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Increased Hydrophilicity (increased + hydrophilicity)
Selected AbstractsEffect of lipid bilayer alteration on transdermal delivery of a high-molecular-weight and lipophilic drug: Studies with paclitaxelJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 9 2004Ramesh Panchagnula Abstract Skin forms an excellent barrier against drug permeation, due to the rigid lamellar structure of the stratum corneum (SC) lipids. Poor permeability of drugs can be enhanced through alteration in partition and diffusion coefficients, or concentration gradient of drug with an appropriate choice of solvent system, along with penetration enhancers. The aim of the current investigation was to assess applicability of lipid bilayer alteration by fatty acids and terpenes toward the permeation enhancement of a high-molecular-weight, lipophilic drug, paclitaxel (PCL) through rat skin. From among the fatty acids studied using ethanol/isopropyl myristate (1:1) vehicle, no significant enhancement in flux of PCL was observed (p,>,0.05). In the case of cis mono and polyunsaturated fatty acids lag time was found to be similar to control (p,>,0.05). This suggests that the permeation of a high-molecular-weight, lipophilic drug may not be enhanced by the alteration of the lipid bilayer, or the main barrier to permeation could lie in lower hydrophilic layers of skin. A significant increase in lag time was observed with trans unsaturated fatty acids unlike the cis isomers, and this was explained on the basis of conformation and preferential partitioning of fatty acids into skin. From among the terpenes, flux of PCL with cineole was significantly different from other studied terpenes and controls, and after treatment with menthol and menthone permeability was found to be reduced. Menthol and menthone cause loosening of the SC lipid bilayer due to breaking of hydrogen bonding between ceramides, resulting in penetration of water into the lipids of the SC lipid bilayer that leads to creation of new aqueous channels and is responsible for increased hydrophilicity of SC. This increased hydrophilicity of the SC bilayer might have resulted in unfavorable conditions for ethanol/isopropyl myristate (1:1) along with PCL to penetrate into skin, therefore permeability was reduced. The findings of this study suggest that the permeation of a high-molecular-weight and lipophilic drug cannot be enhanced through bilayer alteration by penetration enhancers, and alteration in partitioning of drug into skin could be a feasible mode to enhance the permeation of drug. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 93:2177,2183, 2004 [source] Biodegradable comb polyesters containing polyelectrolyte backbones facilitate the preparation of nanoparticles with defined surface structure and bioadhesive properties,POLYMERS FOR ADVANCED TECHNOLOGIES, Issue 10-12 2002A. Breitenbach Abstract A major challenge in oral peptide and protein delivery remains the search for suitable carrier systems. Therefore, a new concept was investigated combining a modified three-dimensional architecture, increased hydrophilicity of poly(lactic- co -glycolic acid) (PLGA) and charged groups in a single polymer. Biodegradable comb PLGA were synthesized by grafting short PLGA chains onto different poly(vinyl alcohol) (PVA) based backbone polyols, poly(2-sulfobutyl-vinyl alcohol) and poly(diethylaminoethyl-vinyl alcohol). The polyelectrolyte backbones were obtained by etherification of PVA with charge-containing pendent groups. The comb polymer structure could be confirmed by nuclear magnetic resonance, infrared spectroscopy, differential scanning calorimetry, elemental analysis and measurement of intrinsic viscosity. Nanoparticles (NP), as potential mucosal carriers systems, were prepared by controlled precipitation and investigated as a function of polymer composition. The amphiphilic character and the three-dimensional architecture of the novel polyesters allowed the preparation of small nanoparticles even without the use of surfactants. Surface NMR, surface charge and hydrophobicity determination indicate a core,corona-like NP structure, especially in the case of negatively charged polyesters. A structural model is proposed for the NP with an inner polyester core and an outer charged-groups-containing surface, depending on polymer composition and backbone charge density. The higher the polymer backbone charge density, the more pronounced its influence on the nanoparticle surface properties. The possibility of preparing NP without the use of a surfactant, as well as of designing the NP surface characteristics by polymer backbone charge density and polymer hydrophilic,hydrophobic balance, will be a major advantage in protein adsorption, bioadhesion and organ distribution. This makes these biodegradable polymers promising candidates for colloidal protein and peptide delivery. Copyright © 2003 John Wiley & Sons, Ltd. [source] Enhanced Chondrogenic Responses of Human Articular Chondrocytes Onto Silk Fibroin/Wool Keratose Scaffolds Treated With Microwave-Induced Argon PlasmaARTIFICIAL ORGANS, Issue 5 2010Young Woo Cheon Abstract Silk fibroin (SF) is a natural, degradable, fibrous protein that is biocompatible, is easily processed, and possesses unique mechanical properties. Another natural material, wool keratose (WK), is a soluble derivative of wool keratin, containing amino acid sequences that induce cell adhesion. Here, we blended SF and WK to improve the poor electrospinability of WK and increase the adhesiveness of SF. We hypothesized that microwave-induced argon plasma treatment would improve chondrogenic cell growth and cartilage-specific extracellular matrix formation on a three-dimensional SF/WK scaffold. After argon plasma treatment, static water contact angle measurement revealed increased hydrophilicity of the SF/WK scaffold, and scanning electron microscopy showed that treated SF/WK scaffolds had deeper and more cylindrical pores than nontreated scaffolds. Attachment and proliferation of neonatal human knee articular chondrocytes on treated SF/WK scaffolds increased significantly, followed by increased glycosaminoglycan synthesis. Our results suggest that microwave-induced, plasma-treated SF/WK scaffolds have potential in cartilage tissue engineering. [source] A novel characteristic of porous titanium oxide implantsCLINICAL ORAL IMPLANTS RESEARCH, Issue 6 2007Takashi Sawase Abstract Objective: The anatase form of titanium dioxide (TiO2) is one of the most common crystalline forms of TiO2 and is normally produced by oxidation of titanium via thermal oxidation or anodizing. This crystalline form exhibits photocatalytic activity when it is irradiated with ultraviolet A (UVA) light. The aim of the current study was to analyze the crystal structure of anodic-oxidized TiUnite® implants and to confirm the photocatalytic properties in vitro and in vivo. Material and methods: Cross-sectional observations by transmission electron microscopy were used to determine the surface crystal structure on the TiUnite implant. Subsequently, photocatalytic activity was confirmed by degradation of methylene blue, and hydrophilicity was measured based on the water contact angle. Furthermore, the in vivo effects of the photocatalytic activity of this compound were investigated. Results: An amorphous layer that was about 10 ,m thick was observed on the TiUnite implant surface. In the amorphous layer, the anatase form of the crystalline TiO2 was identified. Photocatalytic activity was clearly demonstrated by the bleaching effect of methylene blue under UVA illumination. The contact angle decreased from 44° to 11° after UVA illumination. Although these data suggest increased hydrophilicity for the TiUnite implant, the bone-to-metal contact at 4 weeks was not influenced. Conclusion: The anodic-oxidized TiUnite implant has inherent photocatalytic activity. UVA illumination increases the surface hydrophilicity of the implant. However, this increase in hydrophilicity does not improve bone apposition to the implant surface at 4 weeks. [source] | ||||||||||