Formulation development, optimization, and characterization of anti-fungal topical biopolymeric film using a niosomal approach

Background: Griseofulvin is an antifungal drug that is currently available in the market only in oral dosage forms. So, the development of topical treatment could be advantageous for the treatment of superficial fungal infections. Though for superficial fungal treatment, the skin acts as a major target as well as a principal barrier for drug delivery. To overcome this the colloidal carrier system niosome was used. Niosomes being in the nanometer size range would allow the delivery of the drug at the desired site. Niosomes being non-ionic surfactant-based vehicles would facilitate the passage of the drugs through as skin is composed of both lipid and aqua, which would create problems for any other delivery system.
Methodology: Griseofulvin belonging to the BCS Class II was formulated in the form of niosomes to enhance the drug’s solubility. In this study, optimization of niosomal formulation was done using OVAT (one variable at a time) method. Here, the CMAs (critical material attributes) such as surfactant type, conc. of charge inducer and the ratio of surfactant: cholesterol and CPPs (critical processing parameters) such as rotational speed of evaporator flask, external phase temperature, hydration time, and external phase volume (both aqueous and organic), which are independent variables influencing factors at different levels. These are said to have a potential risk on the CQAs (critical quality attributes), which are dependent variables, such as vesicle size, vesicle shape, vesicle lamellarity, niosome aggregation, and drug entrapment efficiency, for the final selection of improved optimum batch. The films were prepared from the incorporation of griseofulvin-loaded optimized niosomes in chitosan film for topical drug delivery in superficial fungal infections.
Characterization: The films properties were characterized by physical appearance, film thickness, weight variation, folding endurance, tensile strength, moisture, uptake, moisture content, drug content uniformity, In-vitro drug diffusion studies, ex-vivo studies, and antifungal efficacy against Candida albicans sp.
Result and Discussion: Thus, chitosan film formulation integrating griseofulvin-loaded niosomes for topical delivery enhanced the solubility of the drug and avoided the side effects associated with the orally-administered marketed formulation.
Conclusion: Biopolymer chitosan exhibited antifungal activity implying enhanced drug efficacy. Therefore, two concepts of using optimized vesicular carrier systems and biopolymeric films have been combined and this topical novel composite film having the potential for griseofulvin delivery to superficial fungal infections has been formulated.