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1.
Hosp Pharm ; 59(2): 234-240, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38450352

RESUMEN

The DECAF score (the Dyspnea, Eosinopenia, Consolidation, Academia, and Atrial fibrillation score) has been adopted in some hospitals to predict the severity of Acute Exacerbation of Chronic Obstructive Pulmonary Disease (AECOPD). However, DECAF score has not been widely evaluated or used in Middle Eastern countries. The present study aimed to validate the DECAF score for predicting in-hospital mortality in patients with AECOPD in the United Arab Emirates (UAE). This was a retrospective, observational study conducted in 19 hospitals in the UAE. Data were retrieved from the electronic records of patients admitted for AECOPD in 17 hospitals across the country. Patients aged more than 35 years who were diagnosed with AECOPD were included in the study. The validation of the DECAF Score for inpatient death, 30-days death, and 90-day readmission was conducted using the Area Under the Receiver Operator curve (AUROC). The AUROCDECAF curves for inpatient death, 30-days death, and 90-day readmission were 0.8 (95% CI: 0.8-0.9), 0.8 (95% CI: 0.7-0.8), and 0.8 (95% CI: 0.8-0.8), respectively. The model was a satisfactory fit to the data (Hosmer-Lemeshow statistic = 0.195, Nagelkerke R2 = 31.7%). There were significant differences in means of length of stay across patients with different DECAF score (P = .008). Patients with a DECAF score of 6 had the highest mean length of stay, which was 29.8 ± 31.4 days. Patients with a DECAF score of 0 had the lowest mean length of stay, which was 3.6 ± 2.0 days. The DECAF score is a strong predictive tool for inpatient death, 30 days mortality and 90-day readmission in UAE hospital settings. The DECAF score is an effective tool for predicating mortality and other disease outcomes in patients with AECOPD in the UAE; hence, clinicians would be more empowered to make appropriate clinical decisions by using the DECAF score.

2.
Saudi Pharm J ; 31(8): 101689, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37457370

RESUMEN

The antihyperglycemic effect of Plicosepalus acaciae (P. acaciae) extract was proven, but it still needs to be formulated into a suitable dosage form. We aimed at preparing an oral stabilized SLNs for P. acaciae with high payload, to be used as powder for reconstitution, filled into capsule or compressed into tablet. SLNs were prepared by emulsion solvent evaporation technique. Preliminary characterization was performed followed by full assessment of the optimized SLNs suspension and/or its lyophilized form: particle size, zeta potential, surface morphology, percentage entrapment efficiency (% EE), DSC, FTIR and in vitro release studies. The optimized SLNs lyophilized formula (F3L) exhibited acceptable compressibility and flowability. The reconstituted F3L showed % sedimentation volume of 91.83 %, re-dispersibility of 95%, viscosity of 764.33 cp, uniform particle size of 30.28 nm as shown by TEM, polydispersity index (PDI) of 0.16, zeta potential of -36.4 mV, % EE of 89.64 % and drug content of 97.69 %. The physical mixture and F3L FTIR spectrum indicated compatibility of components. In vitro release study showed a burst release in lyophilized formulations followed by slow-release, calculated as total phenolic content. Our previously reported work revealed that the total extracts of P. acaciae and SLNs formulations with the greatest lipid content F3s, demonstrated a considerable blood glucose-lowering effect in diabetic rats. The obtained lyophilized SLNs is promising for preparation of a suitable stable dosage form for P. acaciae extract to be used in treatment of diabetes.

3.
Acta Odontol Scand ; 76(3): 212-219, 2018 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-29145771

RESUMEN

OBJECTIVE: Autogenous soft-tissue grafting is a commonly used procedure nowadays in dentistry. However, the prolonged healing time needed for the donor site leads to increase the patient's pain and discomfort. Statin has been observed to be beneficial in reducing bacterial burden, improving epithelization and wound healing. The aim of this study was to evaluate intra-oral topical application of simvastatin/chitosan gel (10 mg/mL) over the palatal donor site following free gingival graft (FGG) procedure. MATERIAL AND METHODS: Subjects indicated for FGG procedure were divided into four groups. Group I: Simvastatin suspension (S), group II: simvastatin/chitosan gel (SC), group III: chitosan gel (C), group IV: petroleum gel (P). Treatment was applied three times/day for the following 7 days. Wound healing was evaluated at day 3, 7 and 14 post-surgery. A visual analogue scale (VAS) was used to measure the experienced discomfort at 1, 3, 5, 7 and 14 days. RESULTS: Statistical significant reduction in wound-healing scores was observed after 3 and 7 days for group II compared to other groups (p = .015). A significant reduction was also observed in VAS score for group II compared to other groups at day 1, 3, 5 and 7. CONCLUSION: Topical application of S/C gel could be used as a novel therapeutic modality that improved healing and reduced pain in the palatal donor site following FGG procedure.


Asunto(s)
Geles/administración & dosificación , Encía/trasplante , Simvastatina/administración & dosificación , Administración Tópica , Adulto , Femenino , Encía/efectos de los fármacos , Humanos , Masculino , Procedimientos Quirúrgicos Orales/métodos , Dimensión del Dolor/métodos , Hueso Paladar/cirugía , Cicatrización de Heridas
4.
Drug Dev Ind Pharm ; 43(1): 120-131, 2017 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-27589817

RESUMEN

INTRODUCTION: Periodontal disease broadly defines group of conditions in which the supportive structure of the tooth (periodontium) is destroyed. Recent studies suggested that the anti-diabetic drug metformin hydrochloride (MF) has an osteogenic effect and is beneficial for the management of periodontitis. OBJECTIVE: Development of strong mucoadhesive multiple layer film loading small dose of MF for intra-pocket application. METHODOLOGY: Multiple layer film was developed by double casting followed by compression method. Either 6% carboxy methyl cellulose sodium (CMC) or sodium alginate (ALG) constituted the inner drug (0.6%) loaded layer. Thiolated sodium alginate (TSA; 2 or 4%) constituted the outer drug free layers to enhance mucoadhesion and achieve controlled drug release. Optimized formulation was assessed clinically on 20 subjects. RESULTS: Films were uniform, thin and hard enough for easy insertion into periodontal pockets. Based on water uptake and in vitro drug release, CMC based film with 4% TSA as an outer layer was the optimized formulation with enhanced mucoadhesion and controlled drug release (83.73% over 12 h). SEM showed the effective fabrication of the triple layer film in which connective lines between the layers could be observed. FTIR examination suggests possibility of hydrogen bonding between the -NH groups of metformin and -OH groups of CMC. DSC revealed the presence of MF mainly in the amorphous form. Clinical results indicated improvement of all clinical parameters six months post treatment. CONCLUSION: The results suggested that local application of the mucoadhesive multiple layer films loaded with metformin hydrochloride was able to manage moderate chronic periodontitis.


Asunto(s)
Alginatos/administración & dosificación , Cementos Dentales , Sistemas de Liberación de Medicamentos/métodos , Metformina/administración & dosificación , Bolsa Periodontal/tratamiento farmacológico , Compuestos de Sulfhidrilo/administración & dosificación , Adulto , Alginatos/química , Animales , Preparaciones de Acción Retardada/química , Cementos Dentales/química , Femenino , Ácido Glucurónico/administración & dosificación , Ácido Glucurónico/química , Ácidos Hexurónicos/administración & dosificación , Ácidos Hexurónicos/química , Humanos , Masculino , Metformina/química , Persona de Mediana Edad , Bolsa Periodontal/diagnóstico , Periodontitis/diagnóstico , Periodontitis/tratamiento farmacológico , Compuestos de Sulfhidrilo/química , Porcinos , Tionucleótidos/administración & dosificación , Tionucleótidos/química
5.
Pharm Dev Technol ; 20(3): 297-305, 2015 May.
Artículo en Inglés | MEDLINE | ID: mdl-24438021

RESUMEN

Local intra-pocket drug delivery devices can provide an effective concentration of the antimicrobial agent at the site of action with avoidance of undesirable side effects. This study explored the application of chitosan-alginate and chitosan-pectin polyelectrolyte complex (PEC) films as drug release regulators for tetracycline HCl (Tc) to treat periodontal pockets. Periodontal films with 1:1 Tc:PEC ratio were prepared using 1:1 chitosan (Ch) to sodium alginate (A) or 1:3 Ch to pectin (P). The scanning electron microscope showed acceptable film appearance and differential scanning calorimetry analysis confirmed complex formation. The in vitro release studies for both films showed a burst drug release, followed by prolonged release for 70 h. A prolonged antibacterial activity of both films against Staphylococcus aureus ATCC 6538 was observed over a period of 21 days. Aging studies indicated that the five months storage period in freezer did not significantly influence the drug release profile or the antibacterial activity of both films. Clinical evaluation showed a significant reduction in pocket depth (p < 0.0001) to their normal values (≤3 mm). PEC films could be exploited as a prolonged drug release devices for treatment of periodontal pockets.


Asunto(s)
Antibacterianos/administración & dosificación , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Tetraciclina/administración & dosificación , Alginatos/química , Antibacterianos/farmacología , Rastreo Diferencial de Calorimetría , Química Farmacéutica/métodos , Quitosano/química , Preparaciones de Acción Retardada , Liberación de Fármacos , Estabilidad de Medicamentos , Almacenaje de Medicamentos , Electrólitos/química , Ácido Glucurónico/química , Ácidos Hexurónicos/química , Humanos , Pectinas/química , Staphylococcus aureus/efectos de los fármacos , Tetraciclina/farmacología , Factores de Tiempo
6.
J Liposome Res ; 24(4): 280-9, 2014 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-24779560

RESUMEN

Mefenamic acid (MA) is a BCS II class NSAID drug. It is available only in the form of tablets, capsules, and pediatric suspensions. Oral administration of MA is associated with severe gastrointestinal side effects. The aim of this study was to develop a convenient and low-cost transdermal drug delivery system for MA using proniosome as a novel carrier without the addition of penetration enhancers. The formulation factors, such as the presence of cholesterol, types of lecithin, and surfactants were investigated for their influence on the entrapment efficiency, rate of hydration, vesicle size, and zeta potential, in vitro drug release and skin permeation in order to optimize the proniosomal formulations with the minimum dose of the drug. Furthermore, the in vivo anti-inflammatory effect was evaluated on a formalin-induced rat paw edema model. The results showed that the type of surfactants had higher impact on the entrapment efficiency than the type of lecithins, with the highest in Span 80 (82.84%). The release of MA from Span 80 proniosomal gel was significantly affected by the type of lecithin used. The addition of cholesterol significantly increased both the drug release and the skin permeation flux of MA. Zeta potential showed a stable A4 noisomal suspension. DSC revealed the molecular dispersion of MA into the loaded proniosomes. In vivo study of the treatment group with MA proniosome gel showed a significant inhibition of rat paw edema compared with the same gel without the drug (control). The results of this study suggest that proniosomes are promising nano vesicular carriers and safe alternatives to enhance the transdermal delivery of MA.


Asunto(s)
Antiinflamatorios no Esteroideos/administración & dosificación , Portadores de Fármacos/administración & dosificación , Edema/tratamiento farmacológico , Ácido Mefenámico/administración & dosificación , Nanopartículas/química , Enfermedades de la Piel/tratamiento farmacológico , Piel/efectos de los fármacos , Administración Cutánea , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/metabolismo , Antiinflamatorios no Esteroideos/uso terapéutico , Fármacos Dermatológicos/administración & dosificación , Fármacos Dermatológicos/química , Fármacos Dermatológicos/metabolismo , Fármacos Dermatológicos/uso terapéutico , Portadores de Fármacos/química , Portadores de Fármacos/metabolismo , Portadores de Fármacos/uso terapéutico , Composición de Medicamentos , Edema/metabolismo , Edema/patología , Geles , Técnicas In Vitro , Liposomas , Masculino , Ácido Mefenámico/química , Ácido Mefenámico/metabolismo , Ácido Mefenámico/uso terapéutico , Ratas Wistar , Piel/metabolismo , Piel/patología , Absorción Cutánea , Enfermedades de la Piel/metabolismo , Enfermedades de la Piel/patología , Solubilidad
7.
AAPS PharmSciTech ; 15(4): 1021-8, 2014 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-24831089

RESUMEN

In situ gelling formulations allow easy application to the target area. Gelation is induced by physiological stimuli at the site of application where the formula attains semisolid properties and exerts sustained drug release. In situ gelling formulations containing either 3% meloxicam (Mx) or 2% minocycline HCl (MH) were prepared for local application into the periodontal pockets. Gel formulations were based on the thermosensitive Pluronic(®) (Pl) and the pH-sensitive Carbopol(®) (C) polymers. C gels were prepared in combination with HPMC (H) to decrease its acidity. The total percent drug released from Pl formulae was 21.72% after 1 week for Mx and 85% after 3 days for MH. Their release kinetics data indicated anomalous non-Fickian behavior that could be controlled by both diffusion and chain relaxation. Addition of MH to C/H gels (1:2.5) resulted in liquefaction, followed by drug precipitation. Regarding C/H gel containing Mx, it showed a prolonged release rate up to 7 days with an initial burst effect; the kinetics data revealed Fickian-diffusion mechanism. The in vitro antibacterial activity studies for MH gel in Pl revealed that the drug released exceeded the minimum inhibitory concentration (MIC) of MH against Staphylococcus aureus ATCC 6538; placebo gel showed no effect on the microorganism. Clinical evaluation of Pl gels containing either Mx or MH showed significant improvement in chronic periodontitis patients, manifested by decrease in pocket depth and gingival index and increase in bone density.


Asunto(s)
Geles/química , Geles/farmacología , Minociclina/química , Minociclina/farmacología , Bolsa Periodontal/tratamiento farmacológico , Tiazinas/química , Tiazinas/farmacología , Tiazoles/química , Tiazoles/farmacología , Adulto , Antibacterianos/química , Antibacterianos/farmacología , Química Farmacéutica/métodos , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacología , Difusión , Liberación de Fármacos , Femenino , Humanos , Cinética , Meloxicam , Polímeros/química , Polímeros/farmacología , Staphylococcus aureus/efectos de los fármacos , Adulto Joven
8.
Saudi Pharm J ; 22(6): 570-9, 2014 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-25561871

RESUMEN

Gastroretentive levofloxacin (LVF) floating mini-tablets for the eradication of Helicobacter pylori (H. pylori) were prepared using the matrix forming polymer hydroxypropyl methylcellulose (HPMC K100M), alone or with Carbopol 940P in different ratios by wet granulation technique. Buoyancy of mini-tablets was achieved by an addition of an effervescent mixture consisting of sodium bicarbonate and anhydrous citric acid to some formulations. The prepared mini-tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy, water uptake and in vitro release. The optimized formula was subjected to further studies: FT-IR, DSC analysis and in vivo examination in healthy volunteers. The prepared mini-tablets exhibited satisfactory physicochemical characteristics. Incorporation of gas-generating agent improved the floating parameters. HPMC K100M mini-tablet formulation (F1) offered the best controlled drug release (>8 h) along with floating lag time <1 s and total floating time >24 h. The obtained DSC thermograms and FT-IR charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. The in vivo test confirmed the success of the optimized formula F1 in being retained in the stomach of the volunteers for more than 4 h. LVF floating mini-tablets based on HPMC K100M is a promising formulation for eradication of H. pylori.

9.
Pharmaceutics ; 14(4)2022 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-35456717

RESUMEN

There has been an increasing demand for the development of nanocarriers targeting multiple diseases with a broad range of properties. Due to their tiny size, giant surface area and feasible targetability, nanocarriers have optimized efficacy, decreased side effects and improved stability over conventional drug dosage forms. There are diverse types of nanocarriers that have been synthesized for drug delivery, including dendrimers, liposomes, solid lipid nanoparticles, polymersomes, polymer-drug conjugates, polymeric nanoparticles, peptide nanoparticles, micelles, nanoemulsions, nanospheres, nanocapsules, nanoshells, carbon nanotubes and gold nanoparticles, etc. Several characterization techniques have been proposed and used over the past few decades to control and predict the behavior of nanocarriers both in vitro and in vivo. In this review, we describe some fundamental in vitro, ex vivo, in situ and in vivo characterization methods for most nanocarriers, emphasizing their advantages and limitations, as well as the safety, regulatory and manufacturing aspects that hinder the transfer of nanocarriers from the laboratory to the clinic. Moreover, integration of artificial intelligence with nanotechnology, as well as the advantages and problems of artificial intelligence in the development and optimization of nanocarriers, are also discussed, along with future perspectives.

10.
World Allergy Organ J ; 15(5): 100647, 2022 May.
Artículo en Inglés | MEDLINE | ID: mdl-35663273

RESUMEN

Background: While crucial to the assessment and improvement of asthma control, insights on treatment practices in patients with severe diseases across Gulf nations are lacking. This observational study describes the treatment patterns of adolescents and adults with severe asthma across four countries of the Gulf region and evaluates current levels of asthma control; quality of life (QoL); exacerbation frequency; and the application of cellular, protein, and respiratory biomarkers in assessing asthma severity and inflammation. Methods: Patients (aged >12 years, body weight ≥40 kg) with clinician-diagnosed, severe asthma (guided by the 2018 Global Initiative for Asthma definition) were included in this cross-sectional, multicenter, observational study conducted in the four Gulf countries of Kuwait, Oman, Qatar, and the United Arab Emirates. Data on demographics, treatment patterns, and laboratory parameters (blood eosinophil count [BEC], levels of serum immunoglobulin E [IgE], and fractional exhaled nitric oxide [FeNO]) were extracted from the medical records of patients during a 12-month retrospective period and transcribed onto case report forms. At the Enrollment visit, patients assessed their asthma control and QoL with the self-administered Asthma Control Questionnaire (ACQ) and a standardized version of the Asthma Quality of Life Questionnaire (AQLQ(S)), respectively. Results: Among the 243 patients analyzed, (mean [standard deviation (SD)] age, 48.4 [13.9] years; female, 67.5%), the inhaled corticosteroid (ICS)/long-acting ß2 agonist (LABA) combination was the most prescribed asthma medication (n = 240; 98.8%). Most patients were classified as "uncontrolled," (n = 173; 71.2%) and the majority (n = 206; 84.8%) experienced ≥1 exacerbation(s) in the preceding 12 months. The mean (SD) ACQ score was 2.1 (1.2), which indicated uncontrolled asthma, and the mean (SD) total AQLQ(S) score was 4.7 (1.4), suggesting "some limitation" in overall QoL. BECs during the 12-month period were elevated in most patients (>300 cells/µL [n = 183; 41.7%], 150-300 cells/µL [n = 138; 31.4%], <150 cells/µL [n = 118; 26.9%]), suggesting an eosinophilic asthma phenotype, although no standardized threshold by which to define eosinophilia has yet been confirmed. This study revealed that the biomarkers BEC, serum IgE, and FeNO concentrations were obtained inconsistently by the participating centers. Conclusions: Despite recommended ICS/LABA therapy being prescribed to most patients for their severe disease, the majority experienced uncontrolled asthma and exhibited elevated BECs. These findings indicate the need for enhanced treatment strategies to improve and sustain asthma control in the Gulf region.

11.
Int Med Case Rep J ; 14: 853-861, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34992473

RESUMEN

A South Asian male patient in his mid-forties presented with symptoms of severe 2019-nCoV (COVID-19) and recent brain infarction. Subsequently, he was found to have evidence of sepsis, underlying undetected diabetes mellitus (DM) and oral candida mucositis, possibly leading to the rare occurrence of direct spread to the lung, manifesting as a necrotizing candida lung abscess. We describe the diagnosis, clinical course, and management of the unique complication in this case that occurred during his admission, hospitalization, and eventual successful discharge from the hospital. This case highlights the importance of early identification and treatment of suspected COVID-19 infection based on clinical and radiological assessments before the confirmation of COVID-19 by real-time polymerase chain reaction (rtPCR) test result, especially in patients with hyperglycemia. It also indicates the complications that can occur due to COVID-19 such as arteriovenous manifestations and the rare occurrence of pulmonary candida lung abscess. Early detection and prompt management by interdisciplinary teams in the emergency room, followed by close monitoring of complications in the intensive care unit (ICU), can lead to successful outcomes in severe/critical COVID-19 infection.

12.
Int J Pharm ; 548(1): 609-624, 2018 Sep 05.
Artículo en Inglés | MEDLINE | ID: mdl-30033394

RESUMEN

This work aimed at designing efficient safe delivery system for intranasal (IN) brain targeting of the water soluble anti- migraine drug Almotriptan malate (ALM). Solid lipid nanoparticles (SLNs) were prepared by w/o/w double emulsion-solvent evaporation method. Selection of the optimized SLNs formula was based on evaluating particle size (PS), poly dispersity index (PDI) and entrapment efficiency (%EE). Optimized formula exhibited acceptable ranges; PS of 207.9 nm, PDI of 0.41 and %EE of 50.81%. Poloxamer 407 (Plx) at different concentrations (16%, 18%, 20% w/v), with different mucoadhesive polymers (Carbopol-974P, Na alginate, Na-CMC) were evaluated for gelling time and temperature, pH and mucoadhesion. The chosen mucoadhesive in-situ gel formula; 18% Plx 407 based-0.75%w/v Na-CMC, showed acceptable results, so that the optimized SLNs formula was further dispersed in it and evaluated for in vitro release, stability, in vivo and pharmacokinetics studies. Biomarkers' evaluation and histopathological examination were also investigated. Results revealed rapid ALM brain delivery of the optimized formula; Brain/blood ratios at 10 min. for NF (SLNs based IN in-situ gel), ND (Free ALM IN in situ gel) and ALM i.v. (ALM IV solution) were 0.89, 0.19 and 0.31, respectively. Toxicological results confirmed the safety of NF for nasal administration. The achieved out comings are encouraging for further clinical trials of the developed system in humans in future research.


Asunto(s)
Encéfalo/metabolismo , Sistemas de Liberación de Medicamentos , Nanopartículas/administración & dosificación , Agonistas de Receptores de Serotonina/administración & dosificación , Triptaminas/administración & dosificación , Adhesividad , Administración Intranasal , Fosfatasa Alcalina/metabolismo , Animales , Liberación de Fármacos , Femenino , Geles , Inmunoglobulina E/metabolismo , L-Lactato Deshidrogenasa/metabolismo , Lípidos/administración & dosificación , Lípidos/química , Nanopartículas/química , Mucosa Nasal/efectos de los fármacos , Mucosa Nasal/metabolismo , Poloxámero/administración & dosificación , Poloxámero/química , Ratas Sprague-Dawley , Agonistas de Receptores de Serotonina/sangre , Agonistas de Receptores de Serotonina/química , Agonistas de Receptores de Serotonina/farmacocinética , Distribución Tisular , Triptaminas/sangre , Triptaminas/química , Triptaminas/farmacocinética
13.
Curr Pharm Des ; 2017 11 27.
Artículo en Inglés | MEDLINE | ID: mdl-29189137

RESUMEN

BACKGROUND: Lipid based nanocarriers have gained recently enormous interest for pharmaceutical application. They have the potential to provide controlled drug release and to target the drug to a specific area. In addition, lipid based nanocarriers can improve the bioavailability of drugs suffering from high hepatic first-pass metabolism, by enhancing their transport via the lymphatic system. The main components of lipid based nanocarriers are lipids and surfactants. Both have great influence on the prepared lipid based systems characteristics. The criteria for their selection are much related to physicochemical properties of the drug and the required administration route. This work gives an overview on the effect of both the type and amount of lipids and surfactants used in the manufacture of lipid based nanocarriers on their behavior and characteristics. CONCLUSION: Recent studies revealed that the properties of the final product including; particle size, homogeneity, drug loading capacity, zeta potential, drug release profile, stability, permeability, pharmacokinetic properties, crystallinity and cytotoxicity, may be significantly influenced not only by the type but also the amount of the lipids and/or surfactants included in the formulation of the lipid based nanocarriers.

14.
Curr Drug Deliv ; 13(6): 882-98, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27109335

RESUMEN

BACKGROUND: The use of triptans in the treatment of migraine was a breakthrough. Their selective agonistic action at serotonin (5-hydroxytryptamine) receptors has provided insights into the pathophysiology of migraine and represented a significant advance in migraine pharmacotherapy. Sumatriptan was the first synthesized triptan available for clinical use in the United States. Although it revolutionized the treatment of migraine, it demonstrated some drawbacks, e.g. poor oral bioavailability, erratic absorption, and high rate of headache recurrence. New triptans have been developed namely; almotriptan, zolmitriptan, rizatriptan, eletriptan, frovatriptan and naratriptan, with each one demonstrating specific pharmacokinetic parameters that may be translated into clinical advantage. Although second generation triptans possess better bioavailability compared to sumatriptan, they all still need improvement. OBJECTIVE: This review illustrates a survey for the available researches aimed to enhance triptans' bioavailability and hence effectiveness, either by investigating alternative routes of administration, other than oral route and/or designing appropriate formulations. RESULTS: Promising results were gained by many researchers after studying different routes for triptans' administration, e.g. nasal, buccal, sublingual, transdermal and pulmonary using well designed formulations, e.g. nanocarriers, microcarriers, orodispersible tablets or films, in situ gels, microneedles for transdermal application, etc. CONCLUSION: Utilizing alternative routes for triptans' administration in addition to designing appropriate formulations, were successful approaches. However, further investigations should be conducted to establish their bioavailability and in vitro- in vivo correlation studies are also required, to confirm the potential of the designed formulations for use in humans, hence novel efficient triptans' formulations may appear on the market in the near future.


Asunto(s)
Trastornos Migrañosos/tratamiento farmacológico , Triptaminas/administración & dosificación , Disponibilidad Biológica , Vías de Administración de Medicamentos , Composición de Medicamentos , Sistemas de Liberación de Medicamentos , Humanos , Triptaminas/farmacocinética , Triptaminas/uso terapéutico
15.
Int J Pharm ; 486(1-2): 297-305, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25843757

RESUMEN

The study demonstrates the feasibility of prolonging gastric residence time and release rate of metronidazole (Mz) by preparing floating raft system (FRS) using ion-sensitive in situ gel forming polymers. FRSs contained 3, 4, 5 and 0.5, 0.75, 1% w/v sodium alginate (Alg) and gellan gum (G), respectively, 0.25% w/v sodium citrate and calcium carbonate (C). Lipids: glyceryl mono stearate (GMS), Precirol(®) and Compritol(®) were incorporated into G-based formulations (G1%C1%). Mz:lipid ratio was 1:1, except for Mz:GMS, ratios of 1:1.5 and 1:2 were also investigated. Buoyancy, gelation capacity and viscosity parameters were evaluated. Drug release and kinetics for selected formulae were examined. The selected lipid containing formula was subjected to an accelerated stability testing. Alg4%C2% FRS exhibited short gelation lag time (3s), long duration (>24h), floating lag time 1m in and duration >24h, and a reliable sustained drug release (MDT 6h). Gellan gum FRSs achieved successful floating gastroretention, but failed to achieve the required gelation capacity. Incorporation of GMS (Mz:GMS 1:1) enhanced the gelation lag time and duration (6s and >24h, respectively), keeping sustained drug release and formulation stability. The improved characteristics of the selected FRS make them excellent candidates for gastric targeting to eradicate Helicobacter pylori.


Asunto(s)
Antiinfecciosos/química , Sistemas de Liberación de Medicamentos , Metronidazol/química , Alginatos/química , Diglicéridos/química , Liberación de Fármacos , Ácidos Grasos/química , Ácido Glucurónico/química , Glicéridos/química , Infecciones por Helicobacter , Helicobacter pylori , Ácidos Hexurónicos/química , Polisacáridos Bacterianos/química
16.
Int J Pharm ; 487(1-2): 305-13, 2015 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-25865569

RESUMEN

Resveratrol (Res), a polyphenolic phytoalexin, had shown a promising therapeutic efficacy towards treatment of periodontal disease in vitro. This work aims to develop Res microbeads with strong mucoadhesion using thiolated alginate (TA) for local treatment of periodontal pockets. TA was synthesized by conjugating sodium alginate (A) with thioglycolic acid. Product was evaluated by IR and DSC. Both A and A:TA Res microbeads with different ratios were prepared by ionotropic gelation method. Formulations were evaluated regarding their entrapment efficiency (%EE), swelling index (SI), in vitro drug release and kinetics. Selected formula was examined for its mucoadhesion by ex vivo wash-off method, surface morphology using scanning electron microscope (SEM) and stability against light. Clinical evaluation is running.Formation of TA was confirmed. %EE for all formulations ranged from 83.72 to 104.54%. Results revealed a significant lower SI for TA rich formulation (A/TA 1:1) along with slower release rate and zero-order kinetics, in addition to powerful mucoadhesion; 26% remaining of microbeads after 1h, compared to 2% for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its %EE after 5h exposure to direct sunlight. A/TA 1:1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.


Asunto(s)
Alginatos/química , Antioxidantes/administración & dosificación , Membrana Mucosa/efectos de los fármacos , Estilbenos/administración & dosificación , Compuestos de Sulfhidrilo/química , Animales , Química Farmacéutica , Pollos , Sistemas de Liberación de Medicamentos , Excipientes , Encía , Ácido Glucurónico/química , Ácidos Hexurónicos/química , Tamaño de la Partícula , Resveratrol , Solubilidad , Tioglicolatos , Adhesivos Tisulares
17.
Curr Drug Deliv ; 11(3): 306-12, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24678600

RESUMEN

Since the discovery of Helicobacter pylori (H. pylori) in the early 1980s, its eradication has been one of the most important global challenges in gastroenterology. Various circumstances make the treatment with antimicrobials particularly difficult. One problem has been that antibiotics commonly used were designed for the treatment of infections throughout the body rather than for delivering high concentrations locally within the stomach. Many gastroretentive dosage forms were developed in order to eradicate the infection, yet additional advancements are still needed to eliminate the infection completely and decrease its prevalence worldwide. An overview on different antimicrobials and a literature survey about different drug delivery systems used in eradication of H. pylori infection are presented in this review.


Asunto(s)
Antibacterianos/administración & dosificación , Antiulcerosos/administración & dosificación , Sistemas de Liberación de Medicamentos , Infecciones por Helicobacter/tratamiento farmacológico , Adaptación Fisiológica , Animales , Infecciones por Helicobacter/epidemiología , Infecciones por Helicobacter/microbiología , Helicobacter pylori/fisiología , Humanos , Prevalencia , Estómago/microbiología
18.
Int J Pharm ; 464(1-2): 10-8, 2014 Apr 10.
Artículo en Inglés | MEDLINE | ID: mdl-24472642

RESUMEN

Size increasing (plug-type) levofloxacin hemihydrate (LVF) tablets for eradication of Helicobacter pylori (H. pylori) were prepared using in situ gel forming polymers including: gellan gum, sodium alginate, pectin and xanthan gum. Effect of cross-linkers: calcium and aluminum chloride, on the drug release was also studied. The prepared tablets were evaluated for their physicochemical parameters: weight variation, thickness, friability, hardness, drug content, water uptake and in vitro drug release. The optimized formula was subjected to further studies such as radial swelling test, FT-IR and DSC. Results revealed that LVF release depends not only on the nature of the matrix but also on the type of cross linker used to form this polymeric matrix. The addition of either calcium chloride or aluminum chloride, as cross-linkers, to gellan gum formulations significantly decreased drug release. Other polymers' formulations resulted in increased drug release upon addition of the same cross-linkers. The formula containing xanthan gum without any cross linker showed the most sustained LVF release with an increase in diameter with time, thus acting as a plug-type dosage form. IR spectra and DSC thermograms of LVF, xanthan gum, and a physical mixture of both, indicated that there was no interaction between the drug and the polymer and confirmed the drug stability.


Asunto(s)
Antibacterianos/química , Química Farmacéutica/métodos , Mucosa Gástrica , Levofloxacino/química , Polisacáridos Bacterianos/química , Antibacterianos/farmacocinética , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Evaluación Preclínica de Medicamentos/métodos , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Helicobacter pylori/efectos de los fármacos , Levofloxacino/farmacocinética , Polisacáridos Bacterianos/farmacocinética
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