Title:Novel Luliconazole Spanlastic Nanocarriers: Development and Characterisation
Volume: 20
Issue: 6
Author(s): Shirleen Miriam Marques, Dikshita Ullas Chavan, Prashant Jivaji Bhide, Madhusudan Joshi, Lalit Kumar*Rupesh Kalidas Shirodkar*
Affiliation:
- Department of Pharmaceutics,
Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal- Karnataka, 576104,
India
- Department of Pharmaceutics, Goa College of Pharmacy, 18th June Road, Panaji - Goa, 403001, India
Keywords:
Spanlastics, luliconazole, antifungal, edge activator, dermal drug delivery, factorial design.
Abstract:
Background: The formulation of spanlastic vesicles of luliconazole can be used to overcome
its poor skin permeation and improve its antifungal efficacy.
Objective: In this study, we aimed to enhance the dermal delivery of luliconazole, an antifungal drug,
through spanlastic vesicles.
Methods: A 23 regular factorial design was employed, using the Design Expert® software for optimization.
The independent variables chosen were Span: Edge activator ratio, type of edge activator, and sonication
intensity and their effect on the dependent variables, i.e., entrapment efficiency, particle size, and
percentage of drug release after 8h were determined. Spanlastics were formulated by ethanol injection
method using Tween 80 as an edge activator.
Results: Spanlastics were found to possess sizes in the nano range with entrapment efficiencies between
77 - 88% with optimum zeta potential and polydispersity index indicating a stable formulation. Differential
scanning calorimetry, X-ray diffraction, and Fourier transform infrared studies revealed complete
encapsulation of the drug within the elastic carriers. The optimized spanlastic formulation was further
incorporated into a gel base and was found to be sufficiently viscous, spreadable, homogenous, showed
a prolonged release for up to 8h and was also found to be non-irritant. The in-vitro permeation study
revealed that the flux value obtained for luliconazole entrapped in the vesicular spanlastics (0.2292
mg/cm2.h) was also found to be higher than that of the marketed (0.1302 mg/cm2.h) and conventional
gel (0.1122 mg/cm2.h). The optimized gel formulation was also evaluated for its antimycotic activity.
Moreover, the optimized gel formulation also possessed a greater antimycotic activity against Candida
albicans. The spanlastics loaded hydrogel formulation was found to have a greater zone of inhibition in
comparison to the marketed formulation, thus proving to have optimum antifungal activity against Candida
albicans.
Conclusion: Collectively, the results revealed that spanlastics could be a potential nanocarrier for wellcontrolled
delivery and for targeting deeper skin layers, thus providing new opportunities for dermal
treatment.