Development and characterization of effective topical liposomal system for localized treatment of cutaneous candidiasis.
The localized delivery of fluconazole (FLZ) by conventional therapy is a major impediment in achieving its therapeutic efficacy against skin infections, such as cutaneous candidiasis. Therefore, the present study was aimed to develop FLZ-loaded vesicular construct(s), such as liposomes and niosomes, incorporated into carbopol gel (1%; w/w) for sustained, localized application. The liposomes and niosomes were prepared by the lipid/nonionic surfactant-based dry-film hydration method and were characterized for different parameters. In addition, antifungal activity was carried out on experimentally induced cutaneous candidiasis in immunosuppressed albino rats. The results showed that the size of liposomes and niosomes was found to be 0.348 ± 0.054 and 0.326 ± 0.033 μm with encapsulation efficiency of 31.8 ± 1.36 and 27.6 ± 1.08%, respectively. The skin-retention studies of FLZ from in vitro and in vivo experiments showed significantly higher accumulation of drug in the case of liposomal gel. The in vivo localization studies in viable skin showed that liposomal gel could produce 14.2-fold higher drug accumulation, compared with plain gel, while it was 3.3-fold more in the case of an equivalent-dose application in the form of niosomal gel. The antifungal study also confirmed the maximum therapeutic efficacy of liposomal gel, as the lowest number of cfu/mL was recorded following liposomal FLZ application. The studies signify the potential of liposomal gel for topical delivery of FLZ with increased accumulation of drug in various strata of skin vis-a-vis through sustained release of drug could maintain the localized effect, resulting in an effective treatment of a life-threatening cutaneous fungal infection.
Gupta
Madhu
M
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour Vishwavidyalaya, Sagar, India.
Goyal
Amit K
AK
Paliwal
Shivani Rai
SR
Paliwal
Rishi
R
Mishra
Neeraj
N
Vaidya
Bhuvaneshwar
B
Dube
Devyani
D
Jain
Sanjay K
SK
Vyas
Suresh P
SP
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use; D001672:Biocompatible Materials / Q000737:chemistry / Q000378:metabolism; D002179:Candidiasis, Cutaneous / Q000188:drug therapy* / Q000662:veterinary; D016503:Drug Delivery Systems; D015725:Fluconazole / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use; D005782:Gels / Q000008:administration & dosage / Q000737:chemistry; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D008297:Male; D008422:Materials Testing; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism / Q000382:microbiology; D013501:Surface-Active Agents / Q000737:chemistry
D000935:Antifungal Agents; D001672:Biocompatible Materials; D005782:Gels; D008081:Liposomes; D013501:Surface-Active Agents; D015725:Fluconazole