Formulation and optimization of microsponge-loaded emulgel to improve the transdermal application of acyclovir-a DOE...

The cutaneous penetration of acyclovir from the conventional topical formulations such as cream and ointments is poor due to low water solubility and low octanol buffer partition coefficient of the drug. The present investigation was aimed to prepare acyclovir-loaded microsponge-based emulgel to improve its topical delivery. The microsponges were prepared by the quasi-emulsion diffusion method. The central composite design was employed to investigate the effect of changes in various formulation and process parameters on critical product attributes. Homogenization speed (X1), drug/polymer ratio (X2), and concentration of PVA (X3) were selected as independent variables while particle size,b% yield, % drug loading efficiency, % entrapment efficiency, the drug released at 0.25 h and 6 h were selected as response variables. The regression analysis proved a significant effect of all the independent variables on the dependent variables (p < 0.05). All the designed batches released more than 40% drug in less than 1 h and were also able to sustain the drug release for more than 6 h. Based on the solution suggested by the software, the optimized batch was prepared with 1000-rpm homogenization speed, 1.6:1 drug/polymer ratio, and 0.088% of PVA. The optimized microsponge-loaded emulgel had acceptable viscosity (10,897 to 12,416 centipoise), spreadability (32.5 to 36.57 g × cm/s), pH (between 6 and 7), and drug content (93 to 95%). The results of the ex vivo permeation study proved significant improvement in drug permeation from optimized microsponge-loaded emulgel compared to the marketed formulation (f2 < 50).