Development of thermosensitive mucoadhesive gel incorporated lipid microspheres of donepezil for enhanced nose-to-brain delivery DOI

Rachmatya W. Tuna,

Nurafni Annisa Achmad,

Irfan Kurniawan

et al.

Journal of Biomaterials Science Polymer Edition, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 28

Published: April 22, 2025

Alzheimer's disease (ALZ) is a chronic that affects the brain neurons leading to dementia. Donepezil (DPZ), first-line treatment for ALZ potent symptomatic therapeutic agent. However, oral and transdermal route represents non-targeted delivery, causing various adverse effects. This study presents successful incorporation of DPZ-loaded lipid microsphere (DPZ-LM) system into thermosensitive-mucoadhesive gel (TMG), thereby enhancing delivery DPZ through nose-to-brain route. To optimize formulations, several evaluations were conducted, resulting in an optimized formulation LM using Compritol® exhibited particle size 8.75 µm, 98.44% entrapped, 93.40% loaded with sustained release manner vitro studies. The TMG-DPZ-LM was prepared Pluronic® F127 F68, as gelling agents, addition sodium alginate, mucoadhesive polymer. Following TMG-DPZ-LM, excellent physicochemical properties effective nasal ex vivo permeation has found 88.58 ± 12.53 µg/cm2 retention studies mean concentration 0.0077 mg porcine mucosa. pharmacokinetic demonstrated administration via resulted significant (p < 0.05) increase Cmax, 207.24 5.16 µg/cm3 significantly different profile compared other formulation. developed this considered have improved its efficacy ALZ.

Language: Английский

Development of thermosensitive mucoadhesive gel incorporated lipid microspheres of donepezil for enhanced nose-to-brain delivery DOI

Rachmatya W. Tuna,

Nurafni Annisa Achmad,

Irfan Kurniawan

et al.

Journal of Biomaterials Science Polymer Edition, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 28

Published: April 22, 2025

Alzheimer's disease (ALZ) is a chronic that affects the brain neurons leading to dementia. Donepezil (DPZ), first-line treatment for ALZ potent symptomatic therapeutic agent. However, oral and transdermal route represents non-targeted delivery, causing various adverse effects. This study presents successful incorporation of DPZ-loaded lipid microsphere (DPZ-LM) system into thermosensitive-mucoadhesive gel (TMG), thereby enhancing delivery DPZ through nose-to-brain route. To optimize formulations, several evaluations were conducted, resulting in an optimized formulation LM using Compritol® exhibited particle size 8.75 µm, 98.44% entrapped, 93.40% loaded with sustained release manner vitro studies. The TMG-DPZ-LM was prepared Pluronic® F127 F68, as gelling agents, addition sodium alginate, mucoadhesive polymer. Following TMG-DPZ-LM, excellent physicochemical properties effective nasal ex vivo permeation has found 88.58 ± 12.53 µg/cm2 retention studies mean concentration 0.0077 mg porcine mucosa. pharmacokinetic demonstrated administration via resulted significant (p < 0.05) increase Cmax, 207.24 5.16 µg/cm3 significantly different profile compared other formulation. developed this considered have improved its efficacy ALZ.

Language: Английский

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