Following the first successful trial of surfactant replacement therapy for preterm infants with respiratory distress syndrome (RDS) by Fujiwara in 1980, several animal-derived natural surfactants and synthetic surfactants have been developed. Synthetic surfactants were designed to overcome limitations of natural surfactants such as cost, immune reactions, and infections elicited by animal proteins contained in natural surfactants. However, first-generation synthetic surfactants that are protein-free have failed to prove their superiority over natural surfactants because they lack surfactant protein (SP). Lucinactant, a second-generation synthetic surfactant containing the SP-B analog, was better or at least as effective as the natural surfactant, suggesting that lucinactant could act an alternative to natural surfactants. Lucinactant was approved by the U. S. Food and Drug Administration in March 2012 as the fifth surfactant to treat neonatal RDS. CHF5633, a second-generation synthetic surfactant containing SP-B and SP-C analogs, was effective and safe in a human multicenter cohort study for preterm infants. Many comparative studies of natural surfactants used worldwide have reported different efficacies for different preparations. However, these differences are believed to due to site variations, not actual differences. The more important thing than the composition of the surfactant in improving outcome is the timing and mode of administration of the surfactant. Novel synthetic surfactants containing synthetic phospholipid incorporated with SP-B and SP-C analogs will potentially represent alternatives to natural surfactants in the future, while improvement of treatment modalities with less-invasive or noninvasive methods of surfactant administration will be the most important task to be resolved.
Animals ; Cohort Studies ; Humans ; Infant, Newborn ; Infant, Premature ; Pulmonary Surfactants ; Surface-Active Agents ; United States Food and Drug Administration

OBJECTIVETo study the preparation of cantharidin entrapped non-ionic surfactant vesicle (noisome)and evaluate its quality.

METHODThe niosome loaded with cantharidin was prepared using injection method by non-ionic surfactants as the carrier. An centrifugation separation method and HPLC analysis method of the cantharidin were established to detect the entrapment efficiency. The optimum preparation technology was established by a orthogonal experiment. The morphology, and particle size were studied to evaluate the preparation.

RESULTThe average size of niosomes were (209. 8 +/- 0.5) nm. The entrapment efficiency of the CTD-NS was (27.5% +/- 2.0%) and Zeta potential was (41.5 +/- 0.65) mV.

CONCLUSIONThe preparation of cantharidin noisome by TweenA and SpanB is practicable and successful. These experiments can be the basement of developing targeting drug delivery system.

Cantharidin ; administration & dosage ; chemistry ; isolation & purification ; Chromatography, High Pressure Liquid ; Drug Delivery Systems ; Liposomes ; administration & dosage ; chemistry ; Particle Size ; Surface-Active Agents ; administration & dosage

PURPOSE: Bowel cleansing is generally regarded as time-consuming and unpleasant among patients. Patients commonly state that bowel preparation provokes more discomfort than the actual colonoscopic examination. The purpose of this study was to compare two regimens of sodium phosphate (NaP) tablets versus polyethylene glycol (PEG) solution for bowel preparation in healthy Korean adults. MATERIALS AND METHODS: This was a single center, prospective, open-label, investigator-blinded, randomized, controlled-pilot study. A total of 62 healthy Korean subjects were randomly assigned to two groups (NaP vs. PEG). Efficacy, safety, and patient-related outcomes, as well as procedural parameters, were evaluated. RESULTS: Although there were no significant differences in total Ottawa bowel quality score, fluid scores and the rate of adequate bowel preparation were significantly better in the NaP group than the PEG group. Additionally, the NaP group showed better results regarding patient tolerance, satisfaction, preference, and rate of adverse events than the PEG group. Significant fluctuations in specific serum electrolytes were common and of a greater magnitude in the NaP group than the PEG group. However, these abnormalities were transient and did not result in serious complications and side effects. CONCLUSION: In this study, NaP tablets were shown to be an effective, well-tolerated, and acceptable regimen for bowel preparation. Also, our study suggests that NaP tablets may be safe and can be used as a bowel cleansing agent in healthy adults undergoing elective colonoscopy. Further multicenter, large scale studies are needed to confirm these findings.
Adult ; Asian Continental Ancestry Group ; *Colonoscopy ; Female ; Humans ; Male ; Middle Aged ; Phosphates/*administration & dosage/therapeutic use ; Pilot Projects ; Polyethylene Glycols/*administration & dosage/therapeutic use ; Prospective Studies ; Republic of Korea ; Surface-Active Agents/*administration & dosage ; Tablets ; Therapeutic Irrigation/*methods

An Aersol-OT (AOT) included microemulsion containing fluorouracil was prepared by using appropriate proportion of oil, co-surfactant and water for increasing the drug transdermal delivery ability. According to the area of microemulsion basing on the pseudo-tertiary phase diagrams, the optimum formulation was screened initially. And the permeation flux of fluorouracil across excised mice skin was determined in vitro using Franz diffusion cell to optimize the formulation further. The effect of the kind of co-surfactant, the content of water, the content of mixed surfactant, the mass ratio of surfactant/cosurfactant (Km) and the drug load on skin permeation of fluorouracil were evaluated. The optimum formulation was composed of 0.5% (w/v) fluorouracil, 30% water, 20% mix-surfactant (AOT/Tween 85, Km = 2) and 49.5% oil (IPM). The cumulative amount permeated of fluorouracil in 12 hour was 1 355.5 microg x cm(-2), 19.1 folds and 7 folds more than 0.5% fluorouracil aqueous solution and 2.5% (w/w) fluorouracil cream, respectively. The permeation of this microemulsion accorded with first-order model. The water/AOT/Tween 85/IPM microemulsion system promoted the permeation of fluorouracil greatly, which may be a promising vehicle for the transdermal delivery of fluorouracil and other hydrophilic drug.
Administration, Cutaneous ; Animals ; Antimetabolites, Antineoplastic ; administration & dosage ; pharmacokinetics ; Drug Carriers ; Drug Delivery Systems ; methods ; Emulsions ; Fluorouracil ; administration & dosage ; pharmacokinetics ; Male ; Mice ; Myristates ; chemistry ; Oils ; chemistry ; Polysorbates ; chemistry ; Skin Absorption ; Succinates ; chemistry ; Surface-Active Agents ; chemistry ; Water ; chemistry

OBJECTIVETo explore the effects of SDS, PBS re-dissolvent solutions on fluorescence values of radioallergosorbent test (RAST) inhibition.

METHODSDermatophagoides pterronyssinus allergen immunoCAP and UniCAP 100 System were used. The Sera Pool consisted of 20 Dermatophagoides pterronyssinus allergic patients sera, their specific IgE fluorescence values were between 12505 and 24776.

RESULTSFluorescence value percentages decreased: 62.9%, 54.1%, 43.5%, 6.7%, 3.7%, 2.6%, 2.2%, and 1.4% respectively, when SDS concentrations were at 2%, 1%, 0.5%, 0.25%, 0.1%, 0.05%, 0.025%, and 0.01%. Fluorescence values decreased more than 5% with SDS concentrations equal to 0.25% or higher. PBS in 0.1 and 0.01 mol/L concentrations decreased fluorescence values 2.9% and 0.9% respectively.

CONCLUSIONSSDS is a commonly used surfactants in allergen extract and re-dissolvent prepared allergen precipitation for RAST inhibition. Thus effects of surfactants (e.g. SDS) upon the RAST inhibition tests must be considered when they were used as re-dissolvent agents to improve protein resolution in RAST inhibition.

Allergens ; Dermatophagoides pteronyssinus ; immunology ; Dose-Response Relationship, Drug ; Fluorescence ; Humans ; Immunoglobulin E ; blood ; immunology ; Phosphates ; administration & dosage ; pharmacology ; Radioallergosorbent Test ; methods ; Sodium Dodecyl Sulfate ; administration & dosage ; pharmacology ; Solutions ; Surface-Active Agents ; administration & dosage ; pharmacology

AIMTo study the diffusion behaviors of drugs in thermosensitive in situ gels, and provide valuable information for designing such delivery systems.

METHODSA free diffusion model was used to evaluate the effects of concentration, the property of drugs, as well as the gel compositions on the diffusivity of drugs.

RESULTSDrug transport through the aqueous channels of the gel followed Fickian mechanism, and no significant influence on the diffusivity was observed when the drug concentration was lowered from 5% to 0.25%. The diffusion coefficients of propranolol, timolol maleate, and salbutamol sulfate were 0.91, 1.32, and 3.30 x 10(-6) cm2 x s(-1), respectively. The flux of hydrophilic drug was 3.6 fold faster than that of the lipophilic one implied the latter partitioned into the hydrophobic micellar core, and consequently the diffusion was retarded. The diffusivity was decreased with increased poloxamer and sodium hyaluronate concentration, due to the distorted aqueous channels and higher microviscosity.

CONCLUSIONThe result suggested that sustained release could be achieved for the thermosensitive in situ gel by incorporating lipophilic drug or increasing polymer concentration.

Albuterol ; administration & dosage ; chemistry ; Delayed-Action Preparations ; Diffusion ; Drug Carriers ; chemistry ; Drug Delivery Systems ; Gels ; Poloxamer ; chemistry ; Propranolol ; administration & dosage ; chemistry ; Surface-Active Agents ; chemistry ; Timolol ; administration & dosage ; chemistry

BACKGROUNDCapsule endoscopy is a novel non-invasive method for visualization of the entire small bowel. The diagnostic yield of capsule endoscopy depends on the quality of visualization of the small bowel mucosa and its complete passage through the small bowel. To date, there is no standardized protocol for bowel preparation before capsule endoscopy. The addition of simethicone in the bowel preparation for the purpose of reducing air bubbles in the intestinal lumen had only been studied by a few investigators.

METHODSSixty-four participants were randomly divided into two groups to receive a bowel preparation of polyethylene glycol (PEG) solution (Group 1) and both PEG solution and simethicone (Group 2). The PEG solution and simethicone were taken the night before and 20 min prior to capsule endoscopy, respectively. Frames taken in the small intestine were examined and scored for luminal bubbles by two professional capsule endoscopists. Gastric emptying time and small bowel transit time were also recorded.

RESULTSSimethicone significantly reduced luminal bubbles both in the proximal and distal small intestines. The mean time proportions with slight bubbles in the proximal and distal intestines in Group 2 were 97.1% and 99.0%, respectively, compared with 67.2% (P<0.001) and 68.8% (P<0.001) in Group 1. Simethicone had no effect on mean gastric emptying time, 32.08 min in Group 2 compared with 30.88 min in Group 1 (P=0.868), but it did increase mean small intestinal transit time from 227.28 to 281.84 min (P=0.003).

CONCLUSIONBowel preparation with both PEG and simethicone significantly reduced bubbles in the intestinal lumen and improved the visualization of the small bowel by capsule endoscopy without any side effects observed.

Adult ; Aged ; Capsule Endoscopes ; Female ; Humans ; Image Enhancement ; methods ; Intestine, Small ; cytology ; drug effects ; Male ; Middle Aged ; Premedication ; methods ; Simethicone ; administration & dosage ; Surface-Active Agents ; administration & dosage ; Young Adult

To screen a new poorly water-soluble antischistosomal drug QH917 self-microemulsifying drug delivery system which has steady release in vitro and absorption in situ separately. The formulation was optimized using central composite design-response surface methodology. Independent variables were oil content (%) and the weight ratio of surfactant and cosurfactant (Km), while response variables were self-microemulsifying time (t), mean particle size (PS) and polydispersity index (PI). The effects of ionic strength, food, pH, rotation speed and medium volume on drug release of the optimized formulation were evaluated under conditions simulating in vivo physiological situations. The absorption of the optimized formulation was studied using in situ intestinal permeability technique of rats. The optimized formulation was as follows: the content of media chain triglyceride (MCT) was 30%-34% (w/w); and the weight ratio of surfactant polyoxyl 40 hydrogenated castor oil (Cremophor RH40) and co-surfactant ethanol was 4.8-5.2. Release of QH917 from the optimized formulation was nearly unaffected by ionic strength, food, pH, rotation speed and medium volume. There was no marked difference of the absorption rate between rats with and without ligated bile duct in rat intestinal permeability technique. Inter-individual variability in absorption of the optimized formulation was negligible. Central composite design-response surface methodology is an efficient approach for optimizing formulations of self-microemulsifying drug delivery system; drug release in vitro and absorption behavior in situ of the optimized formulation is steady.
Animals ; Artemisinins ; administration & dosage ; pharmacokinetics ; Drug Delivery Systems ; methods ; Emulsions ; Intestinal Absorption ; Male ; Particle Size ; Random Allocation ; Rats ; Rats, Wistar ; Schistosomicides ; administration & dosage ; pharmacokinetics ; Solubility ; Surface-Active Agents ; chemistry ; Triglycerides ; chemistry

OBJECTIVETo screen the optimum formulation and prepare O/W sinomenine microemulsion and investigate its in vitro transdermal delivery ability.

METHODThe microemulsions were prepared with the formulation containing oleic acid-tween 80-dehydrated alcohol-water by the pseudo-ternary phase diagram. The permeation flux of sinomenine was determined in vitro by Franz diffusion cell fitted with rat skin. The sinomenine was determined by HPLC. The transdermal characteristics of sinomenine microemulsion were compared with that of sinomenine gels.

RESULTThe steady state flux of sinomenine microemulsion was significantly higher than that of sinomenine gels. The average permeation rate of sinomenine microemulsion was 116. 44 microg x cm(-2) x h(-1) in vitro.

CONCLUSIONThese results indicated that the studied microemulsion system with high permeation rate may be a potential vehicle for the transdermal delivery of sinomenine.

Administration, Cutaneous ; Animals ; Drug Compounding ; methods ; Drug Delivery Systems ; Emulsions ; Ethanol ; chemistry ; Male ; Morphinans ; administration & dosage ; isolation & purification ; pharmacokinetics ; Oleic Acid ; chemistry ; Particle Size ; Plants, Medicinal ; chemistry ; Polysorbates ; chemistry ; Rats ; Sinomenium ; chemistry ; Skin ; metabolism ; Skin Absorption ; Surface-Active Agents ; chemistry

AIMTo evaluate the effects of surfactants on the pharmacokinetics and distribution in rats after intravenous administration of SOD liposomes.

METHODSThe liposomes were prepared by reverse phase evaporation method. The activity of SOD was assayed by method of xanthine oxidase.

RESULTSThe T1/2 of SOD solution, common SOD liposome, SOD liposomes modified by DSPE-PEG2000 and Tween 80 were 0.25, 0.34, 0.66 and 0.41 h, respectively; AUC were 12.48, 24.66, 41.16 and 33.02 microg x h x mL(-1), respectively. Compared with the common liposome, the liposomes modified by DSPE-PEG and Tween 80 decreased the content of SOD in liver and spleen, but increased in brain.

CONCLUSIONThe three kinds of liposomes could increase T1/2 and AUC in some extent, especially in PEG-L group. Tween-L could increase the SOD content in brain, and PEG-L could decrease the SOD content in the liver and spleen compared with the common liposome.

Animals ; Area Under Curve ; Brain ; enzymology ; Injections, Intravenous ; Liposomes ; Liver ; enzymology ; Male ; Polysorbates ; pharmacology ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Spleen ; enzymology ; Superoxide Dismutase ; administration & dosage ; pharmacokinetics ; Surface-Active Agents ; pharmacology ; Tissue Distribution