Puri, Vinam. Design and development of topical formulations for ungual drug delivery of antifungal moieties. Retrieved from https://doi.org/doi:10.7282/t3-9g5d-8e31
DescriptionGlobally, the most prevalent fungal disturbance of the nail, that not only has physiological effects, but also negatively impacts the quality of life of the affected population, is known as onychomycosis. It occurs more commonly in toenails but also affects fingernails and causes the infected nails to become discolored, brittle and thickened. Systemic treatment is the most effective management approach so far but there is an increasing demand for effective topical approaches due to the adverse effects that may be accompanied with the former approach. Topical drug delivery systems are applied directly at the site of infection and could avoid the first pass metabolism and systemic toxicity that is associated with orally delivered antifungal drugs.
Several antifungal drugs such as polyenes, azoles and allylamines are being explored for delivery via topical formulations applied on the nail unit and they act by inhibiting fungal cell growth and multiplication at different stages of the cell cycle.
This research focused on exploring topical drug delivery systems for some of the most utilized antifungal agents from allylamines and azoles classes, terbinafine and econazole respectively. The research was guided by the quality by design (QbD) approach involving and formulations were developed by the optimization of the material attributes and process parameters that were critical for achieving the desired quality of the products.
Terbinafine hydrochloride (TBH) delivery was explored via polymeric nanospheres loaded into a hydrogel vehicle. This nano-gel delivery system was developed by assigning critical quality attributes (CQAs) to TBH nanospheres required to achieve the quality target product profile (QTPP). The delivery system evaluated for the nail delivery of econazole nitrate (ECN) was a polymeric film-forming and permeation enhancing lacquer. This investigation involved the development of a favorable nail lacquer by design of experiments (DoE) with varied critical material attributes (CMAs) to understand the impact of the type and quantities of the formulation excipients. Finally, the data generated while following the QbD based formulation development of these drug delivery systems was processed using a statistical software called JMP® which helped with the development of the patterns obtained with these experiments.
The results were successful ungual delivery of these antifungal drugs through optimized formulations that met the desired quality specifications for nail drug delivery.