ABSTRACT
Triprolidine-containing matrix was fabricated with poly(4-methyl-1-pentene) (TPX) polymer to control the release of the drug. Effect of penetration enhancer and stripping of skin on the permeation of triprolidine through the excised mouse skin was studied. Penetrating enhancers showed the increased flux probably due to the enhancing effect on the skin barrier, the stratum corneum. Among enhancers used such as glycols, fatty acids and non-ionic surfactants, polyoxyethylene-2-oleyl ether showed the best enhancement. The permeability of triprolidine was markedly increased with stripping the mouse skin to remove the stratum corneum, which acts as a barrier of skin permeation. For the controlling delivery of triprolidine, the TPX matrix containing permeation enhancer could be developed.
Subject(s)
Drug Delivery Systems/methods , Membranes, Artificial , Polyenes/administration & dosage , Polymers/administration & dosage , Triprolidine/administration & dosage , Administration, Cutaneous , Animals , Anti-Allergic Agents/administration & dosage , Anti-Allergic Agents/pharmacokinetics , Male , Mice , Mice, Inbred ICR , Polyenes/pharmacokinetics , Polymers/pharmacokinetics , Skin Absorption/drug effects , Skin Absorption/physiology , Triprolidine/pharmacokineticsABSTRACT
Oral administration of triprolidine, antihistamines, may cause many adverse effects such as dry mouth, sedation, dizziness and transdermal drug delivery was considered. Poly(4-methyl-1-pentene) (TPX) membrane, which has good mechanical strength was fabricated by the casting method. TPX membranes was a little brittle and the plasticizers was added for preparing the membranes. The present study was carried out to evaluate the possibility of using the polymer TPX membrane as a controlling membrane and further develop a TPX matrix system for transdermal delivery of triprolidine. The effects of molecular weights of TPX, plasticizers, polyethylene glycol (PEG) 400, drug concentration, and temperature on drug release were studied. The solubility of triprolidine increased exponentially as the increased volume fraction of PEG 400 in saline, and the rate of permeation through TPX membrane was proportional to PEG 400 volume fraction. The release rate of drug from the TPX matrix increased with increased temperature and drug concentration. Among the plasticizers used such as alkyl citrates, phthalates and sebacate, tetra ethyl citrate (TEC) showed the best enhancing effects. Enhancement factor of TEC was 3.76 from TPX matrix at 37 degrees C. The transdermal controlled release of triprolidine system could be developed using the TPX polymer including the plasticizer.
