Optimization of Eudragit RS100 Nanocapsule Formulation for Encapsulating Perillyl Alcohol and Temozolomide Using Design of Experiments

利用实验设计优化Eudragit RS100纳米胶囊制剂,用于包封紫苏醇和替莫唑胺

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Abstract

Glioblastoma, an aggressive intracranial tumor, presents significant therapeutic challenges due to the restrictive nature of the blood-brain barrier (BBB), which limits the effectiveness of conventional treatments. This study aimed to develop and optimize a nanoencapsulated system for intranasal delivery of temozolomide (TMZ) and perillyl alcohol (POH), designed to circumvent BBB limitations, utilizing Eudragit RS100 as the encapsulation matrix. A factorial design approach optimized key parameters, including Eudragit RS100 concentration, POH amount, drip rate, and organic-to-aqueous phase ratio. The nanocapsules were characterized by dynamic light scattering, zeta potential analysis, scanning electron microscopy, and high-performance liquid chromatography. The optimized nanocapsules demonstrated a mean diameter of 253 ± 52 nm and a polydispersity index of 0.145 ± 0.037, indicating uniform size distribution. A zeta potential of approximately +20 mV supported colloidal stability. Encapsulation efficiencies were 3.7% for POH and 28.5% for TMZ. This nanoencapsulated delivery system offers a promising approach for glioblastoma treatment, potentially enhancing clinical outcomes and reducing treatment-associated toxicity.

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