Abstract
Topical liposomal drug formulations containing AS1411-aptamer conjugated liposomes were designed to deliver in a sustained way the 5-fluorouracil to the tumor site but also to increase the compliance of patients with basal cell carcinoma. The 5-fluorouracil penetrability efficiency through the Strat-M membrane and the skin irritation potential of the obtained topical liposomal formulations were evaluated in vitro and the Korsmeyer Peppas equation was considered as the most appropriate to model the drug release. Additionally, the efficiency of cytostatic activity for targeted antitumor therapy and the hemolytic capacity were performed in vitro. The obtained results showed that the optimal liposomal formulation is a crosslinked gel based on sodium alginate and hyaluronic acid containing AS1411-aptamer conjugated liposomes loaded with 5-fluorouracil, which appeared to have favorable biosafety effects and may be used as a new therapeutic approach for the topical treatment of basal cell carcinoma.
Highlights
Published: 11 June 2021The 5th most common cancer in humans is non-melanoma skin cancer, in 2018 having over 1 million diagnoses worldwide [1]
Liposomes composed of PC, Chol and DSPE-PEG-MAL were prepared, and aptamer AS1411 that targets tumor cells were conjugated onto the surface of liposomes
Topical formulations containing drug-loaded aptamer functionalized liposomes were manufactured by procedures that do not compromise the performance of the drug and which are reproducible
Summary
Published: 11 June 2021The 5th most common cancer in humans is non-melanoma skin cancer, in 2018 having over 1 million diagnoses worldwide [1]. There are some well-established treatments for these non-melanoma skin cancers, such as: curettage and electrodessication; Mohs micrographic surgery; excisional surgery; radiation; cryosurgery; photodynamic therapy; laser surgery and oral medicine [4,5,6]. These conventional treatments lead to severe inflammation, pain and unpleasant scarring [7]. In cases where the cancer has spread to large areas of the body, topical administration of anticancer drugs is recommended to reduce primarily the cost of surgery and unwanted scars and to increase patient compliance. The direct treatment with antitumoral drugs has a number of disadvantages as the toxicity of these drugs limits their dose, while rapid clearance from
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