brij-58 and sorbitan-monooleate

The aim of the present study was to make a comparison of the in vitro release rate of diclofenac sodium (DS) from microemulsion (M) vehicles containing soybean oil, nonionic surfactants (Brij 58 and Span 80), and different alcohols (ethanol [E], isopropyl alcohol [I], and propanol [P]) as cosurfactant. The optimum surfactant:cosurfactant (S:CoS) weight ratios and microemulsion areas were detected by the aid of phase diagrams. Three microemulsion formulations were selected, and their physicochemical properties were examined for the pH, viscosity, and conductivity. According to the release rate of DS, M prepared with P showed the significantly highest flux value (0.059 +/- 0.018 mg/cm(2)/h) among all formulations (P < .05). The conductivity results showed that DS-loaded microemulsions have higher conductivity values (18.8-20.2 microsiemens/cm) than unloaded formulations (16.9-17.9 microsiemens/cm), and loading DS into the formulation had no negative effect on system stability. Moreover, viscosity measurements were examined as a function of shear rate, and Newtonian fluid characterization was observed for each microemulsion system. All formulations had appropriate observed pH values varying from 6.70 to 6.85 for topical application. A skin irritation study was performed with microemulsions on human volunteers, and no visible reaction was observed with any of the formulations. In conclusion, M prepared with P may be a more appropriate formulation than the other 2 formulations studied as drug carrier for topical application.

Topics: 1-Propanol; 2-Propanol; Administration, Cutaneous; Anti-Inflammatory Agents, Non-Steroidal; Cetomacrogol; Chemistry, Pharmaceutical; Diclofenac; Drug Carriers; Drug Compounding; Electric Conductivity; Emulsions; Erythema; Ethanol; Female; Hexoses; Humans; Hydrogen-Ion Concentration; Kinetics; Male; Models, Chemical; Particle Size; Skin; Skin Irritancy Tests; Solubility; Soybean Oil; Surface-Active Agents; Technology, Pharmaceutical; Viscosity; Water

Magnetic micro- and nanoparticles based on ferrofluid (maghemite) were elaborated by inverse emulsion crosslinking of sodium salt of carboxymethylcellulose (CMCNa) and gelatin. Crosslinking was carried out with glutaric aldehyde within aqueous droplets dispersed into toluene in presence of surfactants. The influence of parameters such as the ratio of polymers and maghemite in the initial mixture on the composition, size, size dispersity, particle swelling and their ability for drug inclusion was studied. The ability to take-up drugs is directly correlated with the degree of swelling and gelatin content within the particles. Particle size is between tens of nanometers and a few microns. The magnetic properties of particles are demonstrated from saturation magnetization (between 43 and 44 emu g(-1)) when their superparamagnetic character was shown by the absence of hysteresis on the magnetization curve. Polymer-drug systems elaborated under particles keep their bactericide activity for at least 48 h. The absence of toxicity, associated with the bactericide activity, make these systems potential drug carriers.

Topics: Aldehydes; Animals; Anti-Bacterial Agents; Antimetabolites, Antineoplastic; Carboxymethylcellulose Sodium; Cefotaxime; Cetomacrogol; Chemistry, Pharmaceutical; Cross-Linking Reagents; Delayed-Action Preparations; Diffusion; Drug Carriers; Drug Compounding; Ferric Compounds; Gelatin; Glutarates; Hexoses; Kinetics; Lethal Dose 50; Magnetics; Metal Nanoparticles; Methotrexate; Particle Size; Polysorbates; Pseudomonas aeruginosa; Rats; Solubility; Solvents; Staphylococcus aureus; Surface Properties; Surface-Active Agents; Technology, Pharmaceutical; Toluene

The 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. When the effects of several synthetic membranes (nylon, cellulose, cellulose nitrate) were compared with the sheep nasal mucosa, the cellulose membrane and sheep nasal mucosa showed similar permeation properties for O/W emulsion (P > 0.05). To examine the absorption characteristics of IND, the anti-inflammatory properties of intravenous solution of IND, intranasal O/W emulsions of IND (with or without enhancers) and intranasal solution of IND (IND-Sol) were investigated in rats with carrageenan-induced paw edema. When citric acid was added to the nasal emulsion, the anti-inflammatory activity was similar to that of intravenous solution (P > 0.05). Finally, it was concluded that, intranasal administration of IND emulsion with citric acid may be considered as an alternative to intravenous and per oral administrations of IND to overcome their adverse effects.

Topics: Administration, Intranasal; Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Cetomacrogol; Chemistry, Pharmaceutical; Citric Acid; Disease Models, Animal; Drug Compounding; Edema; Emulsifying Agents; Emulsions; Hexoses; Indomethacin; Injections, Intravenous; Male; Membranes, Artificial; Nasal Mucosa; Permeability; Polysorbates; Rats; Rats, Wistar; Sheep; Soybean Oil; Time Factors; Water