title: Usefulness of liquid-crystal oral formulations to enhance the bioavailability and skin tissue targeting of p-amino benzoic acid as a model compound.
abstract: Topical formulations are not always suitable to deliver active ingredients to large areas of skin. Thus, in this study, we aimed to develop an oral formulation for skin tissue targeting with a high bioavailability using liquid crystal (LC) dispersions comprising cubosomes of a mal-absorptive model compound, p-amino benzoic acid (PABA), which is an active element in cosmeceuticals, dietary supplements and skin disorder medicines. The bioavailability and skin concentration of PABA were investigated after oral administration in rats. The effect of the remaining amount of the LC formulation in the stomach on the pharmacokinetic profiles of orally administered PABA was evaluated. The skin permeation and concentration of PABA were also investigated using an in vitro permeation experiment. As a result, the bioavailability of PABA was significantly improved by administration of PABA-LC formulations compared with PABA solution alone, although the effect was greatly influenced by the type of LC-forming lipids. The in vitro skin permeation study showed that the PABA concentration in the skin when applied from the dermis side was higher than when applied from the epidermis side. These findings suggested that oral administration advantageously supports skin targeting, and oral LC formulations could be a promising material in cosmeceutical, dietary and clinical fields.
authors.affiliation: Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
authors.forename: Wesam R
authors.initials: WR
authors.lastname: Kadhum
authors.affiliation: Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
authors.forename: Takeshi
authors.initials: T
authors.lastname: Oshizaka
authors.affiliation: Farnex Incorporated, Yokohama-shi, Kanagawa, Japan.
authors.forename: Hijikuro
authors.initials: H
authors.lastname: Ichiro
authors.affiliation: Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Todo
authors.affiliation: Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan. Electronic address: sugib@josai.ac.jp.
authors.forename: Kenji
authors.initials: K
authors.lastname: Sugibayashi
mesh_terms: D010129:4-Aminobenzoic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D016503:Drug Delivery Systems; D005989:Glycerides / Q000737:chemistry; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012867:Skin
chemical_list: D005989:Glycerides; D010129:4-Aminobenzoic Acid
keywords: Bioavailability; Liquid crystals; Oral formulation; PABA; Skin tissue targeting