New prospective in treatment of Parkinson's disease: Studies on permeation of ropinirole through buccal mucosa

The aptitude of ropinirole to permeate the buccal tissue was tested using porcine mucosa mounted on Franz-type diffusion cells as ex vivo model. Drug permeation was also evaluated in presence of various penetration enhancers and in iontophoretic conditions. Ropinirole, widely used in treatment of mo...

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Bibliographic Details
Published in:International journal of pharmaceutics 2012-06, Vol.429 (1-2), p.78-83
Main Authors: De Caro, V., Giandalia, G., Siragusa, M.G., Sutera, F.M., Giannola, L.I.
Format: Article
Language:English
Subjects:
absorption
Absorption enhancement
Adjuvants, Pharmaceutic - chemistry
Administration, Buccal
Animal models
Animals
Antiparkinson Agents - administration & dosage
Antiparkinson Agents - pharmacokinetics
Buccal delivery
Buccal mucosa
Cyclohexenes - chemistry
Diffusion
Drug Delivery Systems
Drugs
electric field
Electric fields
Electricity
Feasibility Studies
Indoles - administration & dosage
Indoles - pharmacokinetics
Iontophoresis
Limonene
Membrane permeability
Models, Biological
Mouth Mucosa - metabolism
Movement disorders
mucosa
Neurodegenerative diseases
Parkinson disease
Parkinson Disease - drug therapy
Parkinson's disease
Permeability
pharmacokinetics
Porcine buccal mucosa
Ropinirole
Swine
Terpenes - chemistry
Therapeutic applications
Time Factors
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Summary:The aptitude of ropinirole to permeate the buccal tissue was tested using porcine mucosa mounted on Franz-type diffusion cells as ex vivo model. Drug permeation was also evaluated in presence of various penetration enhancers and in iontophoretic conditions. Ropinirole, widely used in treatment of motor fluctuations of Parkinson's disease, passes the buccal mucosa. Flux and permeability coefficient values suggested that the membrane does not appear a limiting step to the drug absorption. Nevertheless, an initial lag time is observed but the input rate can be modulated by permeation enhancement using limonene or by application of electric fields. Absorption improvement was accompanied by the important reduction of the lag time; at once the time required to reach the steady state plasma concentration was drastically decreased. On the basis of these results we could assume that clinical application of ropinirole by buccal delivery is feasible.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2012.03.022