Characterization of cubosomes as a targeted and sustained transdermal delivery system for capsaicin

• Main Authors: Peng X, Zhou Y, Han K, Qin L, Dian L, Li G, Pan X, Wu C
• Format: Article
• Language: English
• Published: Dove Medical Press 2015-08-01
• Series: Drug Design, Development and Therapy
• Online Access: http://www.dovepress.com/characterization-of-cubosomes-as-a-targeted-and-sustained-transdermal--peer-reviewed-article-DDDT

Xinsheng Peng,1* Yanfang Zhou,1* Ke Han,2,3 Lingzhen Qin,3 Linghui Dian,1 Ge Li,4 Xin Pan,3 Chuanbin Wu3 1Guangdong Medical University, Dongguan, 2The Second Affiliated Hospital of Guangzhou Medical University, 3School of Pharmaceutical Sciences, Sun Yat-Sen University, 4Guangzhou Neworld Pharmaceuticals Co. Ltd., Guangzhou, Guangdong, People’s Republic of China*These authors contributed equally to this work Abstract: Phytantriol- and glycerol monooleate-based cubosomes were produced and characterized as a targeted and sustained transdermal delivery system for capsaicin. The cubosomes were prepared by emulsification and homogenization of phytantriol (F1), glycerol monooleate (F2), and poloxamer dispersions, characterized for morphology and particle size distribution by transmission electron microscope and photon correlation spectroscopy. Their Im3m crystallographic space group was confirmed by small-angle X-ray scattering. An in vitro release study showed that the cubosomes provided a sustained release system for capsaicin. An in vitro diffusion study conducted using Franz diffusion cells indicated that the skin retention of capsaicin from cubosomes in the stratum corneum was much higher (2.75±0.22 µg versus 4.32±0.13 µg, respectively) than that of capsaicin cream (0.72±0.13 µg). The stress testing showed that the cubosome formulations were stable under strong light and high temperature for up to 10 days. After multiapplications on mouse skin, the irritation of capsaicin cubosomes and cream was light with the least amount of side effects. Overall, the present study demonstrated that cubosomes may be a suitable skin-targeted and sustained delivery system for the transdermal administration of capsaicin. Keywords: cubosomes, skin-targeted delivery, capsaicin