Professor-Pharmaceutics and Drug Delivery University of Mississippi Mississippi, Mississippi
Previous in vitro studies with model membranes (i.e. Strat-M®), porcine skin and human skin suggest that cocoyl caprylocaprate, isopropyl myristate and octyldodecanol might be able to enhance the penetration of some common topical drugs, spanning a wide range of Log P values . To validate these observations, in vitro permeation studies through human skin were conducted with topical semi-solid creams containing cocoyl caprylocaprate (Kollicream® 3C), isopropyl myristate (Kollicream® IPM), octyldodecanol (Kollicream® OD), oleyl alcohol (Kollicream® OA), and/ or mineral oil. Each of these excipients was formulated into common cream bases which contained three different topical analgesic drugs: Ketoprofen (Log P = 3.1), Ibuprofen (Log P = 3.97) or Diclofenac Sodium (Log P = 04.51). Critical Quality Attributes (CQAs) such as pH, emulsion globule size, viscosity, API partitioning, water activity, etc. were measured for all of the creams. This presentation will report the effect of the different lipid-based excipients (and mineral oil) on the skin permeation of each of the three APIs and compare with the CQAs to better understand their mechanism of penetration enhancement.
Background on how excipients can impact the skin barrier and potential relationship between CQAs and API skin permeation.
Overview of current standards for IVPT (In Vitro Permeation Testing) and demonstration of the effects of excipient selection on API skin delivery.
Utilizing IVPT data to select the best penetration-enhancing excipient to match your API.