Flexible liposomal gel dual-loaded with all-trans retinoic acid and betamethasone for enhanced therapeutic efficiency of psoriasis

被引:52
作者
Wang, Wei [1 ]
Shu, Gao-feng [2 ]
Lu, Kong-jun [2 ]
Xu, Xiao-ling [2 ]
Sun, Min-cheng [2 ]
Qi, Jing [2 ]
Huang, Qiao-ling [1 ]
Tan, Wei-qiang [3 ]
Du, Yong-zhong [2 ]
机构
[1] Third Peoples Hosp Hangzhou, Dept Pharm, 38 West Lake Ave, Hangzhou 310009, Peoples R China
[2] Zhejiang Univ, Inst Pharmaceut, Coll Pharmaceut Sci, 866 Yuhangtang Rd, Hangzhou 310058, Peoples R China
[3] Zhejiang Univ, Sir Run Run Shaw Hosp, Dept Plast Surg, Sch Med, 3 East Qingchun Rd, Hangzhou 310016, Peoples R China
关键词
Flexible liposomes; All trans-retinoic acid; Betamethasone; Enhanced anti-psoriatic efficacy; SKIN INFLAMMATION; DELIVERY; FORMULATION; TRETINOIN; COMBINATION; EXPRESSION; CARRIERS; ACNE;
D O I
10.1186/s12951-020-00635-0
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Background Psoriasis is a chronic immune-mediated inflammatory skin disease without effective treatment. The utilization of all trans-retinoic acid (TRA) and betamethasone (BT) for the treatment of psoriasis is still facing difficulties, due to their relatively poor stability, limited skin permeation, and systemic side effects. Flexible liposomes are excellent in deeper skin permeation and reducing the side effects of drugs, which is promising for effective treatment of skin disorders. This work aimed to establish dual-loaded flexible liposomal gel for enhanced therapeutic efficiency of psoriasis based on TRA and BT. Results Flexible liposomes co-loaded with TRA and BT were successfully prepared in our study. The characterization examination revealed that flexible liposomes featured nano-sized particles (around 70 nm), high drug encapsulation efficiency (> 98%) and sustained drug release behaviors. Flexible liposomes remarkably increased the drug skin permeation and retention as compared with free drugs. Results on HaCaT cells suggested that flexible liposomes were nontoxic, and its cellular uptake has a time-dependent manner. In vivo studies suggested the topical application of TRA and BT dual-loaded liposomal gel had the best ability to reduce the thickness of epidermal and the level of cytokines (TNF-alpha and IL-6), largely alleviating the symptoms of psoriasis. Conclusions Flexible liposomal gel dual-loaded with TRA and BT exerted a synergistic effect, which is a promising topical therapeutic for the treatment of psoriasis.
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页数:14
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