Targeting delivery and minimizing epidermal diffusion of tranexamic acid by hyaluronic acid-coated liposome nanogels for topical hyperpigmentation treatment
Ying Liu,
Yue Han,
Tingting Zhu,
Xianglei Wu,
Wenxin Yu,
Jiafang Zhu,
Ying Shang,
Xiaoxi Lin,
Tianlan Zhao
Affiliations
Ying Liu
Department of Plastic and Cosmetic Surgery, The Second Affiliated Hospital of Soochow University
Yue Han
Department of Plastic and Cosmetic Surgery, The Second Affiliated Hospital of Soochow University
Tingting Zhu
Department of Dermatology, The First Affiliated Hospital of Soochow University
Xianglei Wu
Department of Laser and Aesthetic Medicine, Department of Plastic and Reconstructive Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine
Wenxin Yu
Department of Laser and Aesthetic Medicine, Department of Plastic and Reconstructive Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine
Jiafang Zhu
Department of Laser and Aesthetic Medicine, Department of Plastic and Reconstructive Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine
Ying Shang
Department of Laser and Aesthetic Medicine, Department of Plastic and Reconstructive Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine
Xiaoxi Lin
Department of Laser and Aesthetic Medicine, Department of Plastic and Reconstructive Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine
Tianlan Zhao
Department of Plastic and Cosmetic Surgery, The Second Affiliated Hospital of Soochow University
Hyperpigmentation is a common complaint and distressing problem in dermatology, and tranexamic acid (TA) is an effective treatment agent but limited by the delivery to melanocytes in the epidermis. Herein, a novel TA naogels (named HA/TA-LP), combining the advantages of liposomes and hyaluronic acid (HA), are prepared and assessed for topical hyperpigmentation treatment with targeting delivery and minimizing epidermal diffusion. Morphological characteristics indicate numerous TA-loaded liposomes packed in HA gels. In vitro cell studies using human A375 melanoma cells show that HA/TA-LP can promote the uptake of TA by targeting delivery with resulting inhibition of tyrosinase activity and melanin production. Guinea pigs are used to construct hyperpigmentation models and investigate the topical delivery and treatment efficacy of HA/TA-LP. In vivo topical delivery studies indicate HA/TA-LP realize the effective delivery into melanocytes with an ideal balance of effective permeability and minimizing epidermal diffusion. Subsequently, hyperpigmentation treatment assessments reveal that HA/TA-LP inhibit tyrosinase activity and melanin production under the radiation of UVB. Our study identifies favorable properties of HA/TA-LP for treating hyperpigmentation, and provides an experimental basis for further clinical application.
