Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA, USA.
Expert Opin Drug Deliv. 2022 Nov;19(11):1539-1548. doi: 10.1080/17425247.2022.2135700. Epub 2022 Oct 14.
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.
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.
Acrylate solution-based TDS, silicone, and PIB suspension-based TDS delivered 58.97 ± 6.59 µg/sq.cm, 129.34 ± 16.59 µg/sq.cm, and 245.00 ± 2.51 µg/sq.cm, respectively, using permeation testing. PIB PSA suspension-based TDS met the 3 days desired target delivery. Skin irritation testing using In vitro EpiDerm skin irritation test (EPI-200-SIT) kit found PIB TDS to be nonirritant.
The PIB PSA suspension-based TDS could serve as a potentially effective transdermal delivery system for olanzapine.
奥氮平（OZP）是一种安全有效的非典型抗精神病药物，用于治疗精神分裂症和双相情感障碍。目前市场上的 OZP 剂型通过口服或肌肉注射途径给药。然而，口服和肌肉注射途径给药存在许多问题。因此，我们的目的是开发一种可用于 3 天的药物贴剂经皮给药系统（TDS）。
我们确定了奥氮平的被动渗透，油酸作为化学增强剂的作用以及不同皮肤类型的药物传递。根据初步研究和奥氮平在不同压敏胶（PSA）中的饱和溶解度，我们在丙烯酸 PSA 中配制并表征了基于溶液的 TDS，在硅酮和 PIB PSA 中配制并表征了基于悬浮液的 TDS，油酸作为化学增强剂。
丙烯酸基溶液 TDS、硅酮和 PIB 基悬浮液 TDS 的经皮渗透测试分别递送 58.97 ± 6.59 µg/sq.cm、129.34 ± 16.59 µg/sq.cm 和 245.00 ± 2.51 µg/sq.cm。PIB PSA 悬浮液 TDS 达到了 3 天的预期目标。使用体外 EpiDerm 皮肤刺激试验（EPI-200-SIT）试剂盒进行皮肤刺激试验发现 PIB TDS 无刺激性。
PIB PSA 悬浮液 TDS 可作为奥氮平的一种潜在有效经皮给药系统。
