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Lan Tang, Lulu Fu, Zhuanfeng Zhu, Yan Yang, Boxuan Sun, Weiguang Shan, Zhenhai Zhang
Polymer nanoparticles modified with collagen peptides (CPs) are an attractive strategy for the oral delivery of active ingredients from Chinese medicine. Thus, in the present study, collagen cationic CPs were simply separated using ion-exchange resin from bovine CPs, to modify mixed nanomicelles (MMs) on the surface to improve the oral bioavailability of Cucurbitacin B (CuB). The physicochemical property of micelles was characterized, which confirmed the successful modification of the nanomicelles. CPs-modified nanomicelles in vitro were found to significantly increase cellular uptake and transportation...
January 1, 2018: Drug Delivery
Abanoub S Sedeky, Islam A Khalil, Amr Hefnawy, Ibrahim M El-Sherbiny
Brain tumor has a low prognosis with only 15% survival rate (5 years after diagnosis). Many of the current therapeutics have limited activity due to their inability to cross the blood brain barrier which retards drug accumulation in tumor site and causes drug resistance. Piperine, a phytochemical drug with poor solubility, could be an alternative to current therapeutics after evading its solubility and permeability limitations. Piperine micellization was optimized to improve drug solubility. Positively charged trimethyl-chitosan was synthesized then electrostatically adsorbed onto piperine nanomicelles forming core-shell nanoparticles...
March 26, 2018: European Journal of Pharmaceutical Sciences
Yaqin Zhu, Yu Jiang, Fenghua Meng, Chao Deng, Ru Cheng, Jian Zhang, Jan Feijen, Zhiyuan Zhong
Glioma is a highly challenging human malignancy as drugs typically exhibit a low blood-brain barrier (BBB) permeability as well as poor glioma selectivity and penetration. Here, we report that tandem nanomicelles co-functionalized with brain tumor-targeting and cell-penetrating peptides, Angiopep-2 and TAT, enable a highly efficacious and specific anti-glioma chemotherapy. Interestingly, tandem nanomicelles with 20 mol% Angiopep-2 and 10 mol% TAT linked via long and short poly(ethylene glycol)s, respectively, while maintaining a high glioma cell selectivity display markedly enhanced BBB permeation, glioma accumulation and penetration, and glioma cell uptake...
March 26, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Yi Zhang, Jielin Pan, Qilan Xu, Hao Li, Jianhao Wang, Chao Zhang, Guobin Hong
Objective: To construct carcinoma vascular endothelial-targeted polymeric nanomicelles with high magnetic resonance imaging (MRI) sensitivity and to evaluate their biological safety and in vitro tumor-targeting effect, and to monitor their feasibility using clinical MRI scanner. Method: Amphiphilic block copolymer, poly(ethylene glycol)- b -poly(ε-caprolactone) (PEG-PCL) was synthesized via the ring-opening polymerization of ε-caprolactone (CL) initiated by poly(ethylene glycol) (PEG), in which cyclic pentapeptide Arg-Gly-Asp (cRGD) was conjugated with the terminal of hydrophilic PEG block...
2018: International Journal of Medical Sciences
Juan Li, Yang Du, Zhenqi Jiang, Yuchen Tian, Nianxiang Qiu, Yinjie Wang, Muhammad Zubair Lqbal, Menying Hu, Ruifen Zou, Lijia Luo, Shiyu Du, Jie Tian, Aiguo Wu
Due to the molecular and cellular heterogeneity of glioma, discovery of novel targeted sites and ligands for glioma imaging and therapy remains challenging. Neuropeptide Y (NPY) Y1 receptors (Y1 Rs) are highly over expressed in various brain tumors including glioma, and can serve as potential targeting sites for glioma imaging and therapy. Here, we show by in vivo fluorescent imaging that a highly selective Y1 R ligand, [Asn6 , Pro34 ] NPY (AP-NPY), facilitated circumvention of the blood brain barrier (BBB) by nanomicelles specifically targeting glioma...
March 15, 2018: Nanoscale
Li-Xuan Cai, Shao-Chuan Li, Dan-Ni Yan, Li-Peng Zhou, Fang Guo, Qing-Fu Sun
Transformations within container-molecules provide a good alternative between traditional homogeneous and heter-ogeneous catalysis, as the containers themselves can be regarded as single molecular nanomicelles. We report here the designed-synthesis of a water-soluble redox-active supramolecular Pd4L2 cage and its application in the encapsulation of aromatic molecules and polyoxometalates (POMs) catalysts. Compared to the previous known Pd6L4 cage, our results show that replacement of two cis-blocked palladium corners with p-xylene bridges through pyridinium bonds formation between the 2,4,6-tri-4-pyridyl-1,3,5-triazine (TPT) ligands not only provides reversible redox-activities for the new Pd4L2 cage, but also realizes the expansion and subdivision of its internal cavity...
March 13, 2018: Journal of the American Chemical Society
Rui-Jun Ju, Li-Min Mu, Xue-Tao Li, Cui-Qing Li, Zhan-Jie Cheng, Wan-Liang Lu
The efficacy of anticancer drugs is rather limited in the treatment of brain glioma due to the hindrance of the blood-brain barrier (BBB). Herein, we reported an easy formulation of functional docetaxel nanomicelles for the treatment of brain glioma using a graft copolymer soluplus as basic material through dual-modifications with a glucose-lipid derivative and a dequalinium-lipid derivative. The studies were performed on brain glioma U87MG cells, in vitro BBB models and brain glioma-bearing nude mice. The functional docetaxel nanomicelles were approximately 100 nm...
March 8, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Martin Andersson, Fabrice Gallou, Piyatida Klumphu, Balaram Takale, Bruce Howard Lipshutz
Using density functional theory and the COSMO-RS implicit solvent model, we predict the structure and physical chemical properties of nanomicelles derived from the designer surfactant TPGS-750-M used in organic synthesis. We predict that the influence of chain length of the PEG region is low, while the termination of the PEG chain (-OH vs. -OCH3) plays a very large role. The interfacial tension is considerably lower between the micellar and water phases for the -OH than the -OCH3 terminated surfactant, and our calculations reproduce the large difference observed in average particle size as a function of PEG chain termination...
March 5, 2018: Chemistry: a European Journal
Alexandra Bukchin, Guillem Pascual-Pasto, Maria Cuadrado-Vilanova, Helena Castillo-Ecija, Carles Monterrubio, Nagore G Olaciregui, Monica Vila-Ubach, Laia Ordeix, Jaume Mora, Ángel M Carcaboso, Alejandro Sosnik
We report for the first time on a nano-drug delivery system based on glucosylated polymeric nanomicelles to actively target the second-generation tyrosine kinase inhibitor dasatinib to glucose-avid pediatric sarcomas by the intravenous route. After a comprehensive physicochemical characterization that confirmed the substantially lower critical micellar concentration and the higher encapsulation capacity of the glucosylated amphiphilic nanocarrier with respect to the pristine counterpart, we showed a 9-fold decrease of the half maximal inhibitory concentration of dasatinib in a rhabdomyosarcoma cell line, Rh30, in vitro...
February 28, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Chenxi Qu, Jizhao Li, Yejuan Zhou, Shudi Yang, Weiliang Chen, Fang Li, Bengang You, Yang Liu, Xuenong Zhang
Low accumulation in tumor sites and slow intracellular drug release remain as the obstacles for nanoparticles to achieve effective delivery of chemotherapeutic drugs. In this study, multifunctional micelles were designed to deliver doxorubicin (Dox) to tumor sites to provide more efficient therapy against hepatic carcinoma. The micelles were based on pH-responsive carboxymethyl chitosan (CMCh) modified with a reactive oxygen species (ROS)-responsive segment phenylboronic acid pinacol ester (BAPE) and an active targeted ligand CD147 monoclonal antibody...
February 23, 2018: AAPS Journal
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
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