Drug Delivery Research Laboratory, Department of Pharmaceutical sciences, Dr. H. S. Gour Viswavidyalaya, Sagar-470003, MP, India.
Pharm Dev Technol. 2013 May-Jun;18(3):550-9. doi: 10.3109/10837450.2011.598161. Epub 2011 Aug 3.
Dermal delivery of fluconazole (FLZ) is still a major limitation due to problems relating to control drug release and achieving therapeutic efficacy. Recently, solid lipid nanoparticles (SLNs) were explored for their potential of topical delivery, possible skin compartments targeting and controlled release in the skin strata. The retention and accumulation of drug in skin is affected by composition of SLNs. Hence, the aim of this study was to develop FLZ nanoparticles consisted of various lipid cores in order to optimize the drug retention in skin. SLNs were prepared by solvent diffusion method and characterized for various in vitro and in vivo parameters. The results indicate that the SLNs composed of compritol 888 ATO (CA) have highest drug encapsulation efficiency (75.7 ± 4.94%) with lower particle size (178.9 ± 3.8 nm). The in vitro release and skin permeation data suggest that drug release followed sustained fashion over 24 h. The antifungal activity shows that SLNs made up of CA lipid could noticeably improve the dermal localization. In conclusion, CA lipid based SLNs are represents a promising carrier means for the topical treatment of skin fungal infection as an alternative to the systemic delivery of FLZ.
由于与控制药物释放和达到治疗效果相关的问题，氟康唑（FLZ）的经皮给药仍然是一个主要的限制。最近，固体脂质纳米粒（SLNs）因其在局部递药、可能的皮肤隔室靶向和在皮肤层中控制释放的潜力而受到探索。药物在皮肤中的保留和积累受 SLNs 组成的影响。因此，本研究的目的是开发由各种脂质核组成的 FLZ 纳米粒，以优化药物在皮肤中的保留。通过溶剂扩散法制备 SLNs，并对其进行各种体外和体内参数的表征。结果表明，由 compritol 888 ATO（CA）组成的 SLNs 具有最高的药物包封效率（75.7±4.94%）和较小的粒径（178.9±3.8nm）。体外释放和皮肤渗透数据表明，药物释放在 24 小时内呈持续释放方式。抗真菌活性表明，由 CA 脂质组成的 SLNs 可显著改善皮肤定位。总之，CA 脂质基 SLNs 作为 FLZ 全身给药的替代方案，代表了皮肤真菌感染局部治疗的一种有前途的载体手段。
