Formulation, in vitro, and in vivo evaluation of matrix-type transdermal patches containing olanzapine

• Published in: Pharmaceutical development and technology 2013-07, Vol.18 (4), p.916-925
• Main Authors: Aggarwal, Geeta, Dhawan, Sanju, Harikumar, S. L.
• Format: Article
• Language: English
• Subjects: Acrylic Resins - chemistry; Administration, Cutaneous; Animals; Antipsychotic Agents - administration & dosage; Antipsychotic Agents - pharmacokinetics; Antipsychotic Agents - pharmacology; atypical antipsychotic; Benzodiazepines - administration & dosage; Benzodiazepines - pharmacokinetics; Benzodiazepines - pharmacology; Delayed-Action Preparations; Drug Carriers - chemistry; eudragit; Excipients - chemistry; In Vitro Techniques; Mice; olive oil; Permeability; permeation enhancers; Rabbits; Rats; Rats, Wistar; Skin Absorption; Skin Irritancy Tests; Surface-Active Agents - chemistry; surfactant; Time Factors; Transdermal drug delivery; Transdermal Patch
• ISSN: 1083-7450; 1097-9867
• DOI: 10.3109/10837450.2011.609993

Transdermal patches of olanzapine were aimed to be prepared to overcome the side effects by oral application. The strategy was formulation of eudragit-based polymeric films to prepare transdermal patches by using nonionic (span-20), anionic (sodium lauryl sulfate), cationic surfactant (benzalkonium chloride), and vegetable oil (olive oil) as permeation enhancers. The patches were subjected to physicochemical, in vitro release and ex vivo permeation studies. On the basis of in vitro release performance, ERL 100:ERS 100 in the ratio of 3:2 was selected for incorporation of permeation enhancers. The permeation studies showed that formulation containing 10% span 20 (OD3) exhibited greatest cumulative amount of drug permeated (19.02 ± 0.21 mg) in 72 h, so OD3 was concluded as optimized formulation and assessed for pharmacokinetic, pharmacodynamic, and skin irritation potential. In vivo studies of optimized olanzapine patch in rabbit model revealed prolongation of action with Frel 116.09% during 72-h study period. Neuroleptic efficacy of transdermal patch was comparable to oral formulation during rotarod and grip test in Wistar albino rats with no skin irritation. Thus, developed formulation of olanzapine is expected to improve the patient compliance, form better dosage regimen, and provide maintenance therapy to psychotic patients.