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A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability BJPS
Pedreiro,Liliane Neves; Cury,Beatriz Stringhetti Ferreira; Chaud,Marco Vinícius; Gremião,Maria Palmira Daflon.
ABSTRACT Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Zidovudine; Solid dispersion; Mucoadhesion; P-glycoprotein; Intestinal permeability..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400715
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ABCB1 C1236T, G2677T/A and C3435T polymorphisms in systemic lupus erythematosus patients BJMBR
Gonzalez,T.P.; Mucenic,T.; Brenol,J.C.T.; Xavier,R.M.; Schiengold,M.; Chies,J.A.B..
P-glycoprotein (Pgp), the ABCB1 gene product, acts as an efflux pump that transports a large variety of substrates and is a mechanism of cell protection against xenobiotics. An increasing number of studies have shown that some ABCB1 polymorphisms may affect Pgp expression and activity, as well as affecting the development and susceptibility to diseases and pharmacological response. High activity of Pgp has been detected in systemic lupus erythematosus (SLE) patients. The C1236T, G2677T/A, and C3435T are the most commonly studied single nucleotide polymorphisms in the ABCB1 gene. Therefore, their frequencies were determined in Brazilian individuals with European ancestry (N = 143) and in SLE patients (N = 137). Genotyping was performed by PCR-RFLP analysis...
Tipo: Info:eu-repo/semantics/other Palavras-chave: ABCB1; MDR1; P-glycoprotein; Polymorphism; Systemic lupus erythematosus.
Ano: 2008 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2008000900005
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Age-related changes of the multidrug resistance P-glycoprotein function in normal human peripheral blood T lymphocytes BJMBR
Machado,C.G.; Calado,R.T.; Garcia,A.B.; Falcão,R.P..
The multidrug resistance P-glycoprotein is a transmembrane efflux pump expressed by lymphocytes and is involved in their cytolytic activity. In the present study, we investigated the age-related changes of P-glycoprotein function in normal peripheral blood lymphocytes. Blood samples from 90 normal volunteers (age range, 0 to 86 years) were analyzed. P-glycoprotein function was assessed by the flow cytometric rhodamine 123 assay. P-glycoprotein function was highest in cord blood and progressively declined with age in peripheral blood T CD4+ and CD8+ cells. In contrast, P-glycoprotein function did not vary with age in CD19+ B or CD16+CD56+ natural killer cells. These data suggest that the decline in P-glycoprotein function in T CD4+ and CD8+ lymphocytes as a...
Tipo: Info:eu-repo/semantics/article Palavras-chave: P-glycoprotein; Multidrug resistance; Lymphocytes; Rhodamine 123; Flow cytometry.
Ano: 2003 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003001200006
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Flow cytometry protocol to evaluate ionizing radiation effects on P-glycoprotein activity BABT
Santos,Neyliane Gonçalves dos; Amaral,Ademir; Cavalcanti,Mariana Brayner; Neves,Maria Amélia Batista; Machado,Cíntia Gonsalves de Faria.
The aim of this work was to establish a protocol to evaluate ionizing radiation effects on P-glycoprotein (P-gp) activity. For this, human peripheral blood samples were irradiated in vitro with different doses and P-gp activity was analyzed for CD4 and CD8 T lymphocytes through rhodamine123-efflux assay by flow cytometry. By simultaneous employment of percentage and mean fluorescence index parameters, subject-by-subject analysis pointed out changes in P-gp activity for some individuals and irradiated samples. Based on this work, the proposed protocol was considered adequate for evaluating P-gp activity on cells after radioactive stress. Besides, this research suggests that P-gp activity could be an important factor to define patient-specific protocols in...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Combined therapy; Radiation effect; P-glycoprotein; Multidrug resistance; Functional analysis; Flow cytometry.
Ano: 2008 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132008000700018
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Multidrug resistance in tumour cells: characterisation of the multidrug resistant cell line K562-Lucena 1 Anais da ABC (AABC)
RUMJANEK,VIVIAN M.; TRINDADE,GILMA S.; WAGNER-SOUZA,KAREN; MELETTI-DE-OLIVEIRA,MICHELE C.; MARQUES-SANTOS,LUIS F.; MAIA,RAQUEL C.; CAPELLA,MÁRCIA A. M..
Multidrug resistance to chemotherapy is a major obstacle in the treatment of cancer patients. The best characterised mechanism responsible for multidrug resistance involves the expression of the MDR-1 gene product, P-glycoprotein. However, the resistance process is multifactorial. Studies of multidrug resistance mechanisms have relied on the analysis of cancer cell lines that have been selected and present cross-reactivity to a broad range of anticancer agents. This work characterises a multidrug resistant cell line, originally selected for resistance to the Vinca alkaloid vincristine and derived from the human erythroleukaemia cell K562. This cell line, named Lucena 1, overexpresses P-glycoprotein and have its resistance reversed by the chemosensitisers...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Multidrug resistance; Leukaemia; P-glycoprotein; Chemosensitisers.
Ano: 2001 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652001000100007
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Multi-drug resistance (MDR1) gene and P-glycoprotein influence on pharmacokinetic and pharmacodymanic of therapeutic drugs Ciência Rural
Linardi,Renata Lehn; Natalini,Cláudio Corrêa.
(MDR1) gene expressed in tumor cells and also in several normal tissues, such as intestine, liver, kidney, blood-brain barrier, spinal cord, and placenta. P-gp has been identified in mice, rat, bovine, monkey, rodents, and human beings and has been receiving a particular clinical relevance because this protein expression limits brain access and intestinal absorption of many drugs. This protein plays a role as a protective barrier against a wide variety of substrates, avoiding drug entry into the central nervous system. P-glycoprotein also interferes with drug bioavailability and disposition, including absorption, distribution, metabolization, and excretion, influencing pharmacokinetic and pharmacodynamic of drugs. Modulation of P-gp may help the efficacy...
Tipo: Info:eu-repo/semantics/article Palavras-chave: MDR1 gene; P-glycoprotein; Therapeutics; Pharmacology.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100056
Registros recuperados: 6
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