Application of Eudragit RS to thermo-sensitive drug delivery systems. II. Effect of temperature on drug permeability through membrane consisting of Eudragit RS/PEG 400 blend polymers

• Published in: Journal of controlled release Vol. 102; no. 1; pp. 49 - 57
• Main Authors: FUJIMORI, Junya, YOSHIHASHI, Yasuo, YONEMOCHI, Etsuo, TERADA, Katsuhide
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier 20.01.2005
• Subjects: Acrylic Resins - administration & dosage; Acrylic Resins - pharmacokinetics; Biological and medical sciences; Drug Delivery Systems - methods; General pharmacology; Medical sciences; Membranes, Artificial; Permeability - drug effects; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polyethylene Glycols - administration & dosage; Polyethylene Glycols - pharmacokinetics; Polymers - administration & dosage; Polymers - pharmacokinetics; Temperature; Drug; Delivery system; Pharmaceutical technology; Controlled release form; Control release polymer; Temperature effect; Thermo-sensitive polymer; Permeability; Glass transition temperature; Eudragit; Ethylene oxide polymer; Polyethylene glycol; Dosage form; Membrane; Controlled release
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2004.09.027

The Eudragit RS and polyethylene glycol 400 (PEG 400) blend polymer (EPG) membranes were prepared by the solvent casting method to pioneer a novel application of Eudragit RS to a thermo-sensitive material. The EPG membranes containing 2.5-10% PEG 400 (2.5-10% EPG) showed the glass transition temperatures (Tgs) around the body temperature (32-42 degrees C). Drug permeation studies through the EPG membranes were carried out using acetaminophen (AAP) and aminopyrine (AMP) as the model drugs. The permeability of AAP and AMP through the EPG membranes has been shown to be a discontinuous function of temperature, that is, their permeability increased steeply above the Tg of the membranes. The amount of AMP permeated at 42 degrees C was nearly eight times as much as that at 36 degrees C. Arrhenius plots of the steady-state permeability coefficient (P) of AAP indicated two straight lines that intersect at the Tg of the 10% EPG membrane. In the water uptake study for the 10% EPG membrane, the degree of the swelling for the membrane tended to increase with increasing temperature above the Tg of the membrane. The thermo-sensitive permeation mechanism for the EPG membranes might be based on the structure change of the membranes caused by the glass transition, so that the membranes could absorb more water. Considering the high biological safety of Eudragit RS and PEG 400, the EPG membranes might be used to develop a novel thermo-sensitive drug delivery system.