ABSTRACT
Topical microemulsion of capsaicin without surfactant was developed in this study. In these systems, the oil phase was benzyl alcohol, and the cosurfactant was propylene glycol and ethanol. The drop-size of the systems was measured by dynamic light scattering method in order to distinguish true solution from microemulsion. The transdermal performance of the microemulsions was evaluated in vitro by Franz diffusion cells fitted with rat skins. The results showed the drop-size of the microemulsions without surfactant was smaller than that of the systems with Tween 80 and the permeation rate of capsaicin decreased as the content of Tween 80 increased. In the system composed of water, benzyl alcohol and propylene glycol, the permeation rate increased with the enhancement of benzyl alcohol and water. But water content had little effect on the permeation rate in the microemulsions with ethanol as cosurfactant.
Subject(s)
Capsaicin/pharmacokinetics , Animals , Benzyl Alcohol/chemistry , Benzyl Alcohol/pharmacology , Capsaicin/administration & dosage , Capsaicin/chemistry , Chemistry, Pharmaceutical , Chromatography, High Pressure Liquid , Drug Stability , Emulsions , Ethanol/pharmacology , In Vitro Techniques , Male , Particle Size , Pharmaceutic Aids/chemistry , Pharmaceutic Aids/pharmacology , Rats , Rats, Sprague-Dawley , Skin Absorption/drug effects , Surface Tension , Surface-Active AgentsABSTRACT
The crystal structure of the title compound, C(9)H(20)NO(+)·Cl(-)·0.33(H(3)O(+)·Cl(-)), is composed of 4-hydr-oxy-2,2,6,6-tetra-methyl-piperidinium cations, hydroxonium cations and chloride anions, which are connected via O-Hâ¯O, O-Hâ¯Cl and N-Hâ¯Cl hydrogen bonding. The 4-hydr-oxy-2,2,6,6-tetra-methyl-piperidinium cation and one of the two crystallographically independent chloride anions are located on a mirror plane. The hydroxonium cation is located on a threefold axis and the second crystallographically independent chloride anion is located on a sixfold rotoinversion axis. Due to symmetry, the hydroxonium cation is disordered over two positions.