Search Results (5)

Innovative hybrid chitosan–sodium alginate (Ch–Ag) microparticles (MPs) were fabricated using both the ionic gelation method as well as the pre-gelation technique. The hybrid Ch–Ag MPs were studied for size, zeta potential, morphology, mucoadhesion, in-vitro release, corneal permeation, and ocular irritation using lens and corneal epithelial cell lines. The average particle size ranged from 1322 nm to 396 nm. The zeta potential for the prepared formulations showed an increase with increasing Ch concentrations up to a value of >35 mV; the polydispersity index (PDI) of some optimized MPs was around 0.1. Compared to drug-free MPs, ketorolac-loaded Ch–Ag MPs demonstrated a drug proportion-dependent increase in their size. SEM, as well as TEM of KT-loaded MPs, confirmed that the formed particles were quasi-spherical to elliptical in shape. The KT release from the MPs demonstrated a prolonged release profile in comparison to the control KT solution. Further, mucoadhesion studies with porcine mucin revealed that the KT-loaded MPs had effective mucoadhesive properties, and polymeric particles were stable in the presence of mucin. Corneal permeation was studied on bovine eyes, and the results revealed that Ch-based MPs were capable of showing more sustained KT release across the cornea compared with that for the control drug solution. Conclusively, the cytotoxicity assay confirmed that the investigated MPs were non-irritant and could confer protection from direct drug irritation of KT on the ocular surface. The MTT cytotoxicity assay confirmed that KT-loaded MPs showed acceptable and reasonable tolerability with both human lens and corneal epithelial cell lines compared to the control samples. Full article

Sialolithiasis mainly affects the oral salivary glands due to the presence of small stones that obstruct the secretion of saliva. The treatment and control of pain and inflammation during the course of this pathology is essential to guarantee the patient’s comfort. For this reason, a ketorolac calcium cross-linked alginate hydrogel was developed, and it was then applied in the area of the buccal cavity. The formulation was characterized (swelling and degradation profile, extrusion, extensibility, surface morphology, viscosity, and drug release). The drug release was studied ex vivo in static Franz cells and with a dynamic ex vivo method under artificial saliva continuous flow. The product exhibits adequate physicochemical properties considering the intended purpose, and the drug concentrations retained in the mucosa were high enough to deliver a therapeutic local concentration able to reduce the pain associated with the patient’s conditions. The results confirmed the suitability of the formulation for application in the mouth. Full article

Biodegradable metal alloys may be successfully used to support bone repair, avoiding second surgery commonly needed when inert metal alloys are used. Combining a biodegradable metal alloy with a suitable pain relief agent could improve patient quality of life. AZ31 alloy was coated using a poly(lactic-co-glycolic) acid (PLGA) polymer loaded with ketorolac tromethamine using the solvent casting method. The ketorolac release profile from the polymeric film and the coated AZ31 samples, the PLGA mass loss of polymeric film, and the cytotoxicity of the optimized coated alloy were assessed. The coated sample showed a ketorolac release that was prolonged for two weeks, which was slower than that of just the polymeric film, in simulated body fluid. PLGA mass loss was complete after a 45-day immersion in simulated body fluid. The PLGA coating was able to lower AZ31 and ketorolac tromethamine cytotoxicity observed in human osteoblasts. PLGA coating also prevents AZ31 cytotoxicity, which was identified in human fibroblasts. Therefore, PLGA was able to control ketorolac release and protect AZ31 from premature corrosion. These characteristics allow us to hypothesize that the use of ketorolac tromethamine-loaded PLGA coating on AZ31 in the management of bone fractures can favor osteosynthesis and relief pain. Full article

This study describes the preparation and evaluation of two formulations, a hydrogel and a nanostructured system, containing ketorolac tromethamine as an anti-inflammatory agent for the local therapy against the inflammatory process derived from the surgical excision of Condyloma acuminata. Both formulations were physicochemically characterized. In vitro release profiles show that the nanoparticles release 92% ± 2.3 of the total ketorolac tromethamine encapsulated, while the chitosan gel releases 18.6% ± 0.2. The ex vivo permeation and distribution through human skin were also assayed and was observed how the main amount of ketorolac tromethamine is retained in the epidermis. In vivo studies were accomplished to evaluate the anti-inflammatory efficacy in mice which also involved the histological analysis to confirm the in vivo results. The nanoparticles present a significantly higher anti-inflammatory efficacy than chitosan gel. The tolerability of developed formulations was assessed by monitoring the biomechanical properties of the skin before and after application of both formulations. No statistical differences in trans-epidermal water loss and skin hydration with respect to the basal values were observed and the formulations exhibited higher anti-inflammatory activity compared to a reference ketotorlac tromethamine solution. Therefore, it can be concluded that both formulations can be proposed as outstanding candidates for offering a local anti-inflammatory therapeutical tool with potential clinical application. Full article

Matrix tablets of ketorolac trometharnine (KT) were prepared by direct compression technique and Carbopol 934, 940 and 1342 have been used as polymers in different concentrations (5-15 % ). For the quality control of tablets; physical tests as crushing strength, diameter-height ratio and fkiability, KT amount assay and in vitro dissolution techniques were performed and dissolution profiles were plotted and evaluated kinetically. The in vitro release kinetics of ten different formulations of KT matrix tablet were studied at pH 1.2 and pH 7.0 using the USP dissolution technique and apparatus with basket assembly. Dissolution results were evaluated kinetically and statistically. According to our results, different types and concentrations of carbopol to tablet formulations may effect in controlled drug release. Full article