Tolentino Seila, Monteiro Mylene M, Saldanha-Araújo Felipe, Cunha-Filho Marcilio, Gratieri Tais, Guerra Eliete N Silva, Gelfuso Guilherme M
Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, Brasília 70910-900, Brazil.
Laboratory of Oral Histopathology, University of Brasilia, Brasília 70910-900, Brazil.
Pharmaceutics. 2024 Dec 26;17(1):18. doi: 10.3390/pharmaceutics17010018.
: This study aimed to evaluate the safety and efficacy of chitosan-based bioadhesive films for facilitating the topical delivery of curcumin in skin cancer treatment, addressing the pharmacokinetic limitations associated with oral administration. : The films, which incorporated curcumin, were formulated using varying proportions of chitosan, polyvinyl alcohol, Poloxamer 407, and propylene glycol. These films were assessed for stability, drug release, in vitro skin permeation, cell viability (with and without radiotherapy), and skin irritation. : The films demonstrated physical stability and preserved curcumin content at room temperature for 90 days. Drug release was effectively controlled during the first 8 h, with release rates ranging from 51.6 ± 4.8% to 65.6 ± 13.0%. The films also enhanced drug penetration into the skin compared to a curcumin solution used as a control (stratum corneum: 1.3 ± 0.1 to 1.9 ± 0.8 µg/cm²; deeper skin layers: 1.7 ± 0.1 to 2.7 ± 0.2 µg/cm²). A cytotoxicity test on metastatic melanoma cells showed that curcumin at topical doses exerted activity similar to that delivered via the skin. Furthermore, curcumin alone was more effective in inhibiting tumor cells than radiotherapy alone ( < 0.01), with no additional benefit observed when curcumin was combined with radiotherapy. Finally, irritation tests confirmed that the films were safe for topical application. : The developed chitosan-based bioadhesive films represent a promising alternative for the topical treatment of skin tumors using curcumin.
本研究旨在评估基于壳聚糖的生物粘附膜在皮肤癌治疗中促进姜黄素局部递送的安全性和有效性，解决与口服给药相关的药代动力学限制。含有姜黄素的薄膜采用不同比例的壳聚糖、聚乙烯醇、泊洛沙姆407和丙二醇制成。对这些薄膜进行了稳定性、药物释放、体外皮肤渗透、细胞活力（有或无放疗）和皮肤刺激性评估。这些薄膜在室温下表现出物理稳定性，姜黄素含量在90天内保持不变。在最初的8小时内药物释放得到有效控制，释放率在51.6±4.8%至65.6±13.0%之间。与用作对照的姜黄素溶液相比，这些薄膜还增强了药物对皮肤的渗透（角质层：1.3±0.1至1.9±0.8μg/cm²；皮肤深层：1.7±0.1至2.7±0.2μg/cm²）。对转移性黑色素瘤细胞的细胞毒性试验表明，局部剂量的姜黄素发挥的活性与经皮肤递送的活性相似。此外，单独使用姜黄素在抑制肿瘤细胞方面比单独放疗更有效（<0.01），当姜黄素与放疗联合使用时未观察到额外益处。最后，刺激性试验证实这些薄膜局部应用是安全的。所开发的基于壳聚糖的生物粘附膜是使用姜黄素局部治疗皮肤肿瘤的一种有前景的替代方法。
