Atorvastatin loaded glycerosomal patch as an effective transdermal drug delivery: optimization and evaluation

<b>Aim:</b> The study explores glycerosomes as effective vesicular systems for transdermal delivery of atorvastatin (ATO) to overcome drawbacks related to its oral administration. <b>Methodology:</b> The objectives of this study were to formulate, by thin-film hydration method, optimize using definitive screening design and evaluate ATO-loaded glycerosomes (ATOG) which were then incorporated into patch followed by the evaluation of glycerosomes containing different concentration of glycerol. <b>Results &amp; discussion:</b> Vesicle size, Polydispersity index (PDI), zeta potential, entrapment efficiency and loading capacity of spherical ATOG (0–30%w/w) showed 137.3–192d.nm, 0.292–0.403, -3.81 to-6.76mV, 80.03–92.77% and 5.80–6.40%, respectively. <i>In-vitro</i> release study showed sustained release, increased skin permeability and better cell viability than pure drug. ATOG patches showed greater skin permeability than pure drug and ATO-liposomal patches. <b>Conclusion:</b> The study concludes that ATOGs are promising for effective transdermal delivery. Glycerol is used in glycerosomes which gives elasticity to the vesicle and is a safe component. It increases fluidity and deformability of lipids, enhancing the penetration of vesicles in transdermal delivery. The drug atorvastatin is a selective inhibitor of HMG-CoA. Its oral bioavailability is only 14 % due to gastrointestinal pre-systemic clearance and hepatic first pass metabolism. The transdermal route is explored in the current article to overcome the oral route limitations. Atorvastatin loaded glycerosomes were prepared by thin film hydration method and evaluated for physicochemical characteristics, <i>in vitro</i>, <i>ex vivo</i> and cell line study. ATO-glycerosomes were incorporated into transdermal patch and evaluated for physicochemical characteristics. The results of <i>in vitro</i> and <i>ex vivo</i> studies concluded that the prepared drug delivery systems enhanced the permeation of drug through skin. The ATO loaded glycerosomes and ATOG transdermal patches were more stable than ATO loaded liposomes and liposomal incorporated transdermal patches at 2–8°C and 25 ± 2°C/65 ± 5% RH.