Absorption of hyaluronan applied to the surface of intact skin. (1/77)

Hyaluronan has recently been introduced as a vehicle for topical application of drugs to the skin. We sought to determine whether hyaluronan acts solely as a hydrophilic reservoir on the surface of intact skin or might partly penetrate it. Drug-free hyaluronan gels were applied to the intact skin of hairless mice and human forearm in situ, with and without [3H] hyaluronan. [3H]hyaluronan was shown by autoradiography to disseminate through all layers of intact skin in mouse and human, reaching the dermis within 30 min of application in mice. Cellular uptake of [3H]hyaluronan was observed in the deeper layers of epidermis, dermis, and in lymphatic endothelium. Absorption through skin was confirmed in mice by chromatographic analysis of blood, urine, and extracts from skin and liver, which identified 3H as intact hyaluronan and its metabolites, free acetate and water. Hyaluronan absorption was similarly demonstrated without polyethylene glycol, which is usually included in the topical formulation. [3H]hyaluronan absorption was not restricted to its smaller polymers as demonstrated by the recovery of polymers of (360-400 kDa) from both blood and skin. This finding suggests that its passage through epidermis does not rely on passive diffusion but may be facilitated by active transport. This study establishes that hyaluronan is absorbed from the surface of the skin and passes rapidly through epidermis, which may allow associated drugs to be carried in relatively high concentration at least as far as the deeper layers of the dermis.  (+info)

Rapid determination of the amount of cetylpyridinium chloride bound by bacteria. (2/77)

A modification of the Colowick and Womack procedure for measuring ligand binding by macromolecules is described for drug binding by bacteria. This technique is based on the determination of drug concentration in the dialysate from a bacteria-drug mixture at equilibrium. The dialysis cell of the original procedure was replaced by a Minibeaker (Bio-Rad), which has a larger membrane surface area, and the dialysate was continuously monitored with a spectrophotometer equipped with a flow cell. With this system, only 3 min was required to determine the amount of cetylpyridinium chloride bound by Escherichia coli K-12 strain P678. Possible applications of the technique are discussed.  (+info)

Testing a degradable topical varnish of cetylpyridinium chloride in an experimental dental biofilm model. (3/77)

Dental biofilms are highly associated with the development of dental caries. Novel drug delivery systems are being developed in order to eliminate cariogenic bacteria from the dental biofilms. We formulated two degradable sustained release varnishes, based on acrylic resin, with cetylpyridinium chloride (CPC) as the active agent. These formulations were tested in a dental biofilm model. The retention of CPC in the biofilm was dependent upon the pharmaceutical additives of the varnish. Both varnishes decreased bacterial adhesion, while also demonstrating marked antibacterial properties against the bacteria in the biofilm.  (+info)

A novel pharmacological probe links the amiloride-insensitive NaCl, KCl, and NH(4)Cl chorda tympani taste responses. (4/77)

Chorda tympani taste nerve responses to NaCl can be dissected pharmacologically into amiloride-sensitive and -insensitive components. It is now established that the amiloride-sensitive, epithelial sodium channel acts as a sodium-specific ion detector in taste receptor cells (TRCs). Much less is known regarding the cellular origin of the amiloride-insensitive component, but its anion dependence indicates an important role for paracellular shunts in the determination of its magnitude. However, this has not precluded the possibility that undetected apical membrane ion pathways in TRCs may also contribute to its origin. Progress toward making such a determination has suffered from lack of a pharmacological probe for an apical amiloride-insensitive taste pathway. We present data here showing that, depending on the concentration used, cetylpyridinium chloride (CPC) can either enhance or inhibit the amiloride-insensitive response to NaCl. The CPC concentration giving maximal enhancement was 250 microM. At 2 mM, CPC inhibited the entire amiloride-insensitive part of the NaCl response. The NaCl response is, therefore, composed entirely of amiloride- and CPC-sensitive components. The magnitude of the maximally enhanced CPC-sensitive component varied with the NaCl concentration and was half-maximal at [NaCl] = 62 +/- 11 (SE) mM. This was significantly less than the corresponding parameter for the amiloride-sensitive component (268 +/- 71 mM). CPC had similar effects on KCl and NH(4)Cl responses except that in these cases, after inhibition with 2 mM CPC, a significant CPC-insensitive response remained. CPC (2 mM) inhibited intracellular acidification of TRCs due to apically presented NH(4)Cl, suggesting that CPC acts on an apical membrane nonselective cation pathway.  (+info)

PVC matrix membrane sensor for potentiometric determination of cetylpyridinium chloride. (5/77)

A novel cetylpyridinium chloride-selective membrane sensor consisting of cetylpyridinium-ferric thiocyanate ion pairs dispersed in a PVC matrix placticized with dioctylphthalate is described. The electrode shows a stable, near-Nernstian response for 1 x 10(-3)-1 x 10(-6) mol l-1 cetylpyridinium chloride (CPC) at 25 degrees C over the pH range 1-6 with a cationic slope of 57.5 +/- 0.4. The lower detection limit is 8 x 10(-7) mol l-1 and the response time is 30-60 s. Selectivity coefficients for CPC relative to a number of interfering substances were investigated. There is negligible interference from many cations, anions and pharmaceutical excipients; however, cetyltrimethylammonim bromide (CTMAB) interfered significantly. The determination of 0.5-350 micrograms/ml of CPC in aqueous solutions shows an average recovery of 98.5% and a mean relative standard deviation of 1.6% at 56.0 micrograms/ml. The direct determination of CPC in Ezafluor mouthwash gave results that compare favorably with those obtained by the British Pharmacopoeia method. Precipitation titrations involving CPC as titrant are monitored with a CP sensor. The CP electrode has been utilized as an end point indicator electrode for the determination of anionic surfactants in some commercial detergents.  (+info)

Mucopolysaccharides associated with nuclei of cultured mammalian cells. (6/77)

Mucopolysaccharides have been isolated, fractionated, and characterized from the nuclei of cultured B16 mouse melanoma cells grown in the presence of (3-H)-glucosamine and (35-S)sulfate. Digestion of the nuclei with DNase followed by Pronase gave a mixture of complex carbohydrates from which the mucopolysaccharides were isolated by precipitation with cetylpyridinium chloride. After fractionation by differential salt extraction and chromatography on controlled pore glass bead columns, the components were identified by chemical and enzymatic methods. The major polysaccharide components were a family of high-molecular-weight chondroitin sulfates with different degrees of sulfation; a minor component has been characterized as heparan sulfate.  (+info)

Cetyl-pyridinium chloride is useful for isolation of Mycobacterium tuberculosis from sputa subjected to long-term storage. (7/77)

Recovery of Mycobacterium tuberculosis from sputa treated with cetyl-pyridinium chloride (CPC) and stored for 20 +/- 9 days was significantly higher than that from sputa that were untreated and processed by the N-acetyl-L-cisteine-NaOH method. Addition of CPC is useful for isolation of M. tuberculosis from sputa subjected to long-term storage received from remote areas of the world.  (+info)

Effects of cetylpyridinium chloride resistance and treatment on fluconazole activity versus Candida albicans. (8/77)

Mouthwash antiseptic cetylpyridinium chloride (CPC) has potent activity against Candida albicans; however, two of five azole-resistant strains showed reduced CPC susceptibility. To further examine the potential for cross-resistance, CPC-resistant mutants were selected in vitro and their fluconazole susceptibility was tested. MICs were unchanged, and trailing growth generally decreased. With CPC-fluconazole combinations, both antagonism and synergism were observed, which can be explained, in part, by CDR1-CDR2 multidrug transporter upregulation.  (+info)