Enhanced Transdermal Peptide‐Modified Flexible Liposomes for Efficient Percutaneous Delivery of Chrysomycin A to Treat Subcutaneous Melanoma and Intradermal MRSA Infection

Author:

Cai Yue1,Chu Yuteng1,Gong Yubei1,Hong Yulu1,Song Fuhang2,Wang Hong13,Zhang Huawei1,Sun Xuanrong1ORCID

Affiliation:

1. Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals & College of Pharmaceutical Science Zhejiang University of Technology Hangzhou 310014 China

2. School of Light Industry Beijing Technology and Business University Beijing 100048 China

3. Key Laboratory of Marine Fishery Resources Employment & Utilization of Zhejiang Province Hangzhou 310014 China

Abstract

AbstractSuperficial skin diseases, including skin infections and tumors, are common healthcare burdens. In this study, the in vivo activity of chrysomycin A (CA) is explored, and a transdermal liposomal CA formulation is further constructed for the simultaneous treatment of cutaneous melanoma and cutaneous methicillin‐resistant Staphylococcus aureus (MRSA) infection. The prepared liposomes (TD‐LP‐CA) display a strong antitumor effect with an IC50 value of less than 0.1 µm in B16‐F10 cells, suppress the proliferation of MRSA with a minimum inhibitory concentration (MIC) of 1 µm, and eradicate established MRSA biofilms at 10× MIC in vitro. More importantly, TD‐LP‐CA shows enhanced stratum corneum (SC) penetration, reaching more than 500 µm beneath the skin's surface due to modification with the TD peptide, and demonstrates excellent subcutaneous tumor penetration after skin application in vivo. TD‐LP‐CA displays an excellent therapeutic effect against intradermal MRSA infection in mice after topical dermal administration, as well as a moderate inhibitory effect on subcutaneous melanoma with a 75% tumor inhibition rate. The liposomes prepared herein can be a promising carrier for transcutaneous CA transfer for the treatment of superficial diseases such as skin tumors and infections due to their ability to overcome the skin barrier.

Funder

National Natural Science Foundation of China

Publisher

Wiley

Subject

Pharmaceutical Science,Biomedical Engineering,Biomaterials

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