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1.
Drug Deliv ; 23(8): 3017-3026, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-26821766

RESUMEN

Contact lenses for ophthalmic drug delivery have become very popular, due to their unique advantages like extended wear and more than 50% bioavailability. To achieve controlled and sustained drug delivery from contact lenses, researchers are working on various systems like polymeric nanoparticles, microemulsion, micelle, liposomes, use of vitamin E, etc. Numerous scientists are working on different areas of therapeutic contact lenses to treat ocular diseases by implementing techniques like soaking method, molecular imprinting, entrapment of drug-laden colloidal nanoparticles, drug plate/film, ion ligand polymeric systems, supercritical fluid technology, etc. Though sustained drug delivery was achieved using contact lens, the critical properties such as water content, tensile strength (mechanical properties), ion permeability, transparency and oxygen permeability were altered, which limit the commercialization of therapeutic contact lenses. Also issues like drug stability during processing/fabrication (drug integrity test), zero order release kinetics (prevent burst release), drug release during monomer extraction step after fabrication (to remove un-reacted monomers), protein adherence, drug release during storage in packaging solution, shelf life study, cost-benefit analysis, etc. are still to be addressed. This review provides an expert opinion on different methodology to develop therapeutic contact lenses with special remark of their advantages and limitations.


Asunto(s)
Sistemas de Liberación de Medicamentos/métodos , Ojo/efectos de los fármacos , Soluciones Oftálmicas/administración & dosificación , Administración Oftálmica , Animales , Disponibilidad Biológica , Lentes de Contacto , Nanopartículas/química , Soluciones Oftálmicas/química , Polímeros/química
2.
J Biomater Sci Polym Ed ; 26(15): 1035-50, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26176811

RESUMEN

Current dry eye treatment includes delivering comfort enhancing agents to the eye via eye drops, but low residence time of eye drops leads to low bioavailability. Frequent administration leads to incompliance in patients, so there is a great need for medical device such as contact lenses to treat dry eye. Studies in the past have demonstrated the efficacy of hyaluronic acid (HA) in the treatment of dry eyes using eye drops. In this paper, we present two methods to load HA in hydrogel contact lenses, soaking method and direct entrapment. The contact lenses were characterized by studying their optical and physical properties to determine their suitability as extended wear contact lenses. HA-laden hydrogel contact lenses prepared by soaking method showed release up to 48 h with acceptable physical and optical properties. Hydrogel contact lenses prepared by direct entrapment method showed significant sustained release in comparison to soaking method. HA entrapped in hydrogels resulted in reduction in % transmittance, sodium ion permeability and surface contact angle, while increase in % swelling. The impact on each of these properties was proportional to HA loading. The batch with 200-µg HA loading showed all acceptable values (parameters) for contact lens use. Results of cytotoxicity study indicated the safety of hydrogel contact lenses. In vivo pharmacokinetics studies in rabbit tear fluid showed dramatic increase in HA mean residence time and area under the curve with lenses in comparison to eye drop treatment. The study demonstrates the promising potential of delivering HA through contact lenses for the treatment of dry eye syndrome.


Asunto(s)
Lentes de Contacto de Uso Prolongado , Síndromes de Ojo Seco/tratamiento farmacológico , Ácido Hialurónico/administración & dosificación , Hidrogeles , Viscosuplementos/administración & dosificación , Animales , Cationes Monovalentes/química , Línea Celular , Preparaciones de Acción Retardada/química , Células Epiteliales/efectos de los fármacos , Células Epiteliales/fisiología , Ácido Hialurónico/efectos adversos , Ácido Hialurónico/farmacocinética , Hidrogeles/química , Ensayo de Materiales , Permeabilidad , Conejos , Sodio/química , Lágrimas/química , Viscosuplementos/efectos adversos , Viscosuplementos/farmacocinética , Agua/química
3.
Curr Drug Deliv ; 11(3): 380-91, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24611664

RESUMEN

The study investigates the combined influence of three independent variables in preparation of aceclofenac ternary solid dispersion (SD) by kneading method. A 3-factor, 3-level Box-Behnken design was used. Independent variables selected were microcrystalline cellulose (Avicel 200 = X1), hydroxypropyl methylcellulose-5 cps (HPMC E-5 = X2), and ratio of drug to polymer mixture (X3). Fifteen batches were prepared and evaluated for angle of repose and percentage drug release at 5 minutes (Q5). The transformed values of variables were subjected to multiple regression analysis to establish a second-order polynomial equation. Contour plots were constructed to evaluate the effects of X1, X2 and X3 on Q5 and angle of repose. Model was validated for accurate prediction of Q5 and angle of repose (AR) by performing checkpoint analysis. The computer optimization process and contour plots predict the levels of independent variables as X1= +0.5, X2 = -1 and X3 = +0.35 for maximized response of Q5 with better flow property. The stability study during 6 months confirms that aceclofenac exhibits high stability in solid dispersion. In vivo studies indicate that optimized ternary solid dispersion provides rapid pharmacological responses in mice and rats compared to marketed formulation.


Asunto(s)
Analgésicos/química , Antiinflamatorios no Esteroideos/química , Diclofenaco/análogos & derivados , Ácido Acético , Analgésicos/administración & dosificación , Animales , Antiinflamatorios no Esteroideos/administración & dosificación , Carragenina , Celulosa/química , Química Farmacéutica , Diclofenaco/administración & dosificación , Diclofenaco/química , Estabilidad de Medicamentos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Derivados de la Hipromelosa/química , Masculino , Ratones , Dolor/inducido químicamente , Dolor/tratamiento farmacológico , Ratas Wistar , Solubilidad
4.
ISRN Pharm ; 2012: 528079, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-22852100

RESUMEN

Conventional drug delivery systems are known to provide an immediate release of drug, in which one can not control the release of the drug and can not maintain effective concentration at the target site for longer time. Controlled drug delivery systems offer spatial control over the drug release. Osmotic pumps are most promising systems for controlled drug delivery. These systems are used for both oral administration and implantation. Osmotic pumps consist of an inner core containing drug and osmogens, coated with a semipermeable membrane. As the core absorbs water, it expands in volume, which pushes the drug solution out through the delivery ports. Osmotic pumps release drug at a rate that is independent of the pH and hydrodynamics of the dissolution medium. The historical development of osmotic systems includes development of the Rose-Nelson pump, the Higuchi-Leeper pumps, the Alzet and Osmet systems, the elementary osmotic pump, and the push-pull system. Recent advances include development of the controlled porosity osmotic pump, and systems based on asymmetric membranes. This paper highlights the principle of osmosis, materials used for fabrication of pumps, types of pumps, advantages, disadvantages, and marketed products of this system.

5.
J Agric Food Chem ; 58(4): 2095-9, 2010 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-20092313

RESUMEN

Curcumin is the lipid-soluble antioxidant compound obtained from the rhizome of Curcuma longa Linn, also known as turmeric. Curcumin targets multiple chemotherapeutic and inflammatory pathways and has demonstrated safety and tolerability in humans, supporting its potential as a therapeutic agent; however, the clinical literature lacks conclusive evidence supporting its use as a therapeutic agent due to its low bioavailability in humans. The purpose of this study was to quantify plasma levels of free curcumin after dosing of a solid lipid curcumin particle (SLCP) formulation versus unformulated curcumin in healthy volunteers and to determine its tolerability and dose-plasma concentration relationship in late-stage osteosarcoma patients. Doses of 2, 3, and 4 g of SLCP were evaluated in 11 patients with osteosarcoma. Plasma curcumin levels were measured using a validated high-performance liquid chromatography method. The limit of detection of the assay was 1 ng/mL of curcumin. In healthy subjects, the mean peak concentration of curcumin achieved from dosing 650 mg of SLCP was 22.43 ng/mL, whereas plasma curcumin from dosing an equal quantity of unformulated 95% curcuminoids extract was not detected. In both healthy individuals and osteosarcoma patients, high interindividual variability in pharmacokinetics and nonlinear dose dependency was observed, suggesting potentially complex absorption kinetics. Overall, good tolerability was noted in both healthy and osteosarcoma groups.


Asunto(s)
Antineoplásicos/farmacocinética , Neoplasias Óseas/tratamiento farmacológico , Curcumina/farmacocinética , Osteosarcoma/tratamiento farmacológico , Adolescente , Adulto , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Química Farmacéutica , Niño , Cromatografía Líquida de Alta Presión/métodos , Curcuma/química , Curcumina/aislamiento & purificación , Curcumina/farmacología , Curcumina/uso terapéutico , Tolerancia a Medicamentos , Femenino , Humanos , Masculino , Valores de Referencia , Seguridad , Adulto Joven
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