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Colloids Surf B Biointerfaces. 2018 Mar 1;163:9-18. doi: 10.1016/j.colsurfb.2017.12.015. Epub 2017 Dec 13.

Orally-dissolving film for sublingual and buccal delivery of ropinirole.

Author information

1
School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, China.
2
Department of Pharmacy and Pharmacology, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong, China.
3
School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, China. Electronic address: thomas.lee@cuhk.edu.hk.

Abstract

Ropinirole is a very important treatment option for Parkinson's disease (PD), a major threat to the aging population. However, this drug undergoes extensive first-pass metabolism, resulting in a low oral bioavailability. Moreover, the necessity of frequent administration due to the short half-life of ropinirole may jeopardize patient compliance. Indeed, taking this drug in solid oral dosage forms (e.g. Tablet) can be a challenge because of the tremor, rigidity, limited mobility, and impaired drug absorption experienced by PD patients. In light of these, there is a pressing need to devise formulations for the delivery of ropinirole that allow simple and easy administration and fast drug action, as well as avoidance of first-pass metabolism and overcoming the challenge of impaired absorption due to gastrointestinal dysfunctions, etc. Herein, we seek to overcome all these challenges via sublingual or buccal delivery of orally-dissolving films. Accordingly, we aimed to fabricate and characterize orally-dissolving films of ropinirole and assess their in vivo pharmacokinetics after sublingual and buccal administration. The ropinirole oral film was non-toxic and exhibited fast disintegration and dissolution and was physically stable for at least 28 days. Upon buccal/sublingual administration of the oral films, ropinirole reached the systemic circulation within 15 min and bioavailability was significantly improved, which may be attributable to avoidance of first-pass metabolism via absorption through the oral cavity. In conclusion, our ropinirole oral film improved bioavailability after sublingual or buccal administration. This formulation potentially overcomes biopharmaceutical challenges and provide a convenient means of administration of ropinirole or other anti-PD drugs.

KEYWORDS:

Buccal delivery; Oral mucosal delivery; Orally-dissolving films; Parkinson’s disease; Ropinirole; Sublingual delivery

PMID:
29268211
DOI:
10.1016/j.colsurfb.2017.12.015
[Indexed for MEDLINE]

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