Brucine-loaded transliposomes nanogel for topical delivery in skin cancer: statistical optimization, in vitro and dermatokinetic evaluation

The aim of the present study was to develop, optimize brucine-loaded transliposomes (BRC-TL) formulation for dermal delivery of brucine for skin cancer. The BRC-TL formulations were evaluated for vesicle size, entrapment efficiency, and in vitro drug release. The optimized formulation was further evaluated for skin penetration by confocal laser microscopy and dermatokinetic study.

The optimized BRC-TL formulation presented sealed lamellar shaped vesicles, with vesicles size, polydispersity index, entrapment efficiency, and in vitro drug release of 136.20 ± 2.87 nm, 0.354 ± 0.02, 86.01 ± 1.27%, and 83.09 ± 2.07%, respectively. Ex vivo permeation study showed that, developed BRC-TL formulation had a 2.4-fold increment in permeation as compared to BRC suspension. Texture analysis showed that the BRC-TL gel presented firmness of 158.91 g, consistency of 615.03 g/s, cohesiveness of  − 115.26 g and a viscosity index of  − 472.05 g/s. The confocal images of rat skin clearly showed the deeper penetration of rhodamine B-loaded TL formulation as compared to the Rhodamine B-hydro alcoholic solution.

The optimized BRC-TL formulation demonstrated significantly higher cytotoxicity than placebo liposome and BRC suspension (P < 0.05). Further, the BRC-TL nanogel treated rat skin showed a substantial increase in C_{Skin max} and AUC_0–8 in comparison to rat skin treated with BRC conventional gel (P < 0.05). The data revealed that the developed TLs formulation could be a promising drug nanocarrier for brucine dermal delivery in the treatment of skin cancer.

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Article information: Alhakamy, N.A., Aldawsari, H.M., Ali, J. et al. Brucine-loaded transliposomes nanogel for topical delivery in skin cancer: statistical optimization, in vitro and dermatokinetic evaluation. 3 Biotech 11, 288 (2021). https://doi.org/10.1007/s13205-021-02841-5