betadex and carprofen

The purpose of this study was the development of poly(d,l-lactide-co-glycolide) acid (PLGA) nanoparticles (NPs) for the dermal delivery of carprofen (CP). The developed nanovehicle was then lyophilized using hydroxypropyl-β-cyclodextrin (HPβCD) as cryoprotectant. The ex vivo permeation profiles were evaluated using Franz diffusion cells using three different types of skin membranes: human, porcine and bovine. Furthermore, biomechanical properties of skin (trans-epidermal water loss and skin hydration) were tested. Finally, the in vivo skin irritation and the anti-inflammatory efficacy were also assayed. Results demonstrated the achievement of NPs 187.32 nm sized with homogeneous distribution, negatively charged surface (-23.39 mV) and high CP entrapment efficiency (75.38%). Permeation studies showed similar diffusion values between human and porcine skins and higher for bovine. No signs of skin irritation were observed in rabbits. Topically applied NPs significantly decreased in vivo inflammation compared to the reference drug in a TPA-induced mouse ear edema model. Thus, it was concluded that NPs containing CP may be a useful tool for the dermal treatment of local inflammation.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Administration, Topical; Animals; Anti-Inflammatory Agents; beta-Cyclodextrins; Carbazoles; Cattle; Edema; Female; Freeze Drying; Humans; In Vitro Techniques; Lactic Acid; Male; Mice; Nanoparticles; Polyglycolic Acid; Polylactic Acid-Polyglycolic Acid Copolymer; Rabbits; Skin; Swine; Tetradecanoylphorbol Acetate

The enantioseparation of acidic and neutral compounds can be successfully achieved in capillary electrophoresis (CE) using dual cyclodextrin (CD) systems. This chapter describes how to separate the enantiomers of acidic or neutral substances using dual CD systems made up of a negatively charged CD derivative, i.e., sulfobutyl-β-CD (SB-β-CD) or carboxymethyl-β-CD (CM-β-CD), in combination with a neutral one, namely, heptakis(2,3,6-tri-O-methyl)-β-CD (TM-β-CD). An acidic compound (carprofen) and a weakly acidic drug (pentobarbital) were selected as model compounds.

Topics: beta-Cyclodextrins; Carbazoles; Electrophoresis, Capillary; Hydrogen-Ion Concentration; Models, Theoretical; Pentobarbital; Stereoisomerism

Some racemic nonsteroidal anti-inflammatory drugs, namely naproxen, indoprofen, ketoprofen, flurbiprofen, carprofen, cicloprofen, flunoxaprofen and suprofen were separated into their enantiomers by nano-LC. Chiral recognition was achieved adding to the mobile phase heptakis (2,3,6-tri-O-methyl)-beta-cyclodextrin (TM-beta-CD). Capillary columns of 100 microm id, packed with different RP particles were used for experiments. Effect of experimental parameters such as mobile phase composition, stationary phase type and length of packed capillary column on retention factor and chiral resolution of analytes were studied. The stationary phase type played a very important role in the enantiorecognition process. Best results in terms of highest enantioresolution factor and largest number of separated enantiomers were obtained reducing the particles size to 3 microm with RP(18) stationary phase. Most favourable mobile phase for enantiodiscrimination was obtained using relatively low concentrations of ACN (30%, v/v), 30 mM of TM-beta-CD and pH value of 3.0. The retention time of all studied enantiomers decreased by increasing the CD derivative concentration. The retention factors of selected studied compounds, specifically flurbiprofen, naproxen and suprofen, were measured employing TM-beta-CD concentrations in the range 0-40 mM. Assuming a 1:1 enantiomer/CD ratio, the apparent association constants of the studied enantiomers were calculated.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Benzoxazoles; beta-Cyclodextrins; Carbazoles; Chromatography, Liquid; Flurbiprofen; Hydrogen-Ion Concentration; Indoprofen; Ketoprofen; Methylation; Molecular Structure; Nanotechnology; Naproxen; Propionates; Stereoisomerism; Suprofen; Time Factors