In vitro, ex vivo, and in vivo studies of binary ethosomes for transdermal delivery of acyclovir: A comparative assessment

The study investigated a comparative assessment of binary ethosomes (ETHOs) and elastic liposomes (ELPs) for transdermal delivery of acyclovir sodium (ACV-Na). Optimized binary ETHO (ETHO2) and ELPs (ELP3) were evaluated for vesicle size, entrapment efficiency, elasticity, extruded volume, in vitro drug release, morphology, ex vivo skin permeation, and drug deposition (albino rat skin). In vivo studies were performed to evaluate transepidermal water loss (TEWL) and skin irritation. The components of ELP3 and ETHO2 (ethanol, propylene glycol, Tween 80, lipids) had a significant impact on in vitro and in vivo parameters. ETHO2 showed convincing findings as compared to ELP3. The permeation steady-state flux (J(ss)) and enhancement ratio (E-R) were significantly (p<0.05) enhanced in ETHO2 (J(ss) = 87.6 +/- 4.8 mu g/cm(2)/h and ER = 7.3) as compared to drug solution (DS) (J(ss) = 12 +/- 2.6 mu g/cm(2)/h) and marketed cream (Jss = 52 +/- 7.0 mu g/cm(2)/h and ER = 4.3). The findings of TEWL and scanning electron microscopy confirmed better permeation of ETHO2. Hemolysis and Draize studies confirmed the hemocompatibility and non-irritant behavior of formulations, respectively. Conclusively, ETHO2 can be a suitable alternative to classical vesicular systems for transdermal application against infections caused by the herpes simplex virus.

Automated summary

The study compared the performance of ETHO2 and ELP3 for transdermal delivery of acyclovir sodium and found that ETHO2 outperformed ELP3 with significantly enhanced permeation flux and enhancement ratio.