Design, Optimization and Characterization of a Transferosomal Gel of Acyclovir for Effective Treatment of Herpes Zoster
A transferosome is the first generation of an elastic liposome prepared from phospholipids and edge activators. An edge activator is often a single-chain surfactant with a high radius of curvature that destabilizes the lipid bilayers of vesicles and increases the deformability of the bilayers, thereby making the vehicle ultra-deformable. Acyclovir is a synthetic purine nucleoside analog derived from guanine, is the most widely used antiviral agent. It is effective in the treatment of herpes simplex virus (HSV), mainly HSV-1 and HSV-2 and varicella-zoster virus. However, it has low skin permeability. Hence, the objective of this study was to prepare acyclovir using transferosomes to overcome the barrier function of the skin. The present study deals with the development of transferosomal gel containing acyclovir by handshaking method for painless acyclovir delivery for use in the treatment of skin disease through 33 Fractional factorial design in which amount of Phospholipid (A), Cholesterol (B) and Tween 80 (C) was selected as independent variables and vesicle size (X1) Polydispersity index (X2) and %entrapment efficiency (X3) as dependent variables. The prepared transferosomes were evaluated with respect to entrapment efficiency (EE %), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of acyclovir transferosomes was incorporated into a Carbapol 934 gel base which was evaluated for drug content, pH, spreadability, viscosity and in vitro permeation. The prepared acyclovir transferosomes had a high EE% ranging from 65 to 81%, with small particle sizes ranging from 181.9 to 401.8nm. The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. The formulation TF2 have better in-vitro drug release profile which contains carbopol 980 concentration 2 %w/w. The kinetic analysis of release profiles of TF2 was found to follow the Korsmeyer-Peppas model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). Therefore, acyclovir in the form of transferosomes can penetrate the skin, overcoming the stratum corneum barrier.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (SeeÂ The Effect of Open Access).