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1.
Pharm Dev Technol ; 26(4): 431-443, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33567946

RESUMO

This study aimed to present an effective formulation targeting oral ulcers that will remain in the application site for a longer period, reducing the frequency of administration. As a candidate formulation, usnic acid (UA) was loaded into the optimum nanogels. The characterization studies included physical, rheological, and bioadhesive properties as well as in vitro release and ex vivo studies. The rheological results revealed that the nanogels present pseudoplastic flow behavior. In vitro drug release showed a prolonged pattern. In further, the chosen UA nanogels showed very low percentages of penetration and permeation. F13, which showed the highest release, suitable bioadhesive properties (0.475 ± 0.033 N/cm2) and eligible particle size (250.22 ± 4.11 nm), PDI (0.089 ± 0.052), and zeta potential (20.56 ± 0.330 mV) values were chosen for in vivo experiments. The selected UA nanogels showed effective antimicrobial activity against Bacillus Cereus and great in vivo wound healing properties. The results indicated that suitable UA nanogels with desired properties could be prepared. The therapeutic potential of the nanogels for oral ulcers was assessed using an animal model and the histopathological findings suggested that the optimized formulation is a good choice for oral ulcer treatment. Nonetheless, further research is recommended to support its efficacy by applying pharmacodynamic and pharmacokinetic studies in human individuals.


Assuntos
Benzofuranos/administração & dosagem , Nanogéis , Úlceras Orais/tratamento farmacológico , Cicatrização/efeitos dos fármacos , Adesividade , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/farmacologia , Bacillus cereus/efeitos dos fármacos , Benzofuranos/farmacologia , Preparações de Ação Retardada , Modelos Animais de Doenças , Liberação Controlada de Fármacos , Masculino , Úlceras Orais/patologia , Tamanho da Partícula , Coelhos , Reologia
2.
Pharm Dev Technol ; 25(10): 1238-1248, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32787718

RESUMO

The objective of the present research was to examine the possible usage of terbinafine loaded hydrogels for vaginal application as part of vaginal candidiasis treatment. Vaginal candidiasis belongs to the most frequent gynecological disorders. Various antifungal drugs are used for its treatment, with Terbinafine being one of them. In this study, new gel formulations were prepared for Terbinafine vaginal delivery. Natural polymers such as chitosan, sodium carboxymethylcellulose, and Carbopol were used for the development of Terbinafine vaginal gels. The developed gels were examined for their viscosity and spreadability, pH and mechanical properties. The most optimal formulations were further evaluated for their in vitro release behavior and antifungal activities. In further, the cytotoxicity and irritation inducing capacity of optimum gel formulations were evaluated. In vitro drug release studies demonstrated that terbinafine release was prolonged whereas anti-candida activity in several species showed the superiority of the gels compared to the marketed product. G-5 and G-8 gels did not cause lysis, hemorrhage and coagulation, therefore, classified as non-irritant. The optimal formulations were also studied for their stability, demonstrating that they were stable for 3 months.


Assuntos
Antifúngicos/administração & dosagem , Candidíase Vulvovaginal/tratamento farmacológico , Portadores de Fármacos/química , Terbinafina/administração & dosagem , Administração Intravaginal , Animais , Antifúngicos/farmacologia , Antifúngicos/toxicidade , Candidíase Vulvovaginal/microbiologia , Galinhas , Membrana Corioalantoide/efeitos dos fármacos , Liberação Controlada de Fármacos , Feminino , Hidrogéis , Concentração de Íons de Hidrogênio , Técnicas In Vitro , Polímeros/química , Terbinafina/farmacologia , Terbinafina/toxicidade , Testes de Toxicidade , Cremes, Espumas e Géis Vaginais , Viscosidade
3.
Saudi Pharm J ; 28(3): 338-348, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32194336

RESUMO

The objective of the present research was to examine the possible usage of microemulsion based gel for fusidic acid (FA) dermal application as burn wound treatment. During the preparation of microemulsion, ethyl oleate as oil phase, tween 80 as a surfactant, ethanol as co-surfactant, water as aqueous phase were used. The prepared microemulsions were evaluated for clarity, pH, viscosity and FA content. Moreover, stability, sterility, antibacterial activity, in vitro release of the formulations were also evaluated. The results showed that the FA loaded microemulsion and microemulsion based gel formation and characteristics were related to many parameters of the components. The performed optimized microemulsion-based gel showed good stability over a period of 3 months. The antibacterial activity of microemulsion-based gel was found to be comparable with marketed cream. RAW 264.7 macrophages were used to determine cell viability (MTT assay) and nitric oxide production. MBG and FA-MBG significantly inhibit the production of the inflammatory mediator NO in LPS-stimulated RAW 264.7 cells in a concentration-dependent manner. The wound healing property was evaluated by histopathological examination and by measuring the wound contraction. The % of wound area in rats treated with FA (2%) loaded microemulsion based gel ranged from 69.30% to 41.39% in the period from 3 to 10 days. In conclusion, FA loaded microemulsion based gel could be offered as encouraging strategy as dermal systems for the burn wound treatment.

4.
Saudi Pharm J ; 27(5): 738-752, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31297030

RESUMO

In this study, novel adhesive films were prepared for Mupirocin dermal delivery. Natural polymers as chitosan, sodium alginate and carbopol were used for films development to evaluate possible interactions and drug release properties. Solvent evaporation method was used for films preparation. Preliminary studies involved FT-IR spectroscopy and Scanning Electron Microscopy to specify interactions and morphology. Thickness, tensile strength and water uptake in phosphate buffer saline were evaluated whereas in vitro release studies were also performed. In vitro drug release studies demonstrated that mupirocin release was improved. Ex vivo bioadhesion and permeation studies using Balb-c mice were performed to check the suitability of the films. Antimicrobial ability was evaluated by agar well diffusion tests. Finally, excisional wound model applied to test the wound healing effect and evaluated macroscopic and histopathologically. One formulation was found more effective compared to the market product for wound healing at Balb-c mice.

5.
J Pharm Pharmacol ; 70(10): 1401-1413, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29984824

RESUMO

OBJECTIVES: The objective of this study was to investigate the wound healing activity of Capparis ovata var. palaestina fruit extract in mice. For this aim, wound healing, in vitro antimicrobial and antioxidant activities, HPLC, phenolic and flavonoid compounds analyses were performed. METHODS: The wound healing effect was tested by excisional wound model. Wound closure was measured for 14 days and at 14th day wound healing was assessed by levels of TGF-ß, VEGF, COL1A1 and angiogenesis, granulation tissue thickness, epidermal and dermal regeneration. The antioxidant activity was calculated by DPPH and ABTS free radical scavenging assays. Antimicrobial ability was evaluated by minimum inhibitory concentration and agar well diffusion tests. KEY FINDINGS: The extract indicated significant antioxidant activity while it also exhibited antimicrobial activity. Rutin was found in the extract according to HPLC study. Moreover, the extract was found to have rich phenolic and flavonoid contents. Histological evaluation showed that extract group induced significant (P < 0.001) wound healing activity compared to control group. Furthermore, extract group increased wound healing rates by promoting granulation tissue, epidermal regeneration, angiogenesis, collagen, TGF-ß and VEGF. CONCLUSIONS: The results clarified that the extract possesses antioxidant, antimicrobial activity and thus could provide a valuable contribution to the wound healing.


Assuntos
Capparis/química , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Indutores da Angiogênese/farmacologia , Animais , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Colágeno Tipo I/metabolismo , Cadeia alfa 1 do Colágeno Tipo I , Frutas/química , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Pele/efeitos dos fármacos , Pele/metabolismo , Fator de Crescimento Transformador beta/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo
6.
Artigo em Inglês | MEDLINE | ID: mdl-29595118

RESUMO

BACKGROUND AND OBJECTIVE: This paper is focused on evaluating the various biological activities of C. ovata var. palaestina extracts which could beneficially influence diabetes and its complications. METHODS: Alloxan-induced diabetic BALB-c mice were administered intraperitoneally with 100, 300, 500mg/kg doses of ethanol and aqueous extracts of buds and fruits. Furthermore, HPLC, phenolic and flavonoid compounds analysis, ABTS and DPPH free radical scavenging activity, anti-inflammatory activity, agar well diffusion and MIC tests were carried out. RESULTS: Fruit-aqueous; 100mg/kg, 300mg/kg and bud-aqueous; 500mg/kg extracts showed significant hypoglycemic activity. All extracts indicated important antioxidant activity, however, bud-aqueous extract demonstrated the most potent activity. HPLC study exhibited that rutin is found in high amounts in bud-aqueous and bud-ethanol extracts. Furthermore, the bud-aqueous extract depicted stronger and broader antimicrobial activity than other extracts. Fruit-ethanol and bud-ethanol extracts denoted the most potent anti-inflammatory effect even though this effect was significantly shown by all extracts. Finally, high levels of phenolic and flavonoid content were involved in all extracts, but the highest levels were found in fruit-ethanol and bud-ethanol extracts. CONCLUSION: The results showed that extracts which indicated hypoglycemic, antioxidant, antiinflammatory, antimicrobial activities may provide a valuable contribution to the management of diabetes and its complications.


Assuntos
Glicemia/efeitos dos fármacos , Capparis , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Rutina/farmacologia , Aloxano , Animais , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Biomarcadores/sangue , Glicemia/metabolismo , Capparis/química , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Frutas , Hipoglicemiantes/isolamento & purificação , Camundongos Endogâmicos BALB C , Extratos Vegetais/isolamento & purificação , Rutina/isolamento & purificação
7.
Environ Monit Assess ; 189(7): 362, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28667414

RESUMO

Pathogenic and/or opportunistic fungal species are major causes of nosocomial infections, especially in controlled environments where immunocompromised patients are hospitalized. Indoor fungal contamination in hospital air is associated with a wide range of adverse health effects. Regular determination of fungal spore counts in controlled hospital environments may help reduce the risk of fungal infections. Because infants have inchoate immune systems, they are given immunocompromised patient status. The aim of the present study was to evaluate culturable airborne fungi in the air of hospital newborn units in the Thrace, Marmara, Aegean, and Central Anatolia regions of Turkey. A total of 108 air samples were collected seasonally from newborn units in July 2012, October 2012, January 2013, and April 2013 by using an air sampler and dichloran 18% glycerol agar (DG18) as isolation media. We obtained 2593 fungal colonies comprising 370 fungal isolates representing 109 species of 28 genera, which were identified through multi-loci gene sequencing. Penicillium, Aspergillus, Cladosporium, Talaromyces, and Alternaria were the most abundant genera identified (35.14, 25.40, 17.57, 2.70, and 6.22% of the total, respectively).


Assuntos
Microbiologia do Ar , Poluição do Ar em Ambientes Fechados/estatística & dados numéricos , Monitoramento Ambiental , Berçários Hospitalares/estatística & dados numéricos , Esporos Fúngicos , Compostos de Anilina , Animais , Infecção Hospitalar , Fungos , Hospitais , Humanos , Lactente , Recém-Nascido , Penicillium , Turquia
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