Characterization of cubosomes as a targeted and sustained transdermal delivery system for capsaicin.
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.
Guangdong Medical University, Dongguan, People's Republic of China.
Xinsheng
X
Peng
Guangdong Medical University, Dongguan, People's Republic of China.
Yanfang
Y
Zhou
The Second Affiliated Hospital of Guangzhou Medical University, Guangdong, People's Republic of China ; School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangdong, People's Republic of China.
Ke
K
Han
School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangdong, People's Republic of China.
Lingzhen
L
Qin
Guangdong Medical University, Dongguan, People's Republic of China.
Linghui
L
Dian
Guangzhou Neworld Pharmaceuticals Co. Ltd., Guangzhou, Guangdong, People's Republic of China.
Ge
G
Li
School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangdong, People's Republic of China.
Xin
X
Pan
School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangdong, People's Republic of China.
Chuanbin
C
Wu
D000279:Administration, Cutaneous; D000818:Animals; D002211:Capsaicin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D004058:Diffusion; D004337:Drug Carriers; D004355:Drug Stability; D004655:Emulsions; D005233:Fatty Alcohols / Q000737:chemistry* / Q000633:toxicity; D005989:Glycerides / Q000737:chemistry* / Q000633:toxicity; D007700:Kinetics; D051379:Mice; D046529:Microscopy, Electron, Transmission; D009824:Ointments; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry* / Q000633:toxicity; D017207:Rats, Sprague-Dawley; D053838:Scattering, Small Angle; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D005233:Fatty Alcohols; D005989:Glycerides; D009824:Ointments; D020442:Poloxamer; C508873:3,7,11,15-tetramethyl-1,2,3-hexadecanetriol; C005953:monoolein; D002211:Capsaicin
capsaicin; cubosomes; skin-targeted delivery