Fluconazole-loaded solid lipid nanoparticles topical gel for treatment of pityriasis versicolor: formulation and clinical study

Drug Delivery

Hoda A. Salem¹  Yasmina Ahmed El-Attar²  Maii Atef Shams Eldeen³  Ehab R. Bendas⁴  Mohamed A. El-Nabarawi⁵  Shaimaa El-Housiny⁶  Dalia Attia⁷ 

[1] Department of Clinical Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt;Department of Dermatology and venereology, Faculty of Medicine, Tanat University, Tanta, Egypt;Department of Microbiology, Faculty of Medicine, Tanta University, Tanta, Egypt;Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt;Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egyp;Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Modern University for Technology and Information, Cairo, Egypt;Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, The British University in Egypt (BUE), Cairo, Egypt;

关键词: Fluconazole;    solid lipid nanoparticles;    topical delivery;    entrapment efficiency;    Carpabol 934;    Pityriasis Versicolor;    clinical study;   

DOI  :  10.1080/10717544.2017.1413444

来源: publisher

【 摘 要 】

Solid lipid nanoparticles (SLNs) are very potential formulations for topical delivery of antifungal drugs. Hence, the purpose of this research was to formulate the well-known antifungal agent Fluconazole (FLZ)-loaded SLNs topical gel to improve its efficiency for treatment of Pityriasis Versicolor (PV). FLZ-SLNs were prepared by modified high shear homogenization and ultrasonication method using different concentration of solid lipid (Compritol 888 ATO, Precirol ATO5) and surfactant (Cremophor RH40, Poloxamer 407). The physicochemical properties and the in vitro release study for all FLZ-SLNs were investigated. Furthermore, the optimized FLZ-SLN formula was incorporated into gel using Carpobol 934. A randomized controlled clinical trial (RCT) of potential batches was carried out on 30 well diagnosed PV patients comparing to market product Candistan® 1% cream. Follow up was done for 4 weeks by clinical and KOH examinations. The results showed that FlZ-SLNs were almost spherical shape having colloidal sizes with no aggregation. The drug entrapment efficiency ranged from 55.49% to 83.04%. The zeta potential values lie between −21 and −33 mV presenting good stability. FLZ showed prolonged in vitro release from SLNs dispersion and its Carbapol gel following Higuchi order equation. Clinical studies registered significant improvement (p < .05) in therapeutic response (1.4-fold; healing%, 4-fold; complete eradication) in terms of clinical cure and mycological cure rate from PV against marketed cream. Findings of the study suggest that the developed FLZ loaded SLNs topical gels have superior significant fast therapeutic index in treatment of PV over commercially available Candistan® cream.

【 授权许可】

CC BY