The reversibility of absorption promoter interaction with red blood cell membranes studied with differential scanning calorimetry.
Absorption promoters, or adjuvants, are used to enhance the gastrointestinal absorption of poorly absorbed drugs such as macromolecules. In the present work, adjuvant-membrane interactions have been studied by differential scanning calorimetry (DSC) using red blood cell (RBC) membranes as model membrane. These interactions caused temperature shifts, amplitude changes, and broadening of the RBC transitions. Because more than one transition may be simultaneously affected by a given adjuvant, complex overlappings occur. Gaussian modeling and nonlinear regression analysis, therefore, were used to resolve these transitions. A correlation, which may serve as an indicator of adjuvant potency, was found between adjuvant concentration and induced transition temperature shifts. Further, these shifts recovered to baseline after successive washings with buffer (for most adjuvants). Sodium lauryl sulfate induced transition alterations, however, never recovered. Thus the DSC might be useful in monitoring reversible adjuvant-membrane interactions.
Holinej
J
J
Department of Pharmaceutics, Philadelphia College of Pharmacy and Science, Pennsylvania 19104.
Ando
H Y
HY
Snow
J W
JW
D000042:Absorption; D000277:Adjuvants, Pharmaceutic; D002152:Calorimetry, Differential Scanning; D004910:Erythrocyte Membrane / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D008298:Maleates; D012967:Sodium Dodecyl Sulfate; D013696:Temperature
D000277:Adjuvants, Pharmaceutic; D008298:Maleates; D012967:Sodium Dodecyl Sulfate; C014476:diethyl maleate