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Dewen Leng, Jun Hu, Xiaolong Huang, Wei He, Yuan Wang, Mei Liu
Initiation and recurrence of lung cancer, the most fatal cancer worldwide, are attributed to lung cancer stem cells (CSCs). Evidence suggests that cancer cells can be turned into CSCs in a spontaneous way, and therefore simultaneous elimination of lung CSCs and cancer cells is crucial to achieve effective therapy of lung cancer. In lung cancer, epidermal growth factor receptor (EGFR) is overexpressed in both CSCs and cancer cells. The present study developed salinomycin poly(ethylene glycol) 2000-distearoylphosphatidylethanolamine nanomicelles conjugated with EGFR aptamers (M-SAL-EGFR) to kill lung CSCs and cancer cells...
August 1, 2018: Journal of Nanoscience and Nanotechnology
Mahdieh Farhangi, Farzad Kobarfard, Arash Mahboubi, Alireza Vatanara, Seyed Alireza Mortazavi
OBJECTIVE: The objective of present study was to evaluate the effect of lipid structure on physicochemical properties of chitosan-fatty acid nanomicelles and prepare an optimum ciprofloxacin loaded formulation from these conjugates which could enhance the antibacterial effects of drug against some important pathogens like P. aeroginosa. SIGNIFICANCE: Nowadays, resistance in infectious diseases is a growing worldwide concern. Nanocarriers can increase the therapeutic index and consequently reduce the antibiotic resistance...
February 16, 2018: Drug Development and Industrial Pharmacy
Reju George Thomas, Myeong Ju Moon, Suchithra Poilil Surendran, Hyeong Ju Park, In-Kyu Park, Byeong-Il Lee, Yong Yeon Jeong
PURPOSE: Paclitaxel (PTX) loaded hydrophobically modified glycol chitosan (HGC) micelle is biocompatible in nature, but it requires cancer targeting ability and stimuli release property for better efficiency. To improve tumor retention and drug release characteristic of HGC-PTX nanomicelles, we conjugated cancer targeting heptamethine dye, MHI-148, which acts as an optical imaging agent, targeting moiety and also trigger on-demand drug release on application of NIR 808 nm laser. PROCEDURES: The amine group of glycol chitosan modified with hydrophobic 5β-cholanic acid and the carboxyl group of MHI-148 were bonded by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide/N-hydroxysuccinimide chemistry...
February 15, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Ling-Hui Dian, Ying-Jie Hu, Jia-Ye Lin, Jing-Ying Zhang, Yan Yan, Yi-Nuo Cui, Zhan-Bo Su, Wan-Liang Lu
Aim: Oral chemotherapy using anticancer drugs would improve the clinical practice and the life quality of patients. The aim of the present study was to develop paclitaxel hybrid nanomicelles for oral administration to treat resistant breast cancer. Methods: Evaluations were performed on human breast cancer MCF-7 cells, drug-resistant breast cancer MCF-7/Adr cells, and in MCF-7/Adr-xenografted BALB/c nude mice. The nanomicelles were composed of the polymer soluplus, d-α-tocopheryl polyethyleneglycol 1000 succinate (TPGS 1000 ), and dequalinium (DQA)...
2018: International Journal of Nanomedicine
Kholoud Arafa, Rehab N Shamma, Omaima N El-Gazayerly, Ibrahim M El-Sherbiny
PURPOSE: Metformin hydrochloride (MF) repurposing as adjuvant anticancer therapy for colorectal cancer (CRC) proved effective. Several studies attempted to develop MF-loaded nanoparticles (NPs), however the entrapment efficiency (EE%) was poor. Thus, the present study aimed at the facile development of a new series of chitosan (CS)-based semi-interpenetrating network (semi-IPN) NPs incorporating Pluronic ® nanomicelles as nanocarriers for enhanced entrapment and sustained release of MF for efficient treatment of CRC...
February 12, 2018: Drug Development and Industrial Pharmacy
Hamed Vakilzadeh, Jaleh Varshosaz, Mohsen Minaiyan
INTRODUCTION: Triptorelin the synthetic analog of gonadotrophin-releasing hormone is used for treatment of sex hormone dependent diseases via parenteral administration. The aim of the present study was investigation the possibility of triptorelin pulmonary delivery and preparation of a pulmonary nanocarrier delivery system for it. METHODS: Triptorelin was loaded in Pluronic-F127 grafted poly (methyl vinyl ether-alt-maleic acid) nanomicelles by direct dissolution method...
February 8, 2018: Current Drug Delivery
Chunqi Zhu, Hanbo Zhang, Wei Li, Lihua Luo, Xiaomeng Guo, Zuhua Wang, Fenfen Kong, Qingpo Li, Jie Yang, Yongzhong Du, Jian You
The treatment of metastatic cancer is a huge challenge at the moment. Highly precise targeting delivery and drug release in tumor have always been our pursuit in cancer therapy, especially to advance cancer with metastasis, for increasing the efficacy and biosafety. We established a smart nanosized micelle, formed by tocopherol succinate (TOS) conjugated hyaluronic acid (HA) using a disulfide bond linker. The micelle (HA-SS-TOS, HSST) can highly specifically bind with CD44 receptor over-expressed tumor, and response selectively to high GSH level in the cells, inducing disulfide bond breakage and the release of the payload (paclitaxel, PTX)...
February 1, 2018: Biomaterials
Naoual Dahmana, Thibault Mugnier, Doris Gabriel, Vassilios Kaltsatos, Thierry Bertaim, Francine Behar-Cohen, Robert Gurny, Yogeshvar Nath Kalia
The objective was to investigate whether mineralocorticoid receptor antagonism using a novel topical micellar formulation of spironolactone could prevent glucocorticoid-induced delayed corneal wound healing in New Zealand white rabbits. Spironolactone micelles (0.1%, w/v) with a mean number weighted diameter of 20 nm were prepared using a pegylated copolymer (mPEG-dihexPLA) and showed a preliminary stability of at least 12 months at 5°C. Preclinical studies in New Zealand white rabbits demonstrated that the 0...
February 4, 2018: Molecular Pharmaceutics
Yu-Hua Weng, Xiao-Wei Ma, Jing Che, Chan Li, Juan Liu, Shi-Zhu Chen, Yu-Qin Wang, Ya-Ling Gan, Hao Chen, Zhong-Bo Hu, Kai-Hui Nan, Xing-Jie Liang
Ocular inflammations are common diseases that may lead to serious vision-threatening obstacles. Eye drops for antiinflammation therapy need to be administered multiple times daily at a high dosage due to the rapid precorneal removal and low bioavailability of drugs. To overcome these problems, a cRGD-functionalized DSPE-PEG2000 nanomicelle (DSPE-PEG2000-cRGD) encapsulated with flurbiprofen is proposed. The tailored nanomicelles trigger specific binding to integrin receptors on the ocular surface, which leads to rapid and robust mucoadhesion, superior ocular surface retention, and transcorneal penetration behaviors of nanomicelles...
January 2018: Advanced Science (Weinheim, Baden-Wurttemberg, Germany)
Nalinikanth Kotagiri, Matthew L Cooper, Michael Rettig, Christopher Egbulefu, Julie Prior, Grace Cui, Partha Karmakar, Mingzhou Zhou, Xiaoxia Yang, Gail Sudlow, Lynne Marsala, Chantiya Chanswangphuwana, Lan Lu, LeMoyne Habimana-Griffin, Monica Shokeen, Xinming Xu, Katherine Weilbaecher, Michael Tomasson, Gregory Lanza, John F DiPersio, Samuel Achilefu
Most cancer patients succumb to disseminated disease because conventional systemic therapies lack spatiotemporal control of their toxic effects in vivo, particularly in a complicated milieu such as bone marrow where progenitor stem cells reside. Here, we demonstrate the treatment of disseminated cancer by photoactivatable drugs using radiopharmaceuticals. An orthogonal-targeting strategy and a contact-facilitated nanomicelle technology enabled highly selective delivery and co-localization of titanocene and radiolabelled fluorodeoxyglucose in disseminated multiple myeloma cells...
January 18, 2018: Nature Communications
Sachin Handa, Justin D Smith, Yitao Zhang, Balaram S Takale, Fabrice Gallou, Bruce H Lipshutz
Complexation of ca. 1000 ppm Pd(OAc)2 with the ligand HandaPhos (1-1.5:1) leads to a precatalyst that efficiently mediates Sonogashira couplings in aqueous nanomicelles under very mild conditions. Neither copper nor organic solvent is required in the reaction medium, and the product can be isolated directly from the reaction flask, leaving behind a reaction mixture that can be recycled without additional additives.
January 17, 2018: Organic Letters
Jaleh Varshosaz, Vahab Ziaei, Mohsen Minaiyan, Ali Jahanian, Leila Seyed Tabatabaei
The purpose of the present study was to enhance the bioavailability and anti-osteoporotic effects of raloxifene HCl (RH) by increasing its solubility and inhibition of the p-glycoprotein-pump using surfactant micelles of Igepal CO-890. The micelles were prepared by the direct method and their critical micellar concentration, drug dissolution rate, saturated solubility, drug loading and surface morphology were defined. The cytotoxicity of Igepal CO-890 and its ability to inhibit the p-glycoprotein pump were studied on Caco-2 cells...
January 16, 2018: Pharmaceutical Development and Technology
Guang-Yu Pan, Hao-Ran Jia, Ya-Xuan Zhu, Fu-Gen Wu
Developing biocompatible and photodegradable photothermal agents (PTAs) holds great promise for potential clinical applications in photothermal cancer therapy. Herein, a new PTA was innovatively constructed by conjugating the hydrophobic near-infrared (NIR) heptamethine cyanine molecule IR825-NH2 with a double hydrophilic block copolymer methoxypoly(ethylene glycol)5k-block-poly(l-aspartic acid sodium salt)10 (abbreviated as PEG-PLD) via amine-carboxyl reaction. The as-designed PEG-PLD(IR825) was amphiphilic and could self-assemble into polymeric nanomicelles in aqueous solutions...
January 12, 2018: Nanoscale
Chi Zhang, Li-Han Liu, Wen-Xiu Qiu, Yao-Hui Zhang, Wen Song, Lu Zhang, Shi-Bo Wang, Xian-Zheng Zhang
Multidrug resistance (MDR) remains one of the biggest obstacles in chemotherapy of tumor mainly due to P-glycoprotein (P-gp)-mediated drug efflux. Here, a transformable chimeric peptide is designed to target and self-assemble on cell membrane for encapsulating cells and overcoming tumor MDR. This chimeric peptide (C16 -K(TPE)-GGGH-GFLGK-PEG8 , denoted as CTGP) with cathepsin B-responsive and cell membrane-targeting abilities can self-assemble into nanomicelles and further encapsulate the therapeutic agent doxorubicin (termed as CTGP@DOX)...
January 11, 2018: Small
Ana V Lechuga-Vieco, Hugo Groult, Juan Pellico, Jesús Mateo, Jose A Enríquez, Jesús Ruiz-Cabello, Fernando Herranz
ApoB-100 and Phosphatidylcholine-specific phospholipase C (PC-PLC) are important contributors to atherosclerosis development. ApoB-100 is the main structural protein of LDL, being directly associated with atherosclerosis plaque generation. PC-PLC is highly expressed in atherosclerosis lesions and contributes to their progression. We show how phosphatidylcholine-coated nanomicelles can be used for specific characterisation of atherosclerosis plaque. Results show that ApoB-100 in the protein corona of the nanomicelle targets the particles to atherosclerotic areas in apolipoprotein E-/- mice...
January 6, 2018: Nanomedicine: Nanotechnology, Biology, and Medicine
Na-Na Han, Xia Li, Ling Tao, Qi Zhou
Tumor targeting delivery system has been suggested as an attractive strategy against tumor progression. Combination chemotherapy is essential and effective in preventing ovarian cancer. Rhein (4, 5-dihydroxyanthraquinone-2-carboxylic acid) is a lipophilic anthraquinone. Emerging evidence indicates that rhein has many pharmacological effects, such as nephroprotective, hepatoprotective, anti-inflammatory, antioxidant, and anticancer activities. In our study, doxorubicin (DOX) and rhein (RHE) co-loaded polymeric micelle (nano-DOX/RHE) were prepared to attenuate drug resistance in ovarian cancer cells while promoting the therapeutic efficiency of DOX...
January 6, 2018: Biochemical and Biophysical Research Communications
Li Zhang, Dandan Ren, Jianyu Zhou, Guangneng Peng, Gang Shu, Zhixiang Yuan, Fei Shi, Ling Zhao, Lizi Yin, Guoqing Fan, Chang Liu, Hualin Fu
Toltrazuril (Tol) is a broad-spectrum anticoccidiosis drug that is widely used in the prevention and treatment of coccidiosis infection in poultry and mammals. However, the drug has poor aqueous solubility (25 °C, 0.41 μg/mL), and its dose escalation for systemic administration remains challenging. We engineered a Tol mixed nanomicelle (TMNM) delivery system based on sodium deoxycholate-Brij C20 polyethylene ether-triton x100 (NaDC-Brij58-Tx100) as surfactants by film hydration method. The physical properties of TMNM were characterized, and the pharmacokinetic parameters of Tol and TMNM were compared...
December 16, 2017: Colloids and Surfaces. B, Biointerfaces
Vino T Cheriyan, Hashem O Alsaab, Sreeja Sekhar, Caitlin Stieber, Prashant Kesharwani, Samaresh Sau, Magesh Muthu, Lisa A Polin, Edi Levi, Arun K Iyer, Arun K Rishi
Current treatments for Renal Cell Carcinoma (RCC) include a combination of surgery, targeted therapy, and immunotherapy. Emergence of resistant RCCs contributes to failure of drugs and poor prognosis, and thus warrants development of new and improved treatment options for RCCs. Here we generated and characterized RCC cells that are resistant to Everolimus, a frontline mToR-targeted therapy, and tested whether our novel class of CARP-1 functional mimetic (CFM) compounds inhibit parental and Everolimus-resistant RCC cells...
December 1, 2017: Oncotarget
Amrutha Manigandan, Vandhana Handi, Niranjana Sri Sundaramoorthy, Ramya Dhandapani, Janani Radhakrishnan, Swaminathan Sethuraman, Anuradha Subramanian
Precluding the progression of metastasis with early-diagnosis of triple-negative breast cancer remains challenging due to lack of targeting specificity with poor diagnostic potential. Herein, an amphipathic chitosan-based targeted nanomicellar theranostics (30-45 nm) comprising doxorubicin-superparamagnetic iron oxide nanoparticles complexes (89.23%) with lower critical micelle concentration (0.1 µg/mL) were developed. Micelles exhibits concentration-based contrast enhancement in MRI (r2 6.27mM-1s-1) and hyperthermia rather than thermal-ablation...
December 27, 2017: Bioconjugate Chemistry
Nicholas R Lee, Agata A Bikovtseva, Margery Cortes-Clerget, Fabrice Gallou, Bruce H Lipshutz
An especially mild, safe, efficient, and environmentally responsible reduction of aromatic and heteroaromatic nitro-group-containing educts is reported that utilizes very inexpensive carbonyl iron powder (CIP), a highly active commercial grade of iron powder. These reductions are conducted in the presence of nanomicelles composed of TPGS-750-M in water, a recyclable aqueous micellar reaction medium. This new technology also shows broad scope and scalability and presents opportunities for multistep one-pot sequences involving this reducing agent...
December 5, 2017: Organic Letters
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