Optimization of Nasal Liposome Formulation of Venlafaxine Hydrochloride using a Box-Behnken Experimental Design

IF 1.6 Q3 MEDICINE, RESEARCH & EXPERIMENTAL Current Therapeutic Research-clinical and Experimental Pub Date : 2023-01-01 DOI:10.1016/j.curtheres.2023.100714

Sulekha Khute MPharm, Rajendra K. Jangde PhD, MPharm

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Abstract

Background

Intranasal administration is among the most effective alternatives to deliver drugs directly to the brain and prevent first-pass metabolism. Venlafaxine-loaded liposomes are biocompatible carriers that enhance transport qualities over the nasal mucosa.

Objective

This research aimed to develop, formulate, characterize, and observe the prepared formulation.

Methods

The formulation was developed using the thin-film hydration technique. The response surface plot interrelationship between three independent variables are lipid, cholesterol and polymer and four dependent variables such as particle size, percentage entrapment efficiency, and percentage drug release were ascertained using the Box-Behnken design.

Results

The drug-release chitosan-coated liposomes were reported to have a particle size distribution, entanglement efficiency, and 84%, respectively, of 191 ± 34.71 nm, 94 ± 2.71% and 94 ± 2.71%. According to in vitro investigations, liposomes as a delivery system for the nasal route provided a more sustained drug release than the oral dosing form.

Conclusions

The intranasal administration of venlafaxine liposomal vesicles effectively enhanced the absolute bioavailability, retention time, and brain delivery of venlafaxine.

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Box-Behnken实验设计优化盐酸文拉法辛鼻脂质体制剂。

背景：鼻腔给药是将药物直接输送到大脑并防止首次代谢的最有效替代方案之一。载有文拉法辛的脂质体是一种生物相容性载体，可提高鼻粘膜的运输质量。目的：本研究旨在开发、配制、表征和观察所制备的制剂。方法：采用薄膜水化技术研制制剂。三个自变量（脂质、胆固醇和聚合物）之间的响应面图相互关系，四个因变量（如粒径、包封率和药物释放率）使用Box-Behnken设计确定。结果：壳聚糖包被脂质体的粒径分布为191±34.71nm，包被率为94±2.71%，包被效率为84%，与口服给药相比，脂质体作为鼻腔给药系统提供了更持久的药物释放。结论：文拉法辛脂质体囊泡的鼻内给药有效地提高了文拉法辛的绝对生物利用度、保留时间和脑给药。

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来源期刊

Current Therapeutic Research-clinical and Experimental 医学-药学

CiteScore

3.50

自引率

0.00%

发文量

审稿时长

3 months

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