Effects of HPE-101, a skin penetration enhancer, on human erythrocyte membranes.

The primary aim of this study was to investigate the skin permeation-enhancing mechanism of HPE-101 using erythrocyte ghost cells prepared from human whole blood as a biomembrane model. The extent of hemolysis of erythrocytes induced by HPE-101 was measured using a spectrophotometer at 540nm. The effect of HPE-101 on lipid fluidity was examined by observing the change of intramolecular excimer formation and fluorescence polarization using an intramolecular probe (1,3-bis(pyrene) propane) and a lipid probe (1,6-diphenyl 1,3,5-hexatriene), respectively.

Effect of glycyrrhizic acid on protein binding of diltiazem, verapamil, and nifedipine.

The effects of glycyrrhizic acid (GLZ) on protein binding of diltiazem, verapamil, and nifedipine were investigated. Protein binding studies (human serum, human serum albumin (HSA) and alpha1-acid glycoprotein (AAG)) were conducted using the equilibrium dialysis method with and without addition of GLZ. The binding parameters, such as the number of moles of bound drug per mole of protein, the number of binding sites per protein molecule, and the association constant, were estimated using the Scatchard plot.

Serially passaged human nasal epithelial cell monolayer for in vitro drug transport studies.

Purpose: To evaluate the feasibility of using a serially passaged culture of human nasal epithelial cell monolayers on a permeable support for in vitro drug transport studies. The optimum conditions for passaged culture as well as the correlation between the transepithelial electrical resistance (TEER) value and drug permeability (Papp) were evaluated.

Methods: Fresh human nasal epithelial cells were collected from normal inferior turbinates and were subcultured repeatedly in serum-free bronchial epithelial cell growth media (BEGM) in petri dishes.

In-vitro and in-vivo antibacterial activity evaluation of a polyurethane matrix.

Various in-vitro and in-vivo methods for evaluation of the duration of antibacterial activity were compared using a controlled-release polyurethane matrix developed for the prevention of surface bacterial adhesion and growth. Cefadroxil was incorporated into this polyurethane matrix by a solvent casting method before the matrix was coated with polyurethane in tetrahydrofuran solution. The release of cefadroxil from the matrix into distilled water at 37 degrees C was measured by HPLC.

Synthesis and evaluation of Ketorolac ester prodrugs for transdermal delivery.

Alkyl esters of ketorolac were synthesized as potential prodrugs for transdermal delivery and evaluated to determine the relationship between their skin permeation characteristics and their physicochemical properties. Solubility of the prodrugs in various vehicles was determined at room temperature while lipophilicity was obtained as 1-octanol/water partition coefficients (logP) and capacity factors (k') using HPLC. Metabolism of the prodrugs to ketorolac was studied both in rat skin homogenate and in plasma.

Development of a novel soft hydrogel for the transdermal delivery of testosterone.

A soft hydrogel formulation for the transdermal delivery of testosterone (TS) was developed, and the effect of various skin-permeation enhancers was studied in vitro and in vivo. Testosterone was incorporated into a polyvinyl alcohol (PVA)-based soft hydrogel with polyisobutylene (PIB) and various skin-permeation enhancers (dodecylamine, HPE101, oleic acid, or lauric acid). In vitro rat-skin permeation of TS from the soft hydrogel was investigated using Keshary-Chien diffusion cells for 24 hr at 37 degrees C.

In vitro evaluation of patch formulations for topical delivery of gentisic acid in rats.

Gentisic acid (GA) is used in cosmetics as a skin-whitening agent for the treatment of skin pigmentary disorders by influencing the synthesis of melanin through inhibition of melanosomal tyrosinase activity. In order to achieve effective topical delivery of GA to the active site in the skin, a matrix-type transdermal delivery system was developed. The in vitro skin permeation as well as skin deposition of GA was studied in rats.

The effects of pressure-sensitive adhesives and solubilizers on the skin permeation of testosterone from a matrix-type transdermal delivery system.

Matrix-type transdermal delivery systems of testosterone (TS) were formulated with three different pressure-sensitive adhesives (PSA). The effects of PSA, skin permeation enhancers, and solubilizers on the rat skin permeation rate of TS were systematically investigated. Without a solubilizer, the skin permeation rate of TS reached its maximum value when only 2% of TS was loaded in the matrix and the crystal formation in the matrix was very rapid and severe.

Proteome of Oriental ginseng Panax ginseng C. A. Meyer and the potential to use it as an identification tool.

Oriental ginseng (Panax ginseng C. A. Meyer) and American ginseng (Panax quinquefolius) are two widely used valuable traditional Chinese medicines (TCM).

Physicochemical properties of CWJ-a-5, a new antitumor 3-arylisoquinoline derivative.

The compound CWJ-a-5 [1-(4-methylpiperazinyl)-3-phenylisoquinoline hydrochloride] is a novel 3-arylisoquinoline derivative which has exhibited potent antitumor activity. As part of an effort to develop a useful formulation for clinical evaluation of this compound, the aqueous stability of CWJ-a-5 as a function of pH, ionic strength, and temperature, as well as its various physicochemical properties, have been examined. The pKa value obtained by potentiometric titration in methanol-water mixtures was 3.

Anthropometric study of alar cartilage in Asians.

Measurements of 52 alar cartilages in 26 Koreans were obtained for an anthropometric study during primary open-approach rhinoplasties. The lateral crura were found most commonly to be concave, exhibited in 40% of the male patients and in 50% of the female patients. The medial crura were most often straight, found in 56% of the male patients and in 46% of the female patients.