Purpose This study aimed to optimize nanosponges loaded with V. opulus water extract formulation to diminish the limitations of extracts such as poor absorption, low bioavailability, inadequate biodistribution. Moreover, to the best of our knowledge, it represents the first investigation of nanosponge loaded with V. opulus water extract formulation. Methods The nanosponges were produced using a quasi-emulsion technique. The optimal formulation was selected using a design of experiments (DOE) approach, incorporating variables such as methylcellulose (MC) (0.5–0.8%, w/w), polyvinyl alcohol (PVA) (0.3–0.7%, w/w), and Tween 80 (TW80) (0.2–0.7%, w/w). The primary quality attributes considered were particle size and encapsulation efficiency. Following optimization, the formulations were subjected to morphological and physicochemical analyses to confirm the compatibility of the components within the nanosponges. The drug release profiles were assessed and compared with a control group using ultra-performance liquid chromatography. Also, total phenolic content and antioxidant activity were assessed to evaluate functional preservation after encapsulation. Results The resulting particle size and encapsulation efficiency were found to be 190.833 ± 8.3 nm and 81.0 ± 6.3 %, respectively. The V. opulus extract nanosponge exhibited distinct release profiles across the pH range of 1.2, 4.5, and 6.8. No significant difference in release was observed between the nanosponge and the control group at pH 1.2 (p > 0.05). However, at pH 4.5 and 6.8, a statistically significant difference was found between the two groups (p < 0.05). Additionally, a notable difference in release patterns was observed between pH 4.5 and pH 6.8 for the V. opulus extract nanosponge. The release mechanisms of The V. opulus extract nanosponge gel were fitted Higuchi kinetics at pH 1.2 (R2: 0.7117), pH 4.5 (R2: 0.7949) and pH 6.8 (R2: 0.7006). The release mechanisms of the control gel were fitted Higuchi kinetics at pH 1.2 (R2: 0.6976), pH 4.5 (R2: 0.8573) and pH 6.8 (R2: 0.6446) and First order kinetics at pH 4.5 (R2: 0.8528). The physicochemical characterization proved that in the formulation used components were compatible with each other. Additionally, formulations containing nanosponges demonstrated superior total phenolic content and antioxidant activity in comparison to their non-nanosponge counterparts. Conclusion The V. opulus nanosponge formulation exhibited a significantly higher drug release profile compared to the V. opulus conventional hydrogel formulation. It could be concluded that V. opulus nanosponges represent a promising delivery system to overcome the limitations of the extract and enhance its potential benefits in specific public health concerns, such as the prevention or management of kidney stones.

A Novel Nanosponge-Based Oral Delivery System for Viburnum opulus L. Fruit Extract: Formulation, Characterization and Antioxidant Assessment

期刊论文
发表日期：

2025年10月20日

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Juste Baranauskaite,
Mehmet Ali Oçkun,
Etil Güzelmeric,
Birce Öztürk,
Alisa Uzunlar,
Hasan Kırmızıbekmez

摘要

Purpose

This study aimed to optimize nanosponges loaded with V. opulus water extract formulation to diminish the limitations of extracts such as poor absorption, low bioavailability, inadequate biodistribution. Moreover, to the best of our knowledge, it represents the first investigation of nanosponge loaded with V. opulus water extract formulation.

Methods

The nanosponges were produced using a quasi-emulsion technique. The optimal formulation was selected using a design of experiments (DOE) approach, incorporating variables such as methylcellulose (MC) (0.5–0.8%, w/w), polyvinyl alcohol (PVA) (0.3–0.7%, w/w), and Tween 80 (TW80) (0.2–0.7%, w/w). The primary quality attributes considered were particle size and encapsulation efficiency. Following optimization, the formulations were subjected to morphological and physicochemical analyses to confirm the compatibility of the components within the nanosponges. The drug release profiles were assessed and compared with a control group using ultra-performance liquid chromatography. Also, total phenolic content and antioxidant activity were assessed to evaluate functional preservation after encapsulation.

Results

The resulting particle size and encapsulation efficiency were found to be 190.833 ± 8.3 nm and 81.0 ± 6.3 %, respectively. The V. opulus extract nanosponge exhibited distinct release profiles across the pH range of 1.2, 4.5, and 6.8. No significant difference in release was observed between the nanosponge and the control group at pH 1.2 (p > 0.05). However, at pH 4.5 and 6.8, a statistically significant difference was found between the two groups (p < 0.05). Additionally, a notable difference in release patterns was observed between pH 4.5 and pH 6.8 for the V. opulus extract nanosponge. The release mechanisms of The V. opulus extract nanosponge gel were fitted Higuchi kinetics at pH 1.2 (R²: 0.7117), pH 4.5 (R²: 0.7949) and pH 6.8 (R²: 0.7006). The release mechanisms of the control gel were fitted Higuchi kinetics at pH 1.2 (R²: 0.6976), pH 4.5 (R²: 0.8573) and pH 6.8 (R²: 0.6446) and First order kinetics at pH 4.5 (R²: 0.8528). The physicochemical characterization proved that in the formulation used components were compatible with each other. Additionally, formulations containing nanosponges demonstrated superior total phenolic content and antioxidant activity in comparison to their non-nanosponge counterparts.

Conclusion

The V. opulus nanosponge formulation exhibited a significantly higher drug release profile compared to the V. opulus conventional hydrogel formulation. It could be concluded that V. opulus nanosponges represent a promising delivery system to overcome the limitations of the extract and enhance its potential benefits in specific public health concerns, such as the prevention or management of kidney stones.