Resveratrol-loaded invasome gel: A promising nanoformulation for treatment of skin cancer.

IF 5.7 3区 医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL
Drug Delivery and Translational Research Pub Date : 2024-12-01 Epub Date: 2024-02-15 DOI:10.1007/s13346-024-01534-9
Bassant Samir, Amal El-Kamel, Noha Zahran, Lamia Heikal
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Abstract

Skin cancer is a widespread type of cancer representing 30% of all cancer types worldwide. Resveratrol (RSV) is an anticancer drug used for skin cancer treatment. Several limitations of RSV such as poor aqueous solubility, first-pass metabolism, and instability limit their topical use. The study aimed to develop and optimize RSV-loaded invasomes for topical administration as well as assess their efficacy in vivo. The optimized RSV-loaded invasomes showed small particle size (208.7 ± 74 nm), PDI (0.3 ± 0.03), high % entrapment efficiency (77.7 ± 6%), and negative zeta potential (-70.4 ± 10.9 mV). They showed an initial burst effect followed by controlled drug release for 24 h. RSV-loaded invasomal gel revealed the highest skin deposition percentage (65%) in ex vivo rat skin, the highest potency (low IC50 of 6.34 μg/mL), and the highest cellular uptake when tested on squamous cancerous cells (SCCs) when compared to other formulations. The antitumor effect of topical RSV-loaded invasomes was also evaluated in vivo in Ehrlich-induced mice models. The results revealed that RSV-loaded invasomal gel exhibited the smallest tumor volume with no signs of organ toxicity indicating its safety in skin cancer treatment. Upregulation of BAX and Caspase-3 gene levels and downregulation of NF-kB and BCL2 protein levels were demonstrated using RT-PCR and ELISA tests, respectively. Interestingly, the present study is the first to develop RSV-loaded invasomal gel for topical skin cancer treatment. According to our results, invasomes are considered promising lipid-based nanosystems for topical RSV delivery having high skin penetration ability and anticancer effect in the treatment of skin carcinoma.

负载藜芦醇的侵袭体凝胶:治疗皮肤癌的前景广阔的纳米制剂。
皮肤癌是一种常见的癌症,占全球所有癌症类型的 30%。白藜芦醇(RSV)是一种用于治疗皮肤癌的抗癌药物。RSV 的一些局限性,如水溶性差、首过代谢和不稳定性,限制了其局部使用。这项研究旨在开发和优化用于局部用药的RSV负载内含体,并评估其体内疗效。优化后的RSV负载内含体显示出小粒径(208.7 ± 74 nm)、PDI(0.3 ± 0.03)、高吸附效率(77.7 ± 6%)和负ZETA电位(-70.4 ± 10.9 mV)。与其他制剂相比,RSV 负载的侵袭体凝胶在大鼠体外皮肤上的沉积率最高(65%),药效最强(IC50 低至 6.34 μg/mL),在鳞状癌细胞(SCC)上的细胞吸收率最高。在艾氏诱导的小鼠模型中,还对局部RSV负载的侵袭体的抗肿瘤效果进行了体内评估。结果显示,RSV-负载型侵袭体凝胶的肿瘤体积最小,且无器官毒性迹象,表明其在皮肤癌治疗中的安全性。RT-PCR和ELISA检测分别证明了BAX和Caspase-3基因水平的上调以及NF-kB和BCL2蛋白水平的下调。有趣的是,本研究首次开发了用于皮肤癌局部治疗的RSV负载型侵袭体凝胶。根据我们的研究结果,内陷体被认为是一种很有前景的脂质纳米系统,可用于RSV的局部递送,具有很高的皮肤渗透能力和抗癌效果,可用于治疗皮肤癌。
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来源期刊
Drug Delivery and Translational Research
Drug Delivery and Translational Research MEDICINE, RESEARCH & EXPERIMENTALPHARMACOL-PHARMACOLOGY & PHARMACY
CiteScore
11.70
自引率
1.90%
发文量
160
期刊介绍: The journal provides a unique forum for scientific publication of high-quality research that is exclusively focused on translational aspects of drug delivery. Rationally developed, effective delivery systems can potentially affect clinical outcome in different disease conditions. Research focused on the following areas of translational drug delivery research will be considered for publication in the journal. Designing and developing novel drug delivery systems, with a focus on their application to disease conditions; Preclinical and clinical data related to drug delivery systems; Drug distribution, pharmacokinetics, clearance, with drug delivery systems as compared to traditional dosing to demonstrate beneficial outcomes Short-term and long-term biocompatibility of drug delivery systems, host response; Biomaterials with growth factors for stem-cell differentiation in regenerative medicine and tissue engineering; Image-guided drug therapy, Nanomedicine; Devices for drug delivery and drug/device combination products. In addition to original full-length papers, communications, and reviews, the journal includes editorials, reports of future meetings, research highlights, and announcements pertaining to the activities of the Controlled Release Society.
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