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[PMID]:29216591
[Au] Autor:Sun Y; Jensen H; Petersen NJ; Larsen SW; Østergaard J
[Ad] Endereço:Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark. Electronic address: yu.sun@sund.ku.dk.
[Ti] Título:Concomitant monitoring of implant formation and drug release of in situ forming poly (lactide-co-glycolide acid) implants in a hydrogel matrix mimicking the subcutis using UV-vis imaging.
[So] Source:J Pharm Biomed Anal;150:95-106, 2018 Feb 20.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:For poly (lactide-co-glycolide acid) (PLGA)-based in situ forming implants, the rate of implant formation plays an important role in determining the overall drug release kinetics. Currently, in vitro techniques capable of characterizing the processes of drug release and implant formation at the same time are not available. A hydrogel-based in vitro experimental setup was recently developed requiring only microliter of formulation and forming a closed system potentially suitable for interfacing with various spectroscopic techniques. The aim of the present proof-of-concept study was to investigate the feasibility of concomitant UV imaging, Vis imaging and light microscopy for detailed characterization of the behavior of in situ forming PLGA implants in the hydrogel matrix mimicking the subcutis. The model compounds, piroxicam and α-lactalbumin were added to PLGA-1-methyl-2-pyrrolidinone and PLGA-triacetin solutions. Upon bringing the PLGA-solvent-compound pre-formulation in contact with the hydrogel, Vis imaging and light microscopy were applied to visualize the depot formation and UV imaging was used to quantify drug transport in the hydrogel. As compared to piroxicam, the α-lactalbumin invoked an acceleration of phase separation and an increase of implant size. α-Lactalbumin was released faster from the PLGA-1-methyl-2-pyrrolidinone system than the PLGA-triacetin system opposite to the piroxicam release pattern. A linear relationship between the rate of implant formation and initial compound release within the first 4h was established for the PLGA-NMP systems. This implies that phase separation may be one of the controlling factors in drug release. The rate of implant formation may be an important parameter for predicting and tailoring drug release. The approach combining UV imaging, Vis imaging and light microscopy may facilitate understanding of release processes and holds potential for becoming a useful tool in formulation development of in situ forming implants.
[Mh] Termos MeSH primário: Sistemas de Liberação de Medicamentos
Lactalbumina/administração & dosagem
Ácido Láctico/química
Piroxicam/administração & dosagem
Ácido Poliglicólico/química
[Mh] Termos MeSH secundário: Química Farmacêutica/métodos
Portadores de Fármacos/química
Implantes de Medicamento
Liberação Controlada de Fármacos
Hidrogéis
Pirrolidinonas/química
Espectrofotometria Ultravioleta/métodos
Análise Espectral/métodos
Tela Subcutânea/metabolismo
Triacetina/química
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Drug Implants); 0 (Hydrogels); 0 (Pyrrolidinones); 0 (polylactic acid-polyglycolic acid copolymer); 13T4O6VMAM (Piroxicam); 26009-03-0 (Polyglycolic Acid); 33X04XA5AT (Lactic Acid); 9013-90-5 (Lactalbumin); JR9CE63FPM (N-methylpyrrolidone); XHX3C3X673 (Triacetin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180130
[Lr] Data última revisão:
180130
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171208
[St] Status:MEDLINE


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[PMID]:28574391
[Au] Autor:Gorgiladze T; Nozadze I; Abzianidze E; Tsagareli M
[Ad] Endereço:1Tbilisi State Medical University; 2Beritashvili Center for Experimental Biomedicine, Tbilisi Georgia.
[Ti] Título:NON-STEROIDAL ANTI-INFLAMMATORY DRUGS'S ANTINOCICEPTION MEDIATED BY THE OPIOID MECHANISM IN THE NUCLEUS RAPHE MAGNUS.
[So] Source:Georgian Med News;(265):99-104, 2017 Apr.
[Is] ISSN:1512-0112
[Cp] País de publicação:Georgia (Republic)
[La] Idioma:eng
[Ab] Resumo:It has been established that the midbrain periaqueductal gray matter (PAG) and rostral ventro-medial medulla (RVM) are involved in the descending pain control system. The latter involves the midline nucleus raphe magnus (NRM) and adjacent reticular formation. These brain structures are is one of important parts of CNS circuit that controls nociceptive transmission at the level of spinal cord. Here we report that microinjection of commonly used non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac, ketorolac, metamizol, and xefocam into the NRM produces strong antinociception which is mediated by the opioid mechanism. The experiments were carried out on experimental and control (saline) white albino male rats. Animals were implanted with a guide cannula in the NRM and tested for antinociception following microinjection of NSAIDs into the NRM in the tail flick (TF) and hot plate (HP) tests. The analysis of variance (ANOVA) with post-hoc Tukey-Kramer multiple comparison tests were used for statistical evaluation. The obtained data show that microinjection of these NSAIDs into the NRM produced antinociception as revealed by a latency increase in the tail-flick (TF) and hot plate (HP) latencies compared to the saline control microinjected into the same nucleus. Furthermore, we definitely showed that pre-treatment with opioid antagonist naloxone in the NRM diminishes NSAID-induced antinociception expressing in significant decrease in TF and HP latencies (P<0.001). The present findings support the concept that antinociceptive effects of NSAIDs are mediated via an endogenous opioid system possibly involving the descending pain modulatory circuit.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Naloxona/farmacologia
Antagonistas de Entorpecentes/farmacologia
Nociceptividade/efeitos dos fármacos
Núcleo Magno da Rafe/efeitos dos fármacos
Peptídeos Opioides/metabolismo
[Mh] Termos MeSH secundário: Animais
Diclofenaco/farmacologia
Dipirona/farmacologia
Cetorolaco/farmacologia
Masculino
Microinjeções
Núcleo Magno da Rafe/fisiologia
Piroxicam/análogos & derivados
Piroxicam/farmacologia
Ratos
Tempo de Reação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Narcotic Antagonists); 0 (Opioid Peptides); 13T4O6VMAM (Piroxicam); 144O8QL0L1 (Diclofenac); 36B82AMQ7N (Naloxone); 6429L0L52Y (Dipyrone); ER09126G7A (lornoxicam); YZI5105V0L (Ketorolac)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171110
[Lr] Data última revisão:
171110
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170603
[St] Status:MEDLINE


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[PMID]:28497473
[Au] Autor:Derry S; Wiffen PJ; Kalso EA; Bell RF; Aldington D; Phillips T; Gaskell H; Moore RA
[Ad] Endereço:Pain Research and Nuffield Department of Clinical Neurosciences (Nuffield Division of Anaesthetics), University of Oxford, Pain Research Unit, Churchill Hospital, Oxford, Oxfordshire, UK, OX3 7LE.
[Ti] Título:Topical analgesics for acute and chronic pain in adults - an overview of Cochrane Reviews.
[So] Source:Cochrane Database Syst Rev;5:CD008609, 2017 05 12.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Topical analgesic drugs are used for a variety of painful conditions. Some are acute, typically strains or sprains, tendinopathy, or muscle aches. Others are chronic, typically osteoarthritis of hand or knee, or neuropathic pain. OBJECTIVES: To provide an overview of the analgesic efficacy and associated adverse events of topical analgesics (primarily nonsteroidal anti-inflammatory drugs (NSAIDs), salicylate rubefacients, capsaicin, and lidocaine) applied to intact skin for the treatment of acute and chronic pain in adults. METHODS: We identified systematic reviews in acute and chronic pain published to February 2017 in the Cochrane Database of Systematic Reviews (the Cochrane Library). The primary outcome was at least 50% pain relief (participant-reported) at an appropriate duration. We extracted the number needed to treat for one additional beneficial outcome (NNT) for efficacy outcomes for each topical analgesic or formulation, and the number needed to treat for one additional harmful outcome (NNH) for adverse events. We also extracted information on withdrawals due to lack of efficacy or adverse events, systemic and local adverse events, and serious adverse events. We required information from at least 200 participants, in at least two studies. We judged that there was potential for publication bias if the addition of four studies of typical size (400 participants) with zero effect increased NNT compared with placebo to 10 (minimal clinical utility). We extracted GRADE assessment in the original papers, and made our own GRADE assessment. MAIN RESULTS: Thirteen Cochrane Reviews (206 studies with around 30,700 participants) assessed the efficacy and harms from a range of topical analgesics applied to intact skin in a number of acute and chronic painful conditions. Reviews were overseen by several Review Groups, and concentrated on evidence comparing topical analgesic with topical placebo; comparisons of topical and oral analgesics were rare.For at least 50% pain relief, we considered evidence was moderate or high quality for several therapies, based on the underlying quality of studies and susceptibility to publication bias.In acute musculoskeletal pain (strains and sprains) with assessment at about seven days, therapies were diclofenac Emulgel (78% Emulgel, 20% placebo; 2 studies, 314 participants, NNT 1.8 (95% confidence interval 1.5 to 2.1)), ketoprofen gel (72% ketoprofen, 33% placebo, 5 studies, 348 participants, NNT 2.5 (2.0 to 3.4)), piroxicam gel (70% piroxicam, 47% placebo, 3 studies, 522 participants, NNT 4.4 (3.2 to 6.9)), diclofenac Flector plaster (63% Flector, 41% placebo, 4 studies, 1030 participants, NNT 4.7 (3.7 to 6.5)), and diclofenac other plaster (88% diclofenac plaster, 57% placebo, 3 studies, 474 participants, NNT 3.2 (2.6 to 4.2)).In chronic musculoskeletal pain (mainly hand and knee osteoarthritis) therapies were topical diclofenac preparations for less than six weeks (43% diclofenac, 23% placebo, 5 studies, 732 participants, NNT 5.0 (3.7 to 7.4)), ketoprofen over 6 to 12 weeks (63% ketoprofen, 48% placebo, 4 studies, 2573 participants, NNT 6.9 (5.4 to 9.3)), and topical diclofenac preparations over 6 to 12 weeks (60% diclofenac, 50% placebo, 4 studies, 2343 participants, NNT 9.8 (7.1 to 16)). In postherpetic neuralgia, topical high-concentration capsaicin had moderate-quality evidence of limited efficacy (33% capsaicin, 24% placebo, 2 studies, 571 participants, NNT 11 (6.1 to 62)).We judged evidence of efficacy for other therapies as low or very low quality. Limited evidence of efficacy, potentially subject to publication bias, existed for topical preparations of ibuprofen gels and creams, unspecified diclofenac formulations and diclofenac gel other than Emulgel, indomethacin, and ketoprofen plaster in acute pain conditions, and for salicylate rubefacients for chronic pain conditions. Evidence for other interventions (other topical NSAIDs, topical salicylate in acute pain conditions, low concentration capsaicin, lidocaine, clonidine for neuropathic pain, and herbal remedies for any condition) was very low quality and typically limited to single studies or comparisons with sparse data.We assessed the evidence on withdrawals as moderate or very low quality, because of small numbers of events. In chronic pain conditions lack of efficacy withdrawals were lower with topical diclofenac (6%) than placebo (9%) (11 studies, 3455 participants, number needed to treat to prevent (NNTp) 26, moderate-quality evidence), and topical salicylate (2% vs 7% for placebo) (5 studies, 501 participants, NNTp 21, very low-quality evidence). Adverse event withdrawals were higher with topical capsaicin low-concentration (15%) than placebo (3%) (4 studies, 477 participants, NNH 8, very low-quality evidence), topical salicylate (5% vs 1% for placebo) (7 studies, 735 participants, NNH 26, very low-quality evidence), and topical diclofenac (5% vs 4% for placebo) (12 studies, 3552 participants, NNH 51, very low-quality evidence).In acute pain, systemic or local adverse event rates with topical NSAIDs (4.3%) were no greater than with topical placebo (4.6%) (42 studies, 6740 participants, high quality evidence). In chronic pain local adverse events with topical capsaicin low concentration (63%) were higher than topical placebo (5 studies, 557 participants, number needed to treat for harm (NNH) 2.6), high quality evidence. Moderate-quality evidence indicated more local adverse events than placebo in chronic pain conditions with topical diclofenac (NNH 16) and local pain with topical capsaicin high-concentration (NNH 16). There was moderate-quality evidence of no additional local adverse events with topical ketoprofen over topical placebo in chronic pain. Serious adverse events were rare (very low-quality evidence).GRADE assessments of moderate or low quality in some of the reviews were considered by us to be very low because of small numbers of participants and events. AUTHORS' CONCLUSIONS: There is good evidence that some formulations of topical diclofenac and ketoprofen are useful in acute pain conditions such as sprains or strains, with low (good) NNT values. There is a strong message that the exact formulation used is critically important in acute conditions, and that might also apply to other pain conditions. In chronic musculoskeletal conditions with assessments over 6 to 12 weeks, topical diclofenac and ketoprofen had limited efficacy in hand and knee osteoarthritis, as did topical high-concentration capsaicin in postherpetic neuralgia. Though NNTs were higher, this still indicates that a small proportion of people had good pain relief.Use of GRADE in Cochrane Reviews with small numbers of participants and events requires attention.
[Mh] Termos MeSH primário: Dor Aguda/tratamento farmacológico
Analgésicos/uso terapêutico
Dor Crônica/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Artrite Reumatoide/tratamento farmacológico
Capsaicina/uso terapêutico
Diclofenaco/uso terapêutico
Seres Humanos
Cetoprofeno
Dor Musculoesquelética/tratamento farmacológico
Neuralgia/tratamento farmacológico
Números Necessários para Tratar
Osteoartrite/tratamento farmacológico
Piroxicam/uso terapêutico
Viés de Publicação
Literatura de Revisão como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Analgesics); 13T4O6VMAM (Piroxicam); 144O8QL0L1 (Diclofenac); 90Y4QC304K (Ketoprofen); S07O44R1ZM (Capsaicin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170803
[Lr] Data última revisão:
170803
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170513
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD008609.pub2


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[PMID]:28411076
[Au] Autor:Goswami S; Sanyal S; Chakraborty P; Das C; Sarkar M
[Ad] Endereço:Chemical Sciences Division, Saha Institute of Nuclear Physics, 1/AF Bidhannagar, Kolkata 700064, India.
[Ti] Título:Interaction of a common painkiller piroxicam and copper-piroxicam with chromatin causes structural alterations accompanied by modulation at the epigenomic/genomic level.
[So] Source:Biochim Biophys Acta;1861(8):2048-2059, 2017 08.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: NSAIDs are the most common class of painkillers and anti-inflammatory agents. They also show other functions like chemoprevention and chemosuppression for which they act at the protein but not at the genome level since they are mostly anions at physiological pH, which prohibit their approach to the poly-anionic DNA. Complexing the drugs with bioactive metal obliterate their negative charge and allow them to bind to the DNA, thereby, opening the possibility of genome level interaction. To test this hypothesis, we present the interaction of a traditional NSAID, Piroxicam and its copper complex with core histone and chromatin. METHODS: Spectroscopy, DLS, and SEM studies were applied to see the effect of the interaction on the structure of histone/chromatin. This was coupled with MTT assay, immunoblot analysis, confocal microscopy, micro array analysis and qRT-PCR. RESULTS: The interaction of Piroxicam and its copper complex with histone/chromatin results in structural alterations. Such structural alterations can have different biological manifestations, but to test our hypothesis, we have focused only on the accompanied modulations at the epigenomic/genomic level. The complex, showed alteration of key epigenetic signatures implicated in transcription in the global context, although Piroxicam caused no significant changes. We have correlated such alterations caused by the complex with the changes in global gene expression and validated the candidate gene expression alterations. CONCLUSION AND GENERAL SIGNIFICANCE: Our results provide the proof of concept that DNA binding ability of the copper complexes of a traditional NSAID, opens up the possibility of modulations at the epigenomic/genomic level.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/química
Cromatina/química
Cobre/química
Epigenômica
Piroxicam/química
[Mh] Termos MeSH secundário: Cobre/metabolismo
DNA/metabolismo
Células HeLa
Histonas/química
Seres Humanos
Piroxicam/metabolismo
Espectrometria de Fluorescência
Transcriptoma
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Chromatin); 0 (Histones); 13T4O6VMAM (Piroxicam); 789U1901C5 (Copper); 9007-49-2 (DNA)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171026
[Lr] Data última revisão:
171026
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170416
[St] Status:MEDLINE


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[PMID]:28373436
[Au] Autor:Silva J; Arantes-Rodrigues R; Pinto-Leite R; Faustino-Rocha AI; Fidalgo-Gonçalves L; Santos L; Oliveira PA
[Ad] Endereço:Department of Veterinary Sciences, Hospital Center of Trás-os-Montes and Alto Douro, Vila Real, Portugal.
[Ti] Título:Synergistic Effect of Carboplatin and Piroxicam on Two Bladder Cancer Cell Lines.
[So] Source:Anticancer Res;37(4):1737-1745, 2017 04.
[Is] ISSN:1791-7530
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIM: This study aimed to evaluate the in vitro efficacy of carboplatin and piroxicam, both in isolation and combined, against T24 and 5637 human urinary bladder cancer cell lines. MATERIALS AND METHODS: Cell viability, drug interaction, cell morphology, cell proliferation, apoptosis and autophagy were analyzed after 72 h of drug exposure. Statistical analysis was performed and values of p<0.05 were considered statistically significant. RESULTS: Drug exposure in combination led to a significant reduction of cell viability comparatively to single-drug exposure. These combinations resulted in a synergistic interaction in the T24 (combination index for 50% effect (CI )=0.65) and 5637 (CI =0.17) cell lines. Notable increase of morphological alterations, a marked decrease of Ki-67 expression, a considerable enhancement of autophagic vacuoles and a minimal effect on apoptosis was observed in both cell lines treated with combined drugs. CONCLUSION: Data showed that in vitro combination of carboplatin and piroxicam produced a more potent antiproliferative effect when compared to single drugs.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Carboplatina/farmacologia
Sinergismo Farmacológico
Piroxicam/farmacologia
Neoplasias da Bexiga Urinária/patologia
[Mh] Termos MeSH secundário: Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Quimioterapia Combinada
Seres Humanos
Células Tumorais Cultivadas
Neoplasias da Bexiga Urinária/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents); 13T4O6VMAM (Piroxicam); BG3F62OND5 (Carboplatin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170413
[Lr] Data última revisão:
170413
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170405
[St] Status:MEDLINE


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[PMID]:28283079
[Au] Autor:Yoshitake R; Saeki K; Watanabe M; Nakaoka N; Ong SM; Hanafusa M; Choisunirachon N; Fujita N; Nishimura R; Nakagawa T
[Ad] Endereço:Laboratory of Veterinary Surgery, Graduate School of Agricultural and Life Sciences, University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan.
[Ti] Título:Molecular investigation of the direct anti-tumour effects of nonsteroidal anti-inflammatory drugs in a panel of canine cancer cell lines.
[So] Source:Vet J;221:38-47, 2017 Mar.
[Is] ISSN:1532-2971
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nonsteroidal anti-inflammatory drugs (NSAIDs) have been suggested as effective adjunctive anti-tumour agents in human and veterinary medicine. However, the molecular mechanisms associated with their anti-tumour effects and correlations with the expression of cyclooxygenase (COX) and related molecules in tumours remain controversial. The objective of this study was to compare the expression profiles of COX and related molecules with NSAID sensitivity and to explore the molecular mechanisms of anti-tumour effects. The expression profiles of COXs, prostaglandins (PGs), PGD synthases, and PGE synthases were obtained, and their correlations with in vitro sensitivity to the NSAIDs piroxicam, carprofen, and robenacoxib were examined, using 26 canine cancer cell lines. Subsequently, microarray analysis was performed using one melanoma cell line to gain insight into mechanisms by which NSAIDs could exert cytotoxic effects. No strong correlation was observed between the cellular expression of COX and related molecules and sensitivity to NSAID treatment. Additionally, NSAIDs inhibited cell growth only at considerably higher concentrations than those required for functional COX inhibition. Microarray data demonstrated that five genes (SLC16A6, PER2, SLC9A8, HTR2B, and BRAF) were significantly upregulated and that four genes (LOC488305, H2AFJ, LOC476445, and ANKRD43) were significantly downregulated by NSAID exposure to the melanoma cell line. These results suggest that the direct in vitro anti-tumour effects of NSAIDs might be mediated by COX/PG-independent pathways. Novel candidate genes that could potentially be involved in the anti-tumour effects of NSAIDs were identified. Further validation and elucidation of their associated mechanisms will contribute to patient selection in clinical settings and the development of effective combination therapies.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/uso terapêutico
Antineoplásicos/uso terapêutico
Doenças do Cão/tratamento farmacológico
Neoplasias/veterinária
[Mh] Termos MeSH secundário: Animais
Carbazóis/uso terapêutico
Linhagem Celular Tumoral
Inibidores de Ciclo-Oxigenase/uso terapêutico
Dinoprostona/metabolismo
Difenilamina/análogos & derivados
Difenilamina/uso terapêutico
Cães
Relação Dose-Resposta a Droga
Perfilação da Expressão Gênica/veterinária
Neoplasias/tratamento farmacológico
Fenilacetatos/uso terapêutico
Piroxicam/uso terapêutico
Prostaglandina D2/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents); 0 (Carbazoles); 0 (Cyclooxygenase Inhibitors); 0 (Phenylacetates); 13T4O6VMAM (Piroxicam); 9N3CBB0BIQ (Diphenylamine); FFL0D546HO (carprofen); K7Q1JQR04M (Dinoprostone); RXY07S6CZ2 (Prostaglandin D2); Z588009C7C (robenacoxib)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170312
[St] Status:MEDLINE


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[PMID]:28235624
[Au] Autor:Shamma RN; Elkasabgy NA; Mahmoud AA; Gawdat SI; Kataia MM; Abdel Hamid MA
[Ad] Endereço:Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, Egypt.
[Ti] Título:Design of novel injectable in-situ forming scaffolds for non-surgical treatment of periapical lesions: In-vitro and in-vivo evaluation.
[So] Source:Int J Pharm;521(1-2):306-317, 2017 Apr 15.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Periapical lesions are considered one of the common pathological conditions affecting alveolar bone. The primary focus of this study was to investigate the effectiveness of formulating an injectable in-situ forming scaffold-loaded with risedronate (bone resorption inhibitor) and with lornoxicam (anti-inflammatory drug) for the non-surgical treatment of periapical lesions. The scaffolds were prepared using solvent-induced phase inversion technique. Two insoluble copolymers were investigated namely; PLGA (ester-terminal) and PLGA-A (acid-terminal), additionally, SAIB was added as a high viscosity water-insoluble carrier. The addition of porogenic agents like hydrolyzed collagen was also investigated. The prepared scaffolds were characterized by analyzing their in-vitro release, DSC and rheological properties, besides their morphological properties. The results showed that the scaffolds prepared using 30% (w/v) PLGA or combined PLGA: SAIB (1:1, w/w) with total polymer concentration of 30% (w/v) possessed the most sustained drug release profile. Selected scaffolds were tested for their therapeutic effect to study the effect of porogenic agent, anti-inflammatory drug and risedronate in periapical lesions induced in dogs' teeth. Results declared that the selected scaffolds succeeded in improving the inflammation and enhancing the formation of new bony regions confirming the success of the prepared scaffolds as an innovative approach in the treatment of bone defects.
[Mh] Termos MeSH primário: Doenças Periapicais/tratamento farmacológico
Piroxicam/análogos & derivados
Risedronato Sódico/administração & dosagem
Tecidos Suporte/química
[Mh] Termos MeSH secundário: Animais
Varredura Diferencial de Calorimetria
Química Farmacêutica
Cães
Injeções
Ácido Láctico/química
Masculino
Piroxicam/administração & dosagem
Piroxicam/química
Ácido Poliglicólico/química
Risedronato Sódico/química
Solubilidade
Sacarose/análogos & derivados
Sacarose/química
Viscosidade
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (polylactic acid-polyglycolic acid copolymer); 13T4O6VMAM (Piroxicam); 26009-03-0 (Polyglycolic Acid); 33X04XA5AT (Lactic Acid); 57-50-1 (Sucrose); ER09126G7A (lornoxicam); H5KI1C3YTV (sucrose acetate isobutyrate); OFG5EXG60L (Risedronate Sodium)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170226
[St] Status:MEDLINE


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[PMID]:28195483
[Au] Autor:Palo M; Kogermann K; Laidmäe I; Meos A; Preis M; Heinämäki J; Sandler N
[Ad] Endereço:Institute of Pharmacy, Faculty of Medicine, University of Tartu , Nooruse 1, EE-50411 Tartu, Estonia.
[Ti] Título:Development of Oromucosal Dosage Forms by Combining Electrospinning and Inkjet Printing.
[So] Source:Mol Pharm;14(3):808-820, 2017 Mar 06.
[Is] ISSN:1543-8392
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Printing technology has been shown to enable flexible fabrication of solid dosage forms for personalized drug therapy. Several methods can be applied for tailoring the properties of the printed pharmaceuticals. In this study, the use of electrospun fibrous substrates in the fabrication of inkjet-printed dosage forms was investigated. A single-drug formulation with lidocaine hydrochloride (LH) and a combination drug system containing LH and piroxicam (PRX) for oromucosal administration were prepared. The LH was deposited on the electrospun and cross-linked gelatin substrates by inkjet printing, whereas PRX was incorporated within the substrate fibers during electrospinning. The solid state analysis of the electrospun substrates showed that PRX was in an amorphous state within the fibers. Furthermore, the results indicated the entrapment and solidification of the dissolved LH within the fibrous gelatin matrix. The printed drug amount (2-3 mg) was in good correlation with the theoretical dose calculated based on the printing parameters. However, a noticeable degradation of the printed LH was detected after a few months. An immediate release (over 85% drug release after 8 min) of both drugs from the printed dosage forms was observed. In conclusion, the prepared electrospun gelatin scaffolds were shown to be suitable substrates for inkjet printing of oromucosal formulations. The combination of electrospinning and inkjet printing allowed the preparation of a dual drug system.
[Mh] Termos MeSH primário: Mucosa Bucal/metabolismo
Piroxicam/química
[Mh] Termos MeSH secundário: Administração Oral
Química Farmacêutica/métodos
Formas de Dosagem
Sistemas de Liberação de Medicamentos/métodos
Liberação Controlada de Fármacos
Gelatina/química
Lidocaína/química
Impressão/métodos
Propriedades de Superfície
Tecnologia Farmacêutica/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dosage Forms); 13T4O6VMAM (Piroxicam); 9000-70-8 (Gelatin); 98PI200987 (Lidocaine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170215
[St] Status:MEDLINE
[do] DOI:10.1021/acs.molpharmaceut.6b01054


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[PMID]:28160506
[Au] Autor:Kumbasar S; Gül Ö; Sik A
[Ad] Endereço:Department of Obstetrics and Gynecology, Sakarya Research and Education Hospital, Sakarya, Turkey.
[Ti] Título:Evaluation of the effect of indomethacin and piroxicam administration before embryo transfer on pregnancy rate.
[So] Source:J Obstet Gynaecol Res;43(3):536-542, 2017 Mar.
[Is] ISSN:1447-0756
[Cp] País de publicação:Australia
[La] Idioma:eng
[Ab] Resumo:AIM: The aim of this study was to evaluate the effect of non-steroidal anti-inflammatory drug (NSAID) administration before embryo transfer (ET) on pregnancy rates in women undergoing in vitro fertilization/intracytoplasmic sperm injection ET. METHODS: Our study included 255 patients diagnosed with primary or secondary infertility caused by a male or tubal-related factor, endometriosis or unexplained factors. The patients were divided randomly into three groups. Two groups were administered oral piroxicam (10 mg capsules) or 100 mg indomethacin (rectal suppository), respectively, 1-2 h before ET. As a control, the third group did not receive any form of treatment before ET. Basal levels of follicle-stimulating hormone, luteinizing hormone, and level 17ß-estradiol on the day of human chorionic gonadotropin administration, the collected and transferred number of embryos, and the number of grade A embryos obtained were determined in all patients. RESULTS: The implantation, clinical pregnancy, and miscarriage rates of the groups were compared. The clinical pregnancy rate per ET and the implantation rate were 35.2% and 12.15% in the piroxicam group, 31.7% and 10.9% in the indomethacin group, and 32.9% and 12.5% in the control, respectively. The miscarriage rates of groups 1, 2 and 3 were 12%, 11.7% and 11.7%, respectively (P = 0.964). The differences in clinical pregnancy rates among the groups were not statistically significant (P = 0.887). There were also no significant differences in the implantation rates (P = 0.842). CONCLUSION: These results suggest that NSAID administration before ET has no additional effect on pregnancy outcome in patients undergoing in vitro fertilization.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/administração & dosagem
Transferência Embrionária/métodos
Indometacina/administração & dosagem
Infertilidade Feminina/terapia
Piroxicam/administração & dosagem
Taxa de Gravidez
[Mh] Termos MeSH secundário: Adulto
Implantação do Embrião/efeitos dos fármacos
Feminino
Fertilização In Vitro
Seres Humanos
Gravidez
Resultado da Gravidez
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 13T4O6VMAM (Piroxicam); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170205
[St] Status:MEDLINE
[do] DOI:10.1111/jog.13244


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[PMID]:28117757
[Au] Autor:Bernal-Chávez SA; Pérez-Carreto LY; Nava-Arzaluz MG; Ganem-Rondero A
[Ad] Endereço:Division de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de Mexico, Cuautitlán Izcalli 54740, Estado de Mexico, Mexico. q901108@hotmail.com.
[Ti] Título:Alkylglycerol Derivatives, a New Class of Skin Penetration Modulators.
[So] Source:Molecules;22(1), 2017 Jan 22.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The absorption modulating activity of two alkylglycerol derivatives (batyl and chimyl alcohol) on skin barrier properties was evaluated. Biophysical tests such as transepidermal water loss (TEWL) and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, as well as in vitro skin permeation studies, were performed in order to determine the effect of these compounds as chemical absorption modulators. Four drugs were used as models: three NSAIDS (diclofenac, naproxen, and piroxicam) and glycyrrhizic acid. The results showed that treatment of the skin with alkylglycerols caused (i) a reduction on the amount of drug permeated; (ii) a reduction in TEWL; and (iii) changes in the ATR-FTIR peaks of stratum corneum lipids, indicative of a more ordered structure. All of these findings confirm that alkyl glycerols have an absorption retarding effect on the drugs tested. Such effects are expected to give rise to important applications in the pharmaceutical and cosmetic sectors, in cases where it is desirable for the drug to remain in the superficial layers of the skin to achieve a local effect.
[Mh] Termos MeSH primário: Portadores de Fármacos/farmacologia
Éteres de Glicerila/farmacologia
Permeabilidade/efeitos dos fármacos
Absorção Cutânea/efeitos dos fármacos
Pele/metabolismo
[Mh] Termos MeSH secundário: Administração Cutânea
Animais
Diclofenaco/administração & dosagem
Diclofenaco/metabolismo
Ácido Glicirrízico/administração & dosagem
Ácido Glicirrízico/metabolismo
Naproxeno/administração & dosagem
Naproxeno/metabolismo
Piroxicam/administração & dosagem
Piroxicam/metabolismo
Pele/efeitos dos fármacos
Espectroscopia de Infravermelho com Transformada de Fourier
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Glyceryl Ethers); 13T4O6VMAM (Piroxicam); 144O8QL0L1 (Diclofenac); 39YR661C4U (batyl alcohol); 57Y76R9ATQ (Naproxen); 6FO62043WK (Glycyrrhizic Acid); UJ10V6YY6H (chimyl alcohol)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170523
[Lr] Data última revisão:
170523
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170125
[St] Status:MEDLINE



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