Transdermal metformin hydrochloride-loaded cubic phases: in silico formulation optimization, preparation, properties, and application for local treatment of melanoma

Drug Delivery

Wei Zhou¹  Hongmei Wang¹  Yiguang Jin¹  Junhui Fu¹  Sheng Lu²  Xiang Yu³ 

[1] Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, Chin;Department of Pharmacy, First Hospital of Huzhou, First Affiliated Hospital of Huzhou University, Huzhou, China;Department of Pharmacy, First Hospital of Huzhou, First Affiliated Hospital of Huzhou University, Huzhou, China;Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, Chin;

关键词: Apoptosis;    cubic phase;    in silico;    metformin hydrochloride;    melanoma;    transdermal delivery;   

DOI  :  10.1080/10717544.2019.1587046

来源: publisher

【 摘 要 】

Metformin hydrochloride (Met) is commonly used for antidiabetic therapy though its antimelanoma action is also reported. Conventional oral administration method of Met is not appropriate for therapy of melanoma because of large dose, adverse reactions, and low efficiency. Here, a transdermal Met-loaded cubic phase was developed for local treatment of melanoma. In silico formulation optimization of the cubic phases was done, and the corresponding formulations were prepared and characterized. The optimized formulations were screened based on the stable microstructure and proper fluidity. Highly efficient mouse skin permeability of Met was found with the cubic phases compared to Met solutions. High antimelanoma effect of transdermal Met-loaded cubic phases also was shown by the significant decrease of tumor volume and the improvement of melanoma cell apoptosis on the B16 melanoma mice. Met-loaded cubic phases are a promising topically applied medication for local therapies of melanoma.

【 授权许可】

CC BY