TY - JOUR
T1 - Dimethysiloxane polymer for the effective transdermal delivery of donepezil in Alzheimer's disease treatment
AU - Lee, Jihyun
AU - Ju, In Gyoung
AU - Lim, Yeon Jin
AU - Kim, Jin Hee
AU - Lee, Seungmin
AU - Choi, Yujin
AU - Oh, Myung Sook
AU - Kim, Jaehoon
AU - Kim, Dokyoung
N1 - Publisher Copyright:
© 2025 The Royal Society of Chemistry.
PY - 2024/11/19
Y1 - 2024/11/19
N2 - Donepezil (DNZ) has been used to treat dementia associated with mild, moderate, or severe Alzheimer's disease (AD). DNZ uptake can alleviate cognitive symptoms in AD patients via acetylcholinesterase (AChE) inhibition. However, oral administration of DNZ has limitations, including first-pass metabolism, difficulties with swallowing, and low patient compliance. In this work, we disclose a novel transdermal DNZ delivery system utilizing T2 polymer, synthesized via the ring-opening polymerization of 2,2,5,5-tetramethyl-2,5-disila-1-oxacyclopentane with trifluoroacetic acid (TFA). In the in vivo studies in an AD animal model, the DNZ-loaded T2 polymer (DNZ@T2) facilitated efficient transdermal DNZ delivery to the bloodstream and improved spatial working memory and long-term memory of the AD mouse model. Both the T2 polymer and DNZ@T2 exhibited low cytotoxicity and non-significant in vivo toxicity. This research highlights a promising transdermal delivery strategy for AD treatment, potentially enhancing therapeutic efficacy and patient compliance.
AB - Donepezil (DNZ) has been used to treat dementia associated with mild, moderate, or severe Alzheimer's disease (AD). DNZ uptake can alleviate cognitive symptoms in AD patients via acetylcholinesterase (AChE) inhibition. However, oral administration of DNZ has limitations, including first-pass metabolism, difficulties with swallowing, and low patient compliance. In this work, we disclose a novel transdermal DNZ delivery system utilizing T2 polymer, synthesized via the ring-opening polymerization of 2,2,5,5-tetramethyl-2,5-disila-1-oxacyclopentane with trifluoroacetic acid (TFA). In the in vivo studies in an AD animal model, the DNZ-loaded T2 polymer (DNZ@T2) facilitated efficient transdermal DNZ delivery to the bloodstream and improved spatial working memory and long-term memory of the AD mouse model. Both the T2 polymer and DNZ@T2 exhibited low cytotoxicity and non-significant in vivo toxicity. This research highlights a promising transdermal delivery strategy for AD treatment, potentially enhancing therapeutic efficacy and patient compliance.
UR - http://www.scopus.com/inward/record.url?scp=85209992264&partnerID=8YFLogxK
U2 - 10.1039/d4bm01368a
DO - 10.1039/d4bm01368a
M3 - Article
C2 - 39576095
AN - SCOPUS:85209992264
SN - 2047-4830
VL - 13
SP - 1189
EP - 1198
JO - Biomaterials Science
JF - Biomaterials Science
IS - 5
ER -