Dr. Prabhakar Kore Basic Science Research Center, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi-590010, Karnataka, India.
Curr Drug Deliv. 2021;18(5):607-619. doi: 10.2174/1567201817666200902150646.
The aim of the study was to formulate, characterize, and evaluate the Resveratrol- loaded Cubosomes (RC) for topical application.
Resveratrol (RV) is a nutraceutical compound with exciting pharmacological potential in different diseases, including cancers. Many studies on resveratrol have been reported for anti- melanoma activity. Due to its low bioavailability, the therapeutic activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been made to increase its activity through transdermal drug delivery.
To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate Resveratrol-loaded Cubosomal Gel (RC-Gel) for its topical application.
RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies.
The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV, respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 3.91%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization.
The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.
本研究的目的是制备、表征和评价姜黄素载药立方液晶（RC）用于局部应用。
姜黄素（RV）是一种具有令人兴奋的药理学潜力的营养化合物，可用于治疗多种疾病，包括癌症。已有许多关于姜黄素的研究报道了其抗黑色素瘤活性。由于其生物利用度低，姜黄素的治疗活性受到很大限制。因此，采用纳米技术的方法通过经皮给药来提高其活性。
制备、表征和评价姜黄素载药立方液晶（RC）。评估姜黄素载药立方液晶凝胶（RC-Gel）的局部应用。
采用匀化技术制备 RC，并采用 2 因素 3 水平析因设计进行优化。对所制备的 RC 进行粒径、Zeta 电位和包封效率的表征。对优化后的 RC 进行体外释放和稳定性研究。进一步将优化后的 RC 用卡波姆制成立方液晶凝胶（RC-Gel），并评价其药物渗透和沉积。此外，对开发的 RC-Gel 进行皮肤刺激性、毒性和体内局部生物利用度研究，以评估其局部应用。
优化后的 RC 呈立方体形结构，平均粒径、包封效率和 Zeta 电位分别为 113±2.36nm、85.07±0.91%和-27.40±1.40mV。优化后的 RC 体外药物释放呈双相药物释放，姜黄素（RV）呈扩散控制释放（87.20±3.91%）。RC-Gel 显示出更好的药物渗透和在小鼠皮肤层中的沉积。RC-Gel 的组成被证明对小鼠皮肤无刺激性。体内局部生物利用度研究表明，RC-Gel 具有良好的皮肤定位潜力。
RC 纳米制剂为通过局部应用治疗黑色素瘤提供了一种有前途的药物传递系统。
