Booravilli Joshna, Sirisolla Janaki Devi
Department of Pharmaceutics, GITAM School of Pharmacy, GITAM (Deemed to be University), Visakhapatnam, India.
Drug Dev Ind Pharm. 2025 Jul;51(7):771-785. doi: 10.1080/03639045.2025.2509274. Epub 2025 Jun 4.
Quercetin, a polyphenolic flavonoid with antioxidant and anticancer effects, has limited use due to poor water solubility. The objective of this study was to improve the therapeutic effectiveness of quercetin by developing a topical quercetin nanoemulgel.
By optimizing the oil (clove oil) and smix ratio (Tween 20:propylene glycol), quercetin nanoemulsion was prepared by spontaneous emulsification method and then evaluated. The optimized nanoemulsion was further prepared to form quercetin nanoemulgel.
According to evaluation studies, the optimized quercetin nanoemulsion (QUE NE 3) exhibited stability with a negative zeta potential (-38.2 mV), a tiny particle size (98.2 nm), and high entrapment effectiveness (96.36%). The optimized nanoemulsion was formulated into a nanoemulgel (QUE NEG 3). Studies on drug release of quercetin nanoemulgel (QUE NEG 3) showed improved permeability, with cumulative drug release of 93.56 ± 1.16% in 8 h, which was greater than standard quercetin gel (QG) and drug free loaded nanoemulgel (DFL NEG). This was proved by CLSM which shows the delivery of QUE NEG 3 into the dermis. Dose-dependent inhibitory effects were found in cytotoxicity assays conducted on skin cancer cell lines (TE 354.T, A431, and A375) by using the MTT assay. The results demonstrated that quercetin nanoemulgel (QUE NEG 3) showed higher cytotoxicity of 66.52% especially against A431 cells. Hence proving its ability to treat squamous cell carcinoma.
These findings imply that the quercetin nanoemulgel is a viable drug delivery method for enhancing quercetin's solubility and therapeutic efficacy.
槲皮素是一种具有抗氧化和抗癌作用的多酚类黄酮，因其水溶性差而应用受限。本研究的目的是通过开发一种局部用槲皮素纳米乳凝胶来提高槲皮素的治疗效果。
通过优化油相（丁香油）和表面活性剂混合比例（吐温20：丙二醇），采用自发乳化法制备槲皮素纳米乳并进行评价。将优化后的纳米乳进一步制成槲皮素纳米乳凝胶。
根据评价研究，优化后的槲皮素纳米乳（QUE NE 3）具有稳定性，zeta电位为负（-38.2 mV），粒径微小（98.2 nm），包封率高（96.36%）。将优化后的纳米乳制成纳米乳凝胶（QUE NEG 3）。槲皮素纳米乳凝胶（QUE NEG 3）的药物释放研究表明其渗透性得到改善，8小时内累积药物释放率为93.56±1.16%，高于标准槲皮素凝胶（QG）和无药物负载纳米乳凝胶（DFL NEG）。共聚焦激光扫描显微镜（CLSM）证明了QUE NEG 3可递送至真皮层。通过MTT法对皮肤癌细胞系（TE 354.T、A431和A375）进行细胞毒性试验，发现具有剂量依赖性抑制作用。结果表明，槲皮素纳米乳凝胶（QUE NEG 3）具有较高的细胞毒性，尤其是对A431细胞的细胞毒性为66.52%。因此证明了其治疗鳞状细胞癌的能力。
这些发现表明，槲皮素纳米乳凝胶是一种可行的药物递送方法，可提高槲皮素的溶解度和治疗效果。
