Development and Evaluation of Thermoreversible Ethosomal Gel of Donepezil Hydrochloride for Intranasal Delivery,Journal of Pharmaceutical Innovation

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Development and Evaluation of Thermoreversible Ethosomal Gel of Donepezil Hydrochloride for Intranasal Delivery
Journal of Pharmaceutical Innovation ( IF 2.7 ) Pub Date : 2022-04-02 , DOI: 10.1007/s12247-022-09636-y
Arka Gangopadhyay ₁ , Panchaxari M. Dandagi ₁ , Kishori P. Sutar ₁

Affiliation

Purpose

The main aim of the present study was to formulate Donepezil Hydrochloride (DH)–loaded ethosomal intranasal gel to increase the transport of the drug through the blood–brain barrier (BBB), thus decreasing plasma fluctuation and also decreasing the oral side effects associated with the drug.

Methods

DH-loaded ethosomes were prepared by ethanol injection method. Nine ethosomal formulations were prepared containing three different concentrations of Phospholipon 90G and ethanol in combination and were evaluated for vesicle size, %entrapment efficiency, and drug content. The optimized ethosomal formulation was incorporated into the gelling base containing Poloxamer 407 (18%) and Poloxamer 188 (6%) as thermosensitive polymers and Carbopol 934 (0.1–0.5%) as mucoadhesive polymer. The prepared gels were further evaluated for gelation temperature, gelation time, drug content, mucoadhesive strength, viscosity, in vitro drug release, and ex vivo drug permeation study through the sheep nasal mucosa.

Results

The optimized ethosomal formulation F4 showed a vesicle size of 110.06 ± 1.910 and a % entrapment efficiency of 70.02 ± 0.353. The mucoadhesive strength and gelation temperature were found to be 3332 ± 4.314 and 31.7 ± 0.033 in the case of optimized gel formulation. The in vitro and ex vivo drug permeation from the optimized gel formulation was almost 100% after a period of 24 h.

Conclusion

Formulated DH-loaded ethosomal intranasal gel could serve as the better alternative for the brain targeting via the intranasal route.

中文翻译：

用于鼻内给药的盐酸多奈哌齐热可逆性溶质凝胶的开发与评价

目的

本研究的主要目的是配制载有盐酸多奈哌齐 (DH) 的鼻内凝胶，以增加药物通过血脑屏障 (BBB) 的转运，从而减少血浆波动并减少与药物相关的口服副作用。毒品。

方法

通过乙醇注射法制备负载 DH 的 ethosomes。制备了九种含有三种不同浓度的 Phospholipon 90G 和乙醇的联合制剂，并评估了囊泡大小、截留率百分比和药物含量。将优化的 ethosomal 配方加入到胶凝基质中，其中含有作为热敏聚合物的 Poloxamer 407 (18%) 和 Poloxamer 188 (6%) 以及作为粘膜粘附聚合物的 Carbopol 934 (0.1–0.5%)。进一步评估制备的凝胶的凝胶温度、凝胶时间、药物含量、粘膜粘附强度、粘度、体外药物释放和体外药物通过绵羊鼻粘膜的渗透研究。

结果

优化的 ethosomal 配方 F4 的囊泡大小为 110.06 ± 1.910，包封率为 70.02 ± 0.353。在优化凝胶配方的情况下，发现粘膜粘附强度和凝胶温度分别为 3332 ± 4.314 和 31.7 ± 0.033。在 24 小时后，优化凝胶制剂的体外和离体药物渗透率几乎为 100%。