Stimulus-responsive drug-loaded poly (N-isopropylacrylamide) nanogels were examined as a means of enhancing the delivery of naproxen into skin ex vivo. Following massaging into skin, the epidermis was probed (with and without base activation) for depth penetration and transdermal delivery of drug, and anti-inflammatory activity in the relative levels of COX-2 expression. Rat paw oedema testing was used to determine anti-inflammatory effects in vivo.
View Article and Find Full Text PDFThe sentinel lymph node (SLN) is defined as the first regional lymph node to receive lymphatic drainage from a malignant tumor. Therefore, this node is a "sentinel" for second metastatic lymph node stations and for labeling regional tumor spread. For SLN detection, many surgeons preferred a combination of a preoperative injection of radiolabeled colloid and the intraoperative injection of blue dye.
View Article and Find Full Text PDFThe ease of application and no requirement of extra energy input make the microemulsion method favorable for solid lipid nanoparticles (SLNs) production. Very limited data are available to date on preparation of SLNs from pre-screened microemulsion phase diagrams. The purpose of this study was to investigate the microemulsion formation area with solid lipids using hot ternary phase diagrams at elevated temperatures and to use selected microemulsions for SLN production.
View Article and Find Full Text PDFThis study aimed to develop a suitable buccal mucoadhesive nanoparticle (NP) formulation containing fluconazole for the local treatment of oral candidiasis. The suitability of the prepared formulations was assessed by means of particle size (PS), polydispersity index, and zeta potential measurements, morphology analysis, mucoadhesion studies, drug entrapment efficiency (EE), in vitro drug release, and stability studies. Based on the optimum NP formulation, ex vivo drug diffusion and in vitro cytotoxicity studies were performed.
View Article and Find Full Text PDFObjectives: The aim of the present study was to develop novel ofloxacin (OFX)-loaded nanostructured lipid carrier (NLC)-based inserts for ocular application for treatment of bacterial keratitis.
Methods: NLC loaded with 0.3% OFX was prepared by means of high shear homogenization and 0.
The objective of this study was to explore the potential of the nanostructured lipid carriers (NLCs) modified with chitosan oligosaccharide lactate (COL) for topical ocular application. Ofloxacin (OFX) loaded NLCs were prepared by microemulsion or high shear homogenization methods. For combination of NLCs Compritol HD5 ATO was used as solid lipid, oleic acid as liquid lipid, Tween 80 as surfactant, ethanol as co-surfactant.
View Article and Find Full Text PDFThe objective of this study is to develop a new textile-based drug delivery system containing naproxen (NAP) microparticles and to evaluate the potential of the system as the carrier of NAP for topical delivery. Microparticles were prepared by spray-drying using an aqueous ethyl cellulose dispersion. The drug content and entrapment efficiency, particle size and distribution, particle morphology and in vitro drug release characteristics of microparticles were optimized for the application of microparticles onto the textile fabrics.
View Article and Find Full Text PDFPurpose: The aim of this study was to prepare a novel oil-in-water microemulsion of ofloxacin (OFX) for topical ocular application.
Methods: Pseudo-ternary phase diagrams were constructed for combination of oleic acid as oil phase, Tween 80 as surfactant, ethanol as co-surfactant, and 0.5 N NaOH solutions as aqueous phase.
Eur J Drug Metab Pharmacokinet
December 2014
The main objective of this study was to investigate the release and pharmacokinetic profiles of ketoprofen (KP) from developed thermosensitive and mucoadhesive liquid suppositories. Thermosensitive liquid suppositories were prepared using KP, poloxamer 407 (P 407), poloxamer 188 (P 188) and various amounts of different mucoadhesive polymers. In vitro release studies was monitored by the USP XXVI paddle method.
View Article and Find Full Text PDFIn this study, a microemulsion system was evaluated for delivery of mitomycin C (MMC). To track the distribution of the formulated drug after intravenous administration, radiochemical labeling and gamma scintigraphy imaging were used. The aim was to evaluate a microemulsion system for intravenous delivery of MMC and to compare its in vivo behavior with that of the MMC solution.
View Article and Find Full Text PDFAim: To develop a suitable buccal bioadhesive gel formulation containing cyclosporine A solid lipid nanoparticles (CsA SLNs) for the treatment of recurrent aphthous stomatitis.
Methods: The suitability of the prepared formulations for buccal application was assessed by means of rheological studies, textural profile analysis, and ex vivo drug-release studies. Plastic flows, typical gel-like spectra, and suitable mechanical properties were obtained from prepared formulations.
The aim of the study was to accelerate the dissolution of the sustained release dosage forms using both elevated temperature and high rpm rates. Teokap(®) SR 200 mg pellets were tested by in vitro sustained and accelerated dissolution studies using USP XXIII rotating paddle method. Sustained dissolution studies were carried out for 12 h in phosphate buffer at 37 ± 0.
View Article and Find Full Text PDFJ Biomed Nanotechnol
August 2009
In this study, the lipophilic matrix tablets of metronidazole were prepared with Cutina HR (hydrogenated castor oil), stearic acid, Compritol ATO 888 (glyceryl behenate) and Precirol ATO 5 (glycerol palmitostearate) in two different shapes; cylinder and hexagonal. Our first aim was to investigate the influence of the lipid excipients and geometric shape on the release behavior of metronidazole, and the second aim was to investigate the influence of tablet surface area/volume (SA/V) ratio on drug release from controlled release matrix tablets. In vitro release test was performed using a standard USP dissolution apparatus I.
View Article and Find Full Text PDFThis study developed and examined the characterization of Benzidamine hydrochloride (BNZ) bioadhesive gels as platforms for oral ulcer treatments. Bioadhesive gels were prepared with four different hydroxypropylmethylcellulose (HPMC) types (E5, E15, E50 and K100M) with different ratios. Each formulation was characterized in terms of drug release, rheological, mechanical properties and adhesion to a buccal bovine mucosa.
View Article and Find Full Text PDFThe purpose of this research was to develop an emulsion formulation of indomethacin (IND) suitable for nasal delivery. IND was incorporated into the oil phases of oil in water (O/W) and water in oil (W/O) emulsions. For this purpose, different emulsifying agents (Tween 80, Span 80 and Brij 58) were used in two emulsion formulations.
View Article and Find Full Text PDFThe objective of this study was to prepare and evaluate biodegradable alginate beads as a controlled-release system for a water-insoluble drug, mefenamic acid (MA), using 3 x 2(2) factorial design by ionotropic gelation method. Therefore, the mefenamic acid dispersion in a solution of alginate was dropped into the cross-linking CaCl(2) solution and a fairly high yield (71-89%) of MA-alginate beads were obtained. Their encapsulation efficiencies were in the range of 79.
View Article and Find Full Text PDFIn some multidrug therapy programs, ketoconazole (KTZ) may be administered with some antacids that could modify its dissolution rate and reduce its absorption, thus leading to therapeutic failures. The primary aim of this study was to evaluate the influence of Compritol HD5 ATO and Compritol 888 ATO on this interaction in comparison with commercial KTZ tablets. The second aim was to prepare lipid granules of KTZ that could be an alternative to the commercial formulation.
View Article and Find Full Text PDFThe aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of w/o microemulsion (M) and gel (G) bases for diclofenac sodium (DS). The effect of dimethyl sulfoxide (DMSO) as a penetration enhancer was also examined when it was added to the M formulation. To study the in vitro potential of these formulations, permeation studies were performed with Franz diffusion cells using excised dorsal rat skin.
View Article and Find Full Text PDFIn this study, the first aim was to investigate the swelling and relaxation properties of lipid matrix on diffusional exponent (n). The second aim was to determine the desired release profile of metronidazole lipid matrix tablets. We prepared metronidazole lipid matrix granules using Carnauba wax, Beeswax, Stearic acid, Cutina HR, Precirol ATO 5, and Compritol ATO 888 by hot fusion method and pressed the tablets of these granules.
View Article and Find Full Text PDFThe purpose of this study is to obtain a drug release at a constant rate with a megaloporous tablet, which was prepared with a simple formulation. These tablets were prepared with two kinds of granules. One of them is the restraining-phase matrix granule (RMG) and it controls the release rate of the drug.
View Article and Find Full Text PDFVaginal suppository formulations of metronidazole were prepared using six different bases as Witepsol H15, Cremao, Ovucire WL2944, Ovucire WL3264, PEG 1500, PEG 6000. Three different dissolution methods were used to evaluate the in vitro drug release from the suppositories. The diffusion studies were performed through synthetic (cellophane) and natural membrane (rabbit vagina), but the drug did not show good permeation characteristics from natural membrane.
View Article and Find Full Text PDFExtended release liphophilic microspheres of indomethacin were prepared using cetostearyl alcohol (CsA), stearyl alcohol (SA) and cetyl alcohol (CA) in the various drug-lipid ratios. The release of indometacin was studied on the basis of USP criteria and the effects of drug-lipid ratio, the size of microspheres and carboxymethylcellulose sodium (CMC-Na) added as a hydrophilic polymer on the drug release were investigated. In vitro dissolution studies were performed using USP XXIII apparatus I at pH 6.
View Article and Find Full Text PDFThe objective of this study was to develop a mathematical equation for the calculation of drug release from different shaped matrix tablets. By this way, release rate related to the geometric shape could be predicted with the help of the developed mathematical equation. So, drug release could be estimated before the dissolution.
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