Aceclofenac (AC) is a phenyl acetic acid derivative [2-(2',6'-dichlorophenyl)amino] phenylacetoxyacetic acid], a novel NSAID indicated for the symptomatic treatment of pain and inflammation (1). The short biological half-life (about 4 h) and high frequency of dosing make aceclofenac an ideal candidate for sustained release. The bioadhesive microspheres of aceclofenac would prolong the residence time at the absorption site to facilitate intimate contact with the absorption surface and thereby improve and enhance bioavailability and increase patient compliance. Natural hydrophilic polymers like alginate and pectin are widely used in numerous biomedical applications for their bioadhesion properties. Alginic acid and pectin are natural polysaccharides that are widely Ionotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigated in vitro for possible sustained drug release and their use in vivo as a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.
Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.
Recent developments in nanotechnology and process chemistry have expanded the scope of nanostructures to the biomedical field. The ability of nanostructures to precisely deliver drugs to the target site not only reduces the amount of drug needed but also reduces systemic adverse effects. Carbon nanostructures gained traction in pharmaceutical technology in the last decade due to their high stability, ease of synthesis, tunable surface chemistry, and biocompatibility. Fullerene, nanotubes, nanodiamonds, nanodots, and nanoribbons are among the major carbon nanostructures that have been extensively studied for applications in tissue engineering, biosensing, bioimaging, theranostics, drug delivery, and gene therapy. Due to the fluorescent properties of functionalized nanostructures, they have been extensively studied for use as probes in cellular imaging. Moreover, these nanostructures are promising candidates for delivering drugs to the brain, bones, and deep-seated tumors. Still, research gaps need to be addressed regarding the toxicity of these materials in animals as well as humans. This review highlights the physicochemical properties of carbon nanostructures and their categories, methods of synthesis, various techniques for surface functionalization, major biomedical applications, mechanisms involving the cellular uptake of nanostructures, pharmacokinetic considerations, recent patents involving carbon-based nanostructures in the biomedical field, major challenges, and future perspectives.
The aim of this present research work was to prepare and evaluate alginate microspheres of aceclofenac by ionic gelation method for targeting the drug release in intestinal region and decrease distinct tissue protection in the stomach. This method offers to prepare microspheres which are important in controlling the release rate and the absorption of aceclofenac from the intestinal region. Variation in polymer concentration was studied systemically for their influence on the encapsulation efficacy, particle size and in vitro drug release. The enteric nature of the microspheres showed very less amount of drug released in acidic medium. The mucoadhesion property was strongly dependent on the pH of the medium and the polymer concentration in the formulations. In vitro drug release study proposed a mixed drug release mechanism, partially involving the sphere matrix disintegration and drug diffusion of the microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t50% values among all the microsphere formulations. In vivo studies revealed that the anti-inflammatory effect induced by the aceclofenac loaded alginate microspheres was significantly high and prolonged than that induced by the pure aceclofenac. So, this aceclofenac loaded alginate microspheres exhibited promising properties to improve the patient compliance by controlling and prolonging the systemic absorption of aceclofenac along with a distinct tissue protection in the stomach.
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