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[PMID]:28456679
[Au] Autor:Khaliq NU; Oh KS; Sandra FC; Joo Y; Lee J; Byun Y; Kim IS; Kwon IC; Seo JH; Kim SY; Yuk SH
[Ad] Endereço:College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea.
[Ti] Título:Assembly of polymer micelles through the sol-gel transition for effective cancer therapy.
[So] Source:J Control Release;255:258-269, 2017 Jun 10.
[Is] ISSN:1873-4995
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Photo-induced apoptosis-targeted chemotherapy (PIATC) was designed and characterized to propose a new protocol for improved chemotherapy. Intratumoral injection was selected as the mode of administration of the anticancer drug, doxorubicin (DOX). To extend the retention time of DOX at the tumor parenchyma, in-situ gel formation was induced through the sol-gel transition of the Pluronic NPs containing a prodrug of DOX or a photosensitizer. The prodrug (DEVD-S-DOX) was designed to be inactive with a peptide moiety (Aspartic acid-Glutamic acid-Valine-Aspartic acid: DEVD) linked to DOX and to be cleaved into free DOX by caspase-3 expressed with apoptosis. For reactive oxygen species (ROS)-mediated apoptosis, photo-irradiation with methylene blue (MB, photosensitizer) was utilized. The sol-gel transition of the Pluronic NPs containing reactive species, DEVD-S-DOX or MB, was examined by measuring the cloud point and the gel strength in response to temperature change. ROS-mediated apoptosis was observed by measuring the ROS and membrane integrity with induced apoptosis. The in vivo antitumor efficacy of PIATC was measured with a cardiotoxicity assay in tumor-bearing mice.
[Mh] Termos MeSH primário: Antineoplásicos/administração & dosagem
Doxorrubicina/administração & dosagem
Azul de Metileno/administração & dosagem
Fotoquimioterapia
Fármacos Fotossensibilizantes/administração & dosagem
Poloxâmero/administração & dosagem
Pró-Fármacos/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/farmacocinética
Antineoplásicos/uso terapêutico
Apoptose/efeitos dos fármacos
Caspase 3/metabolismo
Linhagem Celular Tumoral
Doxorrubicina/farmacocinética
Doxorrubicina/uso terapêutico
Liberação Controlada de Fármacos
Géis
Luz
Masculino
Azul de Metileno/uso terapêutico
Camundongos Endogâmicos C3H
Micelas
Neoplasias/tratamento farmacológico
Neoplasias/metabolismo
Fármacos Fotossensibilizantes/uso terapêutico
Poloxâmero/uso terapêutico
Pró-Fármacos/farmacocinética
Pró-Fármacos/uso terapêutico
Espécies Reativas de Oxigênio/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Gels); 0 (Micelles); 0 (Photosensitizing Agents); 0 (Prodrugs); 0 (Reactive Oxygen Species); 106392-12-5 (Poloxamer); 80168379AG (Doxorubicin); EC 3.4.22.- (Caspase 3); T42P99266K (Methylene Blue)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170501
[St] Status:MEDLINE


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[PMID]:29441997
[Au] Autor:Bhunchu S; Muangnoi C; Rojsitthisak P; Rojsitthisak P
[Ti] Título:Curcumin diethyl disuccinate encapsulated in chitosan/alginate nanoparticles for improvement of its cytotoxicity against MDA-MB-231 human breast cancer cells.
[So] Source:Pharmazie;71(12):691-700, 2016 Dec 01.
[Is] ISSN:0031-7144
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Curcumin diethyl disuccinate (CDD) is a succinate prodrug of curcuminoids that has better stability in human plasma and improved in vitro cytotoxicity compared to curcumin. Therefore, CDD has the potential for further development as an anticancer agent. In this study, we focused on optimization of the formulation of CDD-loaded chitosan/alginate nanoparticles using Box-Behnken statistical design to enhance the therapeutic efficacy of CDD. Oil-in-water emulsification followed by ionotropic gelification was used to prepare the CDD-loaded chitosan/ alginate nanoparticles. A formulation with a 0.05:1 chitosan/alginate mass ratio, 0.65% (w/v) Pluronic F127 and 1.5 mg/ml CDD was found to be optimal. FTIR, TGA and XRD confirmed the encapsulation of CDD molecules in the nanoparticles. In vitro cytotoxicity and cellular uptake studies showed that CDD-loaded chitosan/alginate nanoparticles had significantly higher cytotoxicity and cellular uptake in human breast adenocarcinoma MDA-MB-231 cells, compared to free CDD. Physical and chemical stability studies indicated that the optimally formulated CDD-loaded chitosan/alginate nanoparticles were stable at 4 °C for 3 months.
[Mh] Termos MeSH primário: Alginatos/química
Antineoplásicos Fitogênicos/administração & dosagem
Antineoplásicos Fitogênicos/farmacologia
Neoplasias da Mama/tratamento farmacológico
Quitosana/química
Curcumina/análogos & derivados
Excipientes/química
Nanopartículas
Succinatos/administração & dosagem
Succinatos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/farmacocinética
Neoplasias da Mama/metabolismo
Linhagem Celular Tumoral
Curcumina/administração & dosagem
Curcumina/farmacocinética
Curcumina/farmacologia
Composição de Medicamentos
Estabilidade de Medicamentos
Emulsões
Feminino
Seres Humanos
Poloxâmero
Pró-Fármacos
Succinatos/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alginates); 0 (Antineoplastic Agents, Phytogenic); 0 (Emulsions); 0 (Excipients); 0 (Prodrugs); 0 (Succinates); 0 (curcumin diethyl disuccinate); 106392-12-5 (Poloxamer); 9012-76-4 (Chitosan); IT942ZTH98 (Curcumin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180215
[St] Status:MEDLINE
[do] DOI:10.1691/ph.2016.6105


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[PMID]:29318229
[Au] Autor:Gjerde N; Zhu K; Nyström B; Knudsen KD
[Ad] Endereço:Department of Chemistry, University of Oslo, P.O. Box 1033, Blindern, N-0315 Oslo, Norway. bo.nystrom@kjemi.uio.no.
[Ti] Título:Effect of PCL end-groups on the self-assembly process of Pluronic in aqueous media.
[So] Source:Phys Chem Chem Phys;20(4):2585-2596, 2018 Jan 24.
[Is] ISSN:1463-9084
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Understanding self-assembly of amphiphilic copolymers in aqueous solution is an important issue in many areas, e.g., in order to tailor-make carriers for drugs and genes. We have synthesized modified versions of the copolymer of type PEO-PPO-PEO (Pluronic, F127), with short (PCL(5)) or long (PCL(11)) PCL blocks at both ends. Turbidity, dynamic light scattering (DLS), small angle neutron scattering (SANS), and rheology measurements were carried out on dilute aqueous solutions of these polymers to investigate their self-assembly behavior. The DLS results clearly show that both micellization and inter-micellization can be controlled by polymer concentration, temperature, and length of the PCL block. The interplay between unimers, micelles, and clusters of micelles could be monitored and the size and size distribution of the species were determined. The SANS data could be portrayed by a spherical core-shell model at all considered conditions of temperature and concentration for F127 and PCL(5) apart from F127 at the lowest temperature measured. The SANS data for PCL(11) were described by a spherical core-shell model at low temperatures, whereas at elevated temperatures asymmetric sub-structures appeared and a cylindrical core-shell model was employed in the analysis of the data. The appearance of pronounced correlation peaks at elevated temperatures signalizes marked intermicellar interactions. The shear viscosity data revealed a minor shear thinning effect, suggesting that the interchain structures are rather stable and not easily disrupted. The work shows that PCL-modification of Pluronic has a large influence on the self-assembly process and on the final structure of the assemblies.
[Mh] Termos MeSH primário: Poloxâmero/química
Poliésteres/química
Água/química
[Mh] Termos MeSH secundário: Difusão Dinâmica da Luz
Espectroscopia de Ressonância Magnética
Nefelometria e Turbidimetria
Difração de Nêutrons
Reologia
Espalhamento a Baixo Ângulo
Resistência ao Cisalhamento
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Polyesters); 059QF0KO0R (Water); 106392-12-5 (Poloxamer); 24980-41-4 (polycaprolactone)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE
[do] DOI:10.1039/c7cp07240f


  4 / 2454 MEDLINE  
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[PMID]:28449430
[Au] Autor:Li S; Xiong Y; Zhang X
[Ad] Endereço:Department of Bone and Soft Tissue Tumor Surgery, Cancer Hospital of China Medical University, Liaoning Cancer Hospital & Institute, Shenyang, Liaoning Province 110042, China.
[Ti] Título:Poloxamer surface modified trimethyl chitosan nanoparticles for the effective delivery of methotrexate in osteosarcoma.
[So] Source:Biomed Pharmacother;90:872-879, 2017 Jun.
[Is] ISSN:1950-6007
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The present work is an effort to explore the poloxamer-modified trimethyl chitosan (TMC) encapsulated MTX for osteosarcoma treatment in order to improve the therapeutic efficacy and minimize severe toxicity associated with the clinical usage of MTX. The methotrexate-loaded pluronic-chitosan nanoparticles (MTCN) was nanosized and exhibited a controlled release of drug from the carrier system. The MTCN showed higher accumulation in cell cytoplasm region evident by the high red fluorescence indicating its uptake through energy-dependent endocytosis process. MTCN exhibited the increased cytotoxicity in MG63 cells compared free MTX due to its enhanced cellular uptake. Especially, MTCN exhibited a superior apoptosis effect with bright chromatin condensation and nuclear fragmentation was observed and showed remarkably higher apoptosis (∼48%) compared to that of free drug. The results of this investigation clearly demonstrate that the poloxamer-modified trimethyl chitosan (TMC) seems to have a great potential as a drug carrier in cancer chemotherapy. The present research work offers immense scope for further exploitation of poloxamer-modified trimethyl chitosan (TMC) in future for the development of nanoparticulate drug delivery system for cancer chemotherapy.
[Mh] Termos MeSH primário: Neoplasias Ósseas/tratamento farmacológico
Quitosana/análogos & derivados
Metotrexato/administração & dosagem
Metotrexato/química
Nanopartículas/química
Osteossarcoma/tratamento farmacológico
Poloxâmero/química
[Mh] Termos MeSH secundário: Antineoplásicos/administração & dosagem
Antineoplásicos/química
Linhagem Celular Tumoral
Quitosana/química
Portadores de Fármacos/química
Sistemas de Liberação de Medicamentos/métodos
Endocitose/efeitos dos fármacos
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Drug Carriers); 0 (pluronic-chitosan); 106392-12-5 (Poloxamer); 9012-76-4 (Chitosan); YL5FZ2Y5U1 (Methotrexate)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE


  5 / 2454 MEDLINE  
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[PMID]:28470260
[Au] Autor:Han Y; Zhang Z; Smith GS; Do C
[Ad] Endereço:Biology and Soft Matter Division, Neutron Sciences Directorate, Oak Ridge National Laboratory, Oak Ridge, TN 37831, USA. doc1@ornl.gov.
[Ti] Título:Effect of nucleoside analogue antimetabolites on the structure of PEO-PPO-PEO micelles investigated by SANS.
[So] Source:Phys Chem Chem Phys;19(24):15686-15692, 2017 Jun 21.
[Is] ISSN:1463-9084
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The effect of three nucleoside analogue antimetabolites (5-fluorouracil, floxuridine, and gemcitabine) on the structure of Pluronic L62 copolymer micelles was investigated using small-angle neutron scattering. These antimetabolites used for cancer chemotherapy have analogous molecular structures but different molecular sizes and aqueous solubilities. It was found that the addition of the three antimetabolites slightly reduced the micellar size and aggregation number, and the micellar anisotropy. The added antimetabolites also changed the internal molecular distribution of the micelles as measured by the scattering length densities, resulting in enhanced hydration of the hydrophobic core region of the micelle. The strength of the effect was found to correlate with the molecular properties of the model drugs, i.e. a larger molecular size and a higher aqueous solubility lead to enhanced hydration of the micellar core.
[Mh] Termos MeSH primário: Antimetabólitos/química
Micelas
Difração de Nêutrons
Polietilenoglicóis/química
Propilenoglicóis/química
Espalhamento a Baixo Ângulo
[Mh] Termos MeSH secundário: Desoxicitidina/análogos & derivados
Desoxicitidina/química
Floxuridina/química
Fluoruracila/química
Poloxâmero/química
Temperatura de Transição
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimetabolites); 0 (Micelles); 0 (PEO-PPO-PEO); 0 (Propylene Glycols); 039LU44I5M (Floxuridine); 059QF0KO0R (Water); 0W860991D6 (Deoxycytidine); 106392-12-5 (Poloxamer); 30IQX730WE (Polyethylene Glycols); B76N6SBZ8R (gemcitabine); U3P01618RT (Fluorouracil)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE
[do] DOI:10.1039/c7cp02028g


  6 / 2454 MEDLINE  
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[PMID]:28845687
[Au] Autor:Swain RP; Subudhi BB
[Ad] Endereço:a Drug Development and Analysis Laboratory, School of Pharmaceutical Sciences , Siksha O Anusandhan University , Bhubaneswar , India.
[Ti] Título:Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation.
[So] Source:Drug Dev Ind Pharm;44(1):56-65, 2018 Jan.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study was undertaken to improve solubility and bioavailability of nateglinide by preparation of stable self-emulsifying solid dispersions (SESDs). The influence of semicrystalline polymers (poloxamer 407, gelucire 50/13) and method of preparation on dissolution behavior, in vivo performance and stability of nateglinide SESDs were investigated. After optimization, SESDs were prepared at 1:5 weight ratio of nateglinide and polymer individually. All the SESDs were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Aqueous solubility of nateglinide was enhanced by 91.82-fold. The SESDs (poloxamer 407-based solid dispersions) achieved rapid and complete drug release (∼100% within 45 min) at pH 2. The improved dissolution appeared to be well correlated with the enhanced bioavailability of nateglinide in rabbits. After oral administration of SESDs (poloxamer 407-based solid dispersions), C and AUC of nateglinide were increased by ∼2.92 and 1.77-folds, respectively, signifying the effectiveness of solid dispersions to improve the bioavailability of nateglinide. Stability during storage was established to show prevention of recrystallization. In conclusion, SESDs with poloxamer 407 in solvent method appeared to be an economic and promising technique to improve the dissolution, bioavailability, and stability of nateglinide.
[Mh] Termos MeSH primário: Cicloexanos/química
Portadores de Fármacos/química
Emulsões/farmacocinética
Fenilalanina/análogos & derivados
Poloxâmero/química
Polímeros/química
Espectroscopia de Infravermelho com Transformada de Fourier/métodos
[Mh] Termos MeSH secundário: Administração Oral
Animais
Disponibilidade Biológica
Varredura Diferencial de Calorimetria
Liberação Controlada de Fármacos
Emulsões/química
Fenilalanina/química
Coelhos
Solubilidade
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanes); 0 (Drug Carriers); 0 (Emulsions); 0 (Polymers); 106392-12-5 (Poloxamer); 41X3PWK4O2 (nateglinide); 47E5O17Y3R (Phenylalanine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180111
[Lr] Data última revisão:
180111
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170829
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1371739


  7 / 2454 MEDLINE  
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[PMID]:29016698
[Au] Autor:Pucelik B; Paczynski R; Dubin G; Pereira MM; Arnaut LG; Dabrowski JM
[Ad] Endereço:Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, Krakow, Poland.
[Ti] Título:Properties of halogenated and sulfonated porphyrins relevant for the selection of photosensitizers in anticancer and antimicrobial therapies.
[So] Source:PLoS One;12(10):e0185984, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The impact of substituents on the photochemical and biological properties of tetraphenylporphyrin-based photosensitizers for photodynamic therapy of cancer (PDT) as well as photodynamic inactivation of microorganisms (PDI) was examined. Spectroscopic and physicochemical properties were related with therapeutic efficacy in PDT of cancer and PDI of microbial cells in vitro. Less polar halogenated, sulfonamide porphyrins were most readily taken up by cells compared to hydrophilic and anionic porphyrins. The uptake and PDT of a hydrophilic porphyrin was significantly enhanced with incorporation in polymeric micelles (Pluronic L121). Photodynamic inactivation studies were performed against Gram-positive (S. aureus, E. faecalis), Gram-negative bacteria (E. coli, P. aeruginosa, S. marcescens) and fungal yeast (C. albicans). We observed a 6 logs reduction of S. aureus after irradiation (10 J/cm2) in the presence of 20 µM of hydrophilic porphyrin, but this was not improved with incorporation in Pluronic L121. A 2-3 logs reduction was obtained for E. coli using similar doses, and a decrease of 3-4 logs was achieved for C. albicans. Rational substitution of tetraphenylporphyrins improves their photodynamic properties and informs on strategies to obtain photosensitizers for efficient PDT and PDI. However, the design of the photosensitizers must be accompanied by the development of tailored drug formulations.
[Mh] Termos MeSH primário: Anti-Infecciosos/química
Antineoplásicos/química
Fármacos Fotossensibilizantes/química
Porfirinas/química
[Mh] Termos MeSH secundário: Anti-Infecciosos/síntese química
Anti-Infecciosos/farmacologia
Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Transporte Biológico
Candida albicans/efeitos dos fármacos
Candida albicans/crescimento & desenvolvimento
Candida albicans/efeitos da radiação
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos da radiação
Desenho de Drogas
Enterococcus faecalis/efeitos dos fármacos
Enterococcus faecalis/crescimento & desenvolvimento
Enterococcus faecalis/efeitos da radiação
Escherichia coli/efeitos dos fármacos
Escherichia coli/crescimento & desenvolvimento
Escherichia coli/efeitos da radiação
Halogenação
Seres Humanos
Interações Hidrofóbicas e Hidrofílicas
Luz
Micelas
Testes de Sensibilidade Microbiana
Fotoquimioterapia/métodos
Fármacos Fotossensibilizantes/síntese química
Fármacos Fotossensibilizantes/farmacologia
Poloxâmero/química
Porfirinas/síntese química
Porfirinas/farmacologia
Pseudomonas aeruginosa/efeitos dos fármacos
Pseudomonas aeruginosa/crescimento & desenvolvimento
Pseudomonas aeruginosa/efeitos da radiação
Serratia marcescens/efeitos dos fármacos
Serratia marcescens/crescimento & desenvolvimento
Serratia marcescens/efeitos da radiação
Staphylococcus aureus/efeitos dos fármacos
Staphylococcus aureus/crescimento & desenvolvimento
Staphylococcus aureus/efeitos da radiação
Relação Estrutura-Atividade
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Antineoplastic Agents); 0 (Micelles); 0 (Photosensitizing Agents); 0 (Porphyrins); 0 (Sulfonamides); 106392-12-5 (Poloxamer)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171011
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0185984


  8 / 2454 MEDLINE  
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[PMID]:28982137
[Au] Autor:Risselada M; Linder KE; Griffith E; Roberts BV; Davidson G; Zamboni WC; Messenger KM
[Ad] Endereço:Department of Clinical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, North Carolina, United States of America.
[Ti] Título:Pharmacokinetics and toxicity of subcutaneous administration of carboplatin in poloxamer 407 in a rodent model pilot study.
[So] Source:PLoS One;12(10):e0186018, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The objectives of this study were to assess the pharmacokinetics and safety of subcutaneously delivered carboplatin in poloxamer 407 in rats. Carboplatin (5mg/rat) in 0.5ml poloxamer 407 (1.0 ml total volume) was administered subcutaneously in a right subcutaneous perineal incision in all 12 treatment rats. Three control rats received 1.0 ml of poloxamer 407. Total platinum was measured in plasma q24hrs from 0 to 168hrs. Protein-unbound platinum was measured in plasma at 168hrs. After sacrifice on day 7, total platinum was determined in wound bed muscle. Platinum concentrations in all samples were measured by ICP-MS. Wounds were visually assessed daily for 7 days. Perineal tissues (full wound bed including muscle, subcutis, skin) were assessed histologically and scored. Total platinum was detectable in plasma from 24 to 168 hrs. Total plasma platinum AUC and Cmax were 9,165.3 ng/mL•h and 129.4 ng/mL. Day 7 total platinum concentration in muscle was approximately 10-fold higher than total plasma platinum concentration. No unbound platinum was detected in plasma samples at 168 hours. No wound healing complications were detected at any time point, nor was tissue necrosis observed histologically. The results of this study suggest that subcutaneous carboplatin in poloxamer 407 can be used in vivo providing direct tissue exposure to carboplatin without significant local effects or systemic absorption and without wound healing complications.
[Mh] Termos MeSH primário: Antineoplásicos/farmacocinética
Antineoplásicos/toxicidade
Carboplatina/farmacocinética
Carboplatina/toxicidade
Poloxâmero/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/administração & dosagem
Área Sob a Curva
Carboplatina/administração & dosagem
Feminino
Injeções Subcutâneas
Projetos Piloto
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 106392-12-5 (Poloxamer); BG3F62OND5 (Carboplatin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171006
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0186018


  9 / 2454 MEDLINE  
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[PMID]:28678638
[Au] Autor:Zhang T; Zhou S; Liu Y; Luo X; Di D; Song Y; Liu X; Deng Y
[Ad] Endereço:a College of Pharmacy , Shenyang Pharmaceutical University , Shenyang , P.R. China.
[Ti] Título:Polysialic acid and pluronic F127 mixed polymeric micelles of docetaxel as new approach for enhanced antitumor efficacy.
[So] Source:Drug Dev Ind Pharm;43(11):1827-1835, 2017 Nov.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In our previous study, polysialic acid-octadecyl dimethyl betaine (PSA-BS18) was synthesized and modified to liposomal EPI. Preliminary experiments revealed that the PSA-BS18 was a potential material for targeting tumor site with superior curative effects. In this study, PSA-BS18 and Pluronic F127 (F127) mixed polymeric micelles encapsulated docetaxel (DTX) (FP/DTX) were prepared by a self-assembly method. The FP/DTX was found to have a diameter of 34.83 ± 0.50 nm with a narrow polydispersity, the entrapment efficiency was 99.12 ± 1.17%, and the drug loading efficiency of 1.40 ± 0.01%. The storage and dilution stability of FP/DTX was fine. In vitro release studies demonstrated that FP/DTX had delayed the drug release from the micelles. In vitro cytotoxicity assay on B16 cells presented that FP/DTX led to a stronger cytotoxic activity in comparison to F127 micelles based DTX (F127/DTX) and Tween80-based DTX (Taxotere ). The in vivo imaging study showed that the accumulation of FP/DTX at tumor sites was more than F127/DTX. The in vivo antitumor activity of FP/DTX against B16 tumor xenograft model showed a significant higher inhibition and a lower toxicity compared with F127/DTX and Taxotere . Taken together, the results obtained above showed that PSA-BS18 and F127 mixed polymeric micelles may be a promising strategy for antitumor delivery of DTX.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Poloxâmero/química
Polietilenoglicóis/química
Ácidos Siálicos/química
[Mh] Termos MeSH secundário: Antineoplásicos/química
Portadores de Fármacos
Sistemas de Liberação de Medicamentos
Lipossomos
Micelas
Taxoides
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Drug Carriers); 0 (Liposomes); 0 (Micelles); 0 (Sialic Acids); 0 (Taxoids); 0 (polysialic acid); 106392-12-5 (Poloxamer); 15H5577CQD (docetaxel); 30IQX730WE (Polyethylene Glycols)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170706
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1349784


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[PMID]:28665158
[Au] Autor:Deng L; Wang Y; Gong T; Sun X; Zhang ZR
[Ad] Endereço:a Key Laboratory of Drug Targeting and Delivery Systems , Sichuan University , Chengdu , China.
[Ti] Título:Dissolution and bioavailability enhancement of alpha-asarone by solid dispersions via oral administration.
[So] Source:Drug Dev Ind Pharm;43(11):1817-1826, 2017 Nov.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Alpha (α)-asarone (1-propenyl-2,4,5-methoxybenzol) (ARE) has been extensively used to treat chronic obstructive pulmonary diseases (COPD), bronchial asthma, pneumonia, and epilepsy. Due to its poor solubility and bioavailability, ARE was clinically administered via intravenous injection. However, severe allergies were often reported due to the presence of solublizers in the injection formulation. In our study, we sought to explore the biopharmaceutical classification of ARE, elucidate the mechanisms behind ARE absorption, and to develop a viable formulation to improve the oral bioavailability of ARE. ARE was not a P-glycoprotein substrate, which was absorbed in the passive mode without site specificity in the gastrointestinal tract. Solid dispersions prepared using hydrophilic matrix materials such as Pluronic F68, and polyethylene glycol (PEG) of varying molecular weights (PEG4K, PEG10K, and PEG20K) were proven to significantly improve the dissolution of ARE in vitro and the oral bioavailability of ARE in rats, which represent a promising strategy for the oral administration of ARE and other BCS II compounds.
[Mh] Termos MeSH primário: Anisóis/química
Portadores de Fármacos/química
Poloxâmero/química
Polietilenoglicóis/química
[Mh] Termos MeSH secundário: Administração Oral
Animais
Disponibilidade Biológica
Varredura Diferencial de Calorimetria
Química Farmacêutica
Interações Hidrofóbicas e Hidrofílicas
Poloxâmero/farmacologia
Polietilenoglicóis/farmacologia
Ratos
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anisoles); 0 (Drug Carriers); 0 (asarone); 106392-12-5 (Poloxamer); 30IQX730WE (Polyethylene Glycols)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170701
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1349783



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