-Han; Wu, Han-Chung; Chen, Ming-Shan; Schuyler, Scott; Hsieh, Wu-Shiun; Wu, Mei-Hwan; Lu, Jean // Investigational New Drugs;Aug2013, Vol. 31 Issue 4, p823 

    Due to the development of drug resistance, the outcome for the majority of patients with acute myeloid leukemia (acute myelogenous leukemia; AML) remains poor. To prevent drug resistance and increase the therapeutic efficacy of treating AML, the development of new combinatory drug therapies is...

  • Gallotannin-rich Caesalpinia spinosa fraction decreases the primary tumor and factors associated with poor prognosis in a murine breast cancer model. Urueña, Claudia; Mancipe, Juan; Hernandez, John; Castañeda, Diana; Pombo, Luis; Gomez, Alejandra; Asea, Alexzander; Fiorentino, Susana // BMC Complementary & Alternative Medicine;2013, Vol. 13 Issue 1, p74 

    Background: Several treatment alternatives are available for primary breast cancer, although those for metastatic disease or inflammation associated with tumor progression are ineffective. Therefore, there is a great need for new therapeutic alternatives capable of generating an immune response...

  • Evaluation of two I-radiolabeled acridine derivatives for Auger-electron radionuclide therapy of melanoma. Gardette, Maryline; Viallard, Claire; Paillas, Salomé; Guerquin-Kern, Jean-Luc; Papon, Janine; Moins, Nicole; Labarre, Pierre; Desbois, Nicolas; Wong-Wah-Chung, Pascal; Palle, Sabine; Wu, Ting-Di; Pouget, Jean-Pierre; Miot-Noirault, Elisabeth; Chezal, Jean-Michel; Degoul, Francoise // Investigational New Drugs;Aug2014, Vol. 32 Issue 4, p587 

    We previously selected two melanin-targeting radioligands [I]ICF01035 and [I]ICF01040 for melanoma-targeted I radionuclide therapy according to their pharmacological profile in mice bearing B16F0 tumors. Here we demonstrate in vitro that these compounds present different radiotoxicities in...

  • Essential oil of Melaleuca alternifolia for the treatment of oral candidiasis induced in an immunosuppressed mouse model. de Campos Rasteiro, Vanessa Maria; da Costa, Anna Carolina Borges Pereira; Araújo, Cássia Fernandes; De Barros, Patrícia Pimentel; Rossoni, Rodnei Dennis; Anbinder, Ana Lia; Cardoso Jorge, Antonio Olavo; Junqueira, Juliana Campos // BMC Complementary & Alternative Medicine;2014, Vol. 14 Issue 1, p454 

    Background The search for alternative therapies for oral candidiasis is a necessity and the use of medicinal plants seems to be one of the promising solutions. The objective of this study was to evaluate the in vitro and in vivo effects of the essential oil of Melaleuca alternifolia on Candida...


Read the Article


Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics