title: Development of a Prolonged-Release Pramipexole Transdermal Patch: In Vitro and In Vivo Evaluation.
abstract: The current study aimed to develop a prolonged-release pramipexole (PPX) transdermal patch for the treatment of Parkinson's disease. Permeation parameters of PPX were investigated using human cadaver skin. Pramipexole patches were prepared using DURO-TAK®pressure-sensitive-adhesive (PSA) and evaluated for drug stability, drug loading, in vitro drug release, and in vitro permeation through mouse skin. The results indicated that blends of DURO-TAK®87-2852 and DURO-TAK®87-2510 were suitable for creating a prolonged-release PPX patch due to their advantages in drug release, drug loading, and stability. The final formulation consisted of 87-2852/87-2510 (70:30), 10% PG, and 15% PPX and showed a cumulative permeation amount of 1497.19 ± 102.90 μg/cm2with a continuous flux over 6.0 μg/(cm2·h) across human cadaver skin for 7 days. In vivo studies in rats indicated that PPX patch produced a significantly longer (p < 0.001) half-life (t1/2, 75.16 ± 17.37 h) and mean residence time (MRT, 135.89 ± 24.12 h) relative to oral tablets (Sifrol®) and had a relative bioavailability of 51.64 ± 21.32%. Therefore, this study demonstrated the feasibility of developing a prolonged-release PPX patch, which proposed the potential to serve as an alternate to conventional oral tablets and may therefore improve patient compliance.
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, No.2 Linggong Road, Dalian, 116024, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Pu
authors.affiliation: School of Life Science and Biotechnology, Dalian University of Technology, Dalian, Liaoning, China.
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Li
authors.affiliation: Chemical Analysis and Research Center, Dalian University of Technology, Dalian, Liaoning, China.
authors.forename: Yuming
authors.initials: Y
authors.lastname: Sun
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, No.2 Linggong Road, Dalian, 116024, China.
authors.forename: Xue
authors.initials: X
authors.lastname: Ding
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, No.2 Linggong Road, Dalian, 116024, China.
authors.forename: Yaqing
authors.initials: Y
authors.lastname: Pan
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, No.2 Linggong Road, Dalian, 116024, China. qwang@dlut.edu.cn.
authors.forename: Qing
authors.initials: Q
authors.lastname: Wang
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D052160:Benzothiazoles / Q000008:administration & dosage* / Q000737:chemistry*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D006207:Half-Life; D006801:Humans; D008297:Male; D051379:Mice; D000077487:Pramipexole; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects; D057968:Transdermal Patch
chemical_list: D000269:Adhesives; D052160:Benzothiazoles; D003692:Delayed-Action Preparations; D000077487:Pramipexole
keywords: Parkinson’s disease; pharmacokinetics; pramipexole; prolonged-release; transdermal patch