Development and evaluation of a drug-in-adhesive transdermal delivery system for delivery of olanzapine

摘要

Objectives: Olanzapine (OZP) is a safe and effective atypical antipsychotic drug used in treating schizophrenia and bipolar disorders. The dosage forms currently on the market for OZP are administered via oral or intramuscular routes. However, there are many problems associated with oral and intramuscular routes of drug administration. Thus, our aim was to develop a drug-in-adhesive transdermal delivery system (TDS) that can deliver OZP for 3 days. Methods: We determined passive permeation, effect of oleic acid as chemical enhancer, and delivery of OZP across different skin types. Based on preliminary studies and saturation solubility of OZP in different pressure-sensitive adhesives (PSAs), we formulated and characterized solution-based TDS in acrylate PSA and suspension-based TDS in silicone and PIB PSA, with oleic acid as chemical enhancer. Results: Acrylate solution-based TDS, silicone, and PIB suspension-based TDS delivered 58.97 +/- 6.59 mu g/sq.cm , 129.34 +/- 16.59 mu g/sq.cm, and 245.00 +/- 2.51 mu g/sq.cm, respectively, using in vitro permeation testing. PIB PSA suspension-based TDS met the 3 days desired target delivery. Skin irritation testing using In vitro EpiDerm (TM) skin irritation test (EPI-200-SIT) kit found PIB TDS to be nonirritant. Conclusion: The PIB PSA suspension-based TDS could serve as a potentially effective transdermal delivery system for olanzapine.