Versatile flexible micelles integrating mucosal penetration and intestinal targeting for effectively oral delivery of paclitaxel

Liu, Chao; Liu, Wei; Liu, Yanhong; Duan, Hongxia; Chen, Liqing; Zhang, Xintong; Jin, Mingji; Cui, Minhu; Quan, Xiuquan; Pan, Li-Bin; Hu, Jiachun; Gao, Zhonggao; Wang, Yan; Huang, Wei

doi:10.1016/j.apsb.2023.05.029

Cited by 9 publications

(2 citation statements)

References 62 publications

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“…BAL-PTX has some limitations, such as low bioavailability and poor solubility. 22 , 23 Following the screening of synergistic ratios, we developed lipid nanoparticles and performed subsequent experiments. The particle size of the BAL-PTX-LN sample was found to be 134.36 ± 3.18 nm through a single-factor experiment and CCD central combination optimization.…”

Section: Discussionmentioning

confidence: 99%

“… 20 , 21 The inherent challenges of low solubility and poor bioavailability of PTX and BAL persist as fundamental obstacles in the development of clinical therapeutic preparations, despite their significant medicinal value when combined. 15 , 22 , 23 To overcome these challenges and improve the characteristics of PTX and various drug combinations, the selection of a suitable co-loading delivery system is imperative. Progress in this area includes the development of solvent-free preparations, scalability assessment, and long-term stability evaluation.…”

Section: Introductionmentioning

confidence: 99%

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Construction and Evaluation of BAL-PTX Co-Loaded Lipid Nanosystem for Promoting the Anti-Lung Cancer Efficacy of Paclitaxel and Reducing the Toxicity of Chemotherapeutic Drugs

Chen,

Wei,

Yin

et al. 2024

IJN

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Purpose The present study aimed to develop a lipid nanoplatform, denoted as “BAL-PTX-LN”, co-loaded with chiral baicalin derivatives (BAL) and paclitaxel (PTX) to promote the anti-lung cancer efficacy of paclitaxel and reduce the toxicity of chemotherapeutic drugs. Methods BAL-PTX-LN was optimized through central composite design based on a single-factor experiments. BAL-PTX-LN was evaluated by TEM, particle size, encapsulation efficiency, hemolysis rate, release kinetics and stability. And was evaluated by pharmacokinetics and the antitumor efficacy studied both in vitro and in vivo. The in vivo safety profile of the formulation was assessed using hematoxylin and eosin (HE) staining. Results BAL-PTX-LN exhibited spherical morphology with a particle size of 134.36 ± 3.18 nm, PDI of 0.24 ± 0.02, and with an encapsulation efficiency exceeding 90%, BAL-PTX-LN remained stable after 180 days storage. In vitro release studies revealed a zero-order kinetic model of PTX from the liposomal formulation. No hemolysis was observed in the preparation group. Pharmacokinetic analysis of PTX in the BAL-PTX-LN group revealed an approximately three-fold higher bioavailability and twice longer t 1/2 compared to the bulk drug group. Furthermore, the IC 50 of BAL-PTX-LN decreased by 2.35 times (13.48 μg/mL vs 31.722 μg/mL) and the apoptosis rate increased by 1.82 times (29.38% vs 16.13%) at 24 h compared to the PTX group. In tumor-bearing nude mice, the BAL-PTX-LN formulation exhibited a two-fold higher tumor inhibition rate compared to the PTX group (62.83% vs 29.95%), accompanied by a ten-fold decrease in Ki67 expression (4.26% vs 45.88%). Interestingly, HE staining revealed no pathological changes in tissues from the BAL-PTX-LN group, whereas tissues from the PTX group exhibited pathological changes and tumor cell infiltration. Conclusion BAL-PTX-LN improves the therapeutic effect of poorly soluble chemotherapeutic drugs on lung cancer, which is anticipated to emerge as a viable therapeutic agent for lung cancer in clinical applications.

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Section: Discussionmentioning

confidence: 99%