Quercetin deformable liposome: preparation and efficacy against ultraviolet B induced skin damages in vitro and in vivo.
Ultraviolet (UV) radiation has deleterious effects on cells through direct damage to DNA or through increasing generation of reactive oxygen species (ROS). The flavonol quercetin (Qu) provides cellular protection against UV radiation and the current investigation was carried out to develop a deformable liposome formulation of Qu to enhance its delivery into human skin and to improve its anti-UVB effect. The influence of surfactants (including Span 20, Tween 80 and sodium cholate) on the properties of Qu deformable liposomes was investigated. Liposomes composed of Qu, phosphatidylcholine (PC), cholesterol (Chol), and Tween 80 showed high entrapment efficiencies (80.41±4.22%), small particle sizes (132±14nm), high elasticity (10.48±0.71), and prolonged drug release. The cell viability in UVB-irradiated HaCaT cells increased to 89.89±4.5% at 24h and 78.8±3.19% at 48h following treatment with Qu defomable liposomes. The ROS and malondialdehyde (MDA) level were also reduced. The penetration rate was 3.8-fold greater than that of the Qu suspension. Moreover, the edema and inflammation was alleviated by Qu deformable liposomes. These results showed the potential of deformable liposomes to enhance the anti-UVB effects of Qu both in vitro and in vivo.
School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning Province 110016, PR China; School of Chinese Medicine, Faculty of Science, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong 999077, PR China.
Dan
D
Liu
Haiyang
H
Hu
Zhixiu
Z
Lin
Dawei
D
Chen
Yongyuan
Y
Zhu
Shengtao
S
Hou
Xiaojun
X
Shi
D016923:Cell Death / Q000187:drug effects / Q000528:radiation effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D006801:Humans; D042541:Intracellular Space / Q000187:drug effects / Q000378:metabolism / Q000528:radiation effects; D015603:Keratinocytes / Q000166:cytology / Q000187:drug effects / Q000528:radiation effects; D008081:Liposomes; D008315:Malondialdehyde / Q000378:metabolism; D010539:Permeability; D011794:Quercetin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017382:Reactive Oxygen Species / Q000378:metabolism; D012867:Skin / Q000166:cytology / Q000187:drug effects* / Q000473:pathology / Q000528:radiation effects*; D014466:Ultraviolet Rays / Q000009:adverse effects*
D008081:Liposomes; D017382:Reactive Oxygen Species; D008315:Malondialdehyde; D011794:Quercetin
Anti-UVB; Deformable liposome; HaCaT cells; Quercetin; ROS