Satapathy Bhabani Sankar, Zafar Ameeduzzafar, Warsi Musarrat Husain, Behera Sritam, Mohanty Dibya Iochan, Mujtaba Md Ali, Mohanty Mahaprasad, Upadhyay Atul Kumar, Khalid Mohammad
GITAM School of Pharmacy, GITAM Deemed to be University Hyderabad Campus Telangana-502329 India.
Department of Pharmaceutics, College of Pharmacy, Jouf University Sakaka 72341 Al-Jouf Saudi Arabia
RSC Adv. 2025 Feb 19;15(8):5665-5680. doi: 10.1039/d4ra08397k.
A lipid-based nanocarrier system is a novel technique for the delivery of poorly soluble drugs through topical delivery. This study developed a dual-drug (luliconazole: LZ, and niacinamide: NM) loaded lipid nanocarrier (LN)-laden gel for the treatment of vaginal candidiasis. The LNs were prepared using cholesterol and soya-α-lecithin through a thin-film hydration technique. The average vesicle size, polydispersity index, and zeta potential of the optimized LZNMLNs were 126.40 ± 1.30 nm, 0.276, and -34.6 ± 0.8 mV, respectively, and the formulation showed the sustained release of both drugs over an extended period. Selected LZNMLNs were incorporated into a bio-adhesive gel. The optimized LZNMLNs-gel showed excellent viscosity, spreadability, and bio-adhesiveness. The optimized LZNMLNs-gel exhibited significantly higher permeation of LZ (1.46-fold) and NM (1.55-fold) than LZNM gel. The optimized LZNMLNs-gel showed significantly higher antifungal activity (ZOI = 34 ± 2 mm) than commercial Candid V gel (18 ± 1 mm). The optimized LZNMLNs-gel did not show any cytotoxicity against vaginal epithelial cells. The bioavailability of LZNMLNs-gel was significantly ( < 0.05) increased (1.94-fold for LZ and 1.33-fold for NM) compared to Candid V, with a decrease in total clearance indicating sustained release of the drug, which may lead to the maintenance of therapeutic concentration for an extended period. antifungal activity showed that the optimized LZNMLNs-gel completely treated the infection on the 7th day of treatment in an induced rabbit model, compared to the commercial gel (Candid V gel, 10 days). Based the findings, it can be concluded that LN-laden gel is an alternative carrier for improvement of the topical delivery of drugs for the treatment of vaginal candidiasis.
基于脂质的纳米载体系统是一种通过局部给药递送难溶性药物的新技术。本研究开发了一种载有双药（卢立康唑：LZ，和烟酰胺：NM）的脂质纳米载体（LN）的凝胶，用于治疗阴道念珠菌病。通过薄膜水化技术，使用胆固醇和大豆α-卵磷脂制备了LN。优化后的LZNMLN的平均囊泡大小、多分散指数和zeta电位分别为126.40±1.30nm、0.276和-34.6±0.8mV，并且该制剂显示两种药物在较长时间内持续释放。将选定的LZNMLN掺入生物粘附凝胶中。优化后的LZNMLN凝胶表现出优异的粘度、铺展性和生物粘附性。优化后的LZNMLN凝胶显示LZ（1.46倍）和NM（1.55倍）的渗透显著高于LZNM凝胶。优化后的LZNMLN凝胶显示出比市售的Candid V凝胶（18±1mm）显著更高的抗真菌活性（抑菌圈=34±2mm）。优化后的LZNMLN凝胶对阴道上皮细胞未显示任何细胞毒性。与Candid V相比，LZNMLN凝胶的生物利用度显著（<0.05）提高（LZ为1.94倍，NM为1.33倍），总清除率降低表明药物持续释放，这可能导致治疗浓度在较长时间内维持。抗真菌活性表明，与市售凝胶（Candid V凝胶，10天）相比，优化后的LZNMLN凝胶在诱导兔模型中治疗第7天完全治愈了感染。基于这些发现，可以得出结论，载有LN的凝胶是改善用于治疗阴道念珠菌病的药物局部给药的替代载体。
