Development of solid lipid nanoparticles based controlled release system for topical delivery of terbinafine hydrochloride.
Development of solid lipid nanoparticles based controlled release system for topical delivery of terbinafine hydrochloride.
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DOI：
10.1016/j.ejps.2013.03.013
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发表时间：
2013-05
期刊：
影响因子：
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通讯作者：
Harsha Vaghasiya;Abhinesh Kumar;K. Sawant
中科院分区：
文献类型：
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作者：
Harsha Vaghasiya;Abhinesh Kumar;K. Sawant
本研究旨在研制具有缓释和皮肤靶向性的盐酸特比萘芬固体脂质纳米粒。采用溶剂注射法制备载TH的SLN，并采用33因子设计进行优化。考察了药物脂质比、表面活性剂浓度和有机溶剂体积对包封率和粒径的影响。以期望值（0.945）为基础的最佳配方，其%EE为73.74%，PS为300 nm。将优化的SLN掺入卡波姆凝胶中，并评价药物含量、pH、体外释放、离体保留、体内药效学和稳定性研究。SLN分散体的释药符合Korsmeyer-Peppas模型，表明Fickian释药，而凝胶的释药符合Higuchi模型。通过大鼠腹部皮肤的离体研究表明，与市售产品相比，SLN具有皮肤保留能力。体内药效学研究表明，与商业产品相比，基于SLN的凝胶在较短的持续时间内降低了大鼠中白色念珠菌的真菌负荷。固体脂质纳米粒分散体和凝胶在冷藏条件下可稳定保存3个月。结论：卡波姆凝胶SLNs具有皮肤靶向性，有望成为治疗真菌性皮肤感染的理想载体。
The study describes the development and evaluation of solid lipid nanoparticles (SLNs) of terbinafine hydrochloride (TH) for sustained release and skin targeting. TH-loaded SLNs were prepared by solvent-injection technique and optimized using 33full-factorial design. Effect of drug:lipid ratio, surfactant concentration and volume of organic solvent were studied on % entrapment efficiency (%EE) and particle size (PS). The optimum formulation based on desirability (0.945) exhibited %EE of 73.74% and PS of 300nm. Optimized SLNs were incorporated into Carbopol gel and evaluated for drug content, pH, in vitro release, ex vivo retention, in vivo pharmacodynamic and stability studies. Drug release from SLNs dispersion followed Korsmeyer–Peppas model, indicating Fickian drug release, while that from the gel followed Higuchi model. The ex vivo studies through rat abdominal skin indicated skin retention ability of SLNs as compared to commercial product. In vivo pharmacodynamic studies showed that the SLNs based gel reduced fungal burden of Candida albicans in rats as compared to commercial product in shorter duration of time. The SLNs dispersion and gel exhibited physicochemical stability under refrigeration upto 3months. It was concluded that SLNs incorporated Carbopol gel had skin targeting ability and may serve as a promising carrier in treatment of fungal skin infections.