Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, South Africa.
Afrigen Biologics (Pty) Limited, Formulation Development, Cape Town, South Africa.
Expert Opin Drug Deliv. 2021 Jun;18(6):789-801. doi: 10.1080/17425247.2021.1867533. Epub 2021 Jan 3.
Oral administration of statins for the treatment of familial hypercholesterolemia results in poor therapeutic outcomes and patient compliance. An alternative administration route is proposed to circumvent the current limitations. This research is aimed at developing nano-emulsions and nano-emulgels as the ultimate potential delivery systems of statins for administration the transdermal route.
Oil-in-water (o/w) nano-formulations (nano-emulsions and nano-emulgels) containing 2% (w/w) of the selected statin and 8% apricot kernel oil as oil phase were formulated. The nano-formulations were characterized using transmission electron microscopy (TEM), pH, viscosity, droplet size and zeta-potential.
Nano-emulsions' and nano-emulgels' droplet size ranged between 114.23-169.83 nm and 149.83-267.53 nm, respectively. The addition of Carbopol® Ultrez 20 increased the nano-emulsions' viscosity (3.59-8.38 cP) resulting in the formation of nano-emulgels (viscosity: 1911.00-46,090.00 cP). The entrapment efficiency (90.77-99.55%) confirmed the incorporation of the statins. Membrane release studies indicated that statins were released at higher flux values in nano-emulsions compared to their respective nano-emulgels. (skin diffusion) studies indicated higher median values in the nano-emulgels compared to their nano-emulsion counterparts.
The results indicate the benefits of nano-emulsions and nano-emulgels as potential alternative delivery systems for the transdermal delivery of statins.
口服他汀类药物治疗家族性高胆固醇血症的治疗效果不佳，患者依从性也较差。因此，提出了一种替代给药途径来规避当前的局限性。本研究旨在开发纳米乳液和纳米乳凝胶作为他汀类药物经皮给药的最终潜在递药系统。
制备含 2%（w/w）选定他汀类药物和 8%杏仁油的油包水（o/w）纳米制剂（纳米乳液和纳米乳凝胶）作为油相。采用透射电子显微镜（TEM）、pH 值、黏度、粒径和 Zeta 电位对纳米制剂进行表征。
纳米乳液和纳米乳凝胶的粒径分别为 114.23-169.83nm 和 149.83-267.53nm。加入 Carbopol®Ultrez 20 可增加纳米乳液的黏度（3.59-8.38cP），从而形成纳米乳凝胶（黏度：1911.00-46090.00cP）。包封效率（90.77-99.55%）证实了他汀类药物的掺入。膜释放研究表明，与相应的纳米乳凝胶相比，他汀类药物在纳米乳液中的释放通量值更高。（皮肤扩散）研究表明，纳米乳凝胶的中位数高于其纳米乳液对应物。
结果表明，纳米乳液和纳米乳凝胶作为他汀类药物经皮给药的潜在替代递药系统具有优势。
