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Войти в исследования Drug development and industrial pharmacy · 2026
Development and Optimization of Baicalin-Loaded Transniosomes Using Quality by Design: Dermatokinetic and In Vivo Efficacy Evaluation.
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Aodah Alhussain H, Almutairy Bjad K, Foudah Ahmed I, Ansari Mohd Asif, Imran Mohd, Alam Aftab
Аннотация
OBJECTIVE: This study aimed to develop and optimize a baicalin-loaded transniosomal gel (BCL-TN) to enhance the dermal delivery and therapeutic efficacy of baicalin for the management of skin cancer.
SIGNIFICANCE: Baicalin possesses potent anticancer activity but exhibits poor skin permeability, which limits its clinical utility in topical oncology. A transniosomal gel system was therefore designed to improve cutaneous penetration and therapeutic performance.
METHODS: BCL-TN were prepared by the thin-film hydration technique and optimized for particle size, polydispersity index (PDI) and entrapment efficiency (%EE) using a Box-Behnken design (BBD). The optimized formulation was incorporated into a 1% w/v Carbopol 980 hydrogel and evaluated for physicochemical characteristics, in vitro drug release, and ex vivo skin permeation. Skin penetration depth was assessed by confocal laser scanning microscopy (CLSM), and in vivoantitumour efficacy was evaluated in a 7,12-dimethylbenz[a]anthracene (DMBA)/croton-oil-induced murine skin cancer model and compared with a marketed 5-fluorouracil cream.
RESULTS: The optimized BCL-TN gel exhibited a particle size of 100.5 ± 3.8 nm, a zeta potential of -25.84 ± 1.04 mV, and a PDI of 0.316 ± 0.12. Entrapment efficiency and drug loading were 87.16 ± 2.62% and 12.16 ± 1.06%, respectively, and the gel displayed a skin-compatible pH of 5.9. In vitro release studies showed a 2.53-fold increase in drug release compared with the baicalin suspension, while ex vivo skin permeation was 2.70-fold higher. CLSM demonstrated that the BCL-TN gel penetrated to a depth of approximately 30 µm, compared with only 10 µm for the baicalin suspension. In vivo evaluation revealed a significantly greater reduction in tumour size in animals treated with the BCL-TN gel than in those receiving the marketed formulation.
CONCLUSION: The BCL-TN gel is a promising transdermal delivery platform with considerable therapeutic potential for the treatment of skin cancer.
SIGNIFICANCE: Baicalin possesses potent anticancer activity but exhibits poor skin permeability, which limits its clinical utility in topical oncology. A transniosomal gel system was therefore designed to improve cutaneous penetration and therapeutic performance.
METHODS: BCL-TN were prepared by the thin-film hydration technique and optimized for particle size, polydispersity index (PDI) and entrapment efficiency (%EE) using a Box-Behnken design (BBD). The optimized formulation was incorporated into a 1% w/v Carbopol 980 hydrogel and evaluated for physicochemical characteristics, in vitro drug release, and ex vivo skin permeation. Skin penetration depth was assessed by confocal laser scanning microscopy (CLSM), and in vivoantitumour efficacy was evaluated in a 7,12-dimethylbenz[a]anthracene (DMBA)/croton-oil-induced murine skin cancer model and compared with a marketed 5-fluorouracil cream.
RESULTS: The optimized BCL-TN gel exhibited a particle size of 100.5 ± 3.8 nm, a zeta potential of -25.84 ± 1.04 mV, and a PDI of 0.316 ± 0.12. Entrapment efficiency and drug loading were 87.16 ± 2.62% and 12.16 ± 1.06%, respectively, and the gel displayed a skin-compatible pH of 5.9. In vitro release studies showed a 2.53-fold increase in drug release compared with the baicalin suspension, while ex vivo skin permeation was 2.70-fold higher. CLSM demonstrated that the BCL-TN gel penetrated to a depth of approximately 30 µm, compared with only 10 µm for the baicalin suspension. In vivo evaluation revealed a significantly greater reduction in tumour size in animals treated with the BCL-TN gel than in those receiving the marketed formulation.
CONCLUSION: The BCL-TN gel is a promising transdermal delivery platform with considerable therapeutic potential for the treatment of skin cancer.