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Preparation, evaluation and metabolites study in rats of novel Isoginkgetin-loaded TPGS/soluplus mixed nanomicelles
Xue Feng1, Yu-Ting Chen1, Lu-Ya Li1
1Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, No.361, Zhongshan Road, Shijiazhuang 050017, PR China.
Abstract:
At present, cancer is one of the most lethal diseases in the world, and researchers are committed to developing effective anticancer drugs. Isoginkgetin (IGG) is a kind of biflavone with the potential to treat cancer due to the features of altering the cell cycle and inhibiting tumor cell infiltration. However, its solubility, absorbability and bioavailability are poor, so in this study, IGG was prepared into mixed nanomicelles and evaluated in vitro and in vivo. After condition optimization, IGG-loaded TPGS/soluplus mixed nanomicelles with particle size of 62.34 ± 1.10 nm, entrapment efficiency of 96.92 ± 0.66% and drug loading of 2.42 ± 0.02% were successfully prepared. The physicochemical properties of the nanomicelles were stable within 60 days, and the cytotoxicity of the nanomicelles was significantly higher than that of IGG. The metabolism results showed that 32 kinds of metabolites of IGG and 21 kinds of IGG-loaded nanomicelles were detected. The metabolites of IGG can only be detected in feces of rats, while the metabolites of IGG-loaded nanomicelles can be detected in plasma, bile, urine and feces. All these indicated that after prepared into nanomicelles, the stability, solubility, cytotoxicity and bioavailability of IGG were increased significantly, which provided a new choice for the development of new drugs.
Insights
Researchers developed Isoginkgetin (IGG) nanomicelles to improve anticancer drug delivery. The novel nanomicelles demonstrated enhanced stability, solubility, cytotoxicity, and bioavailability compared to IGG alone.
Area of Science:
- Pharmacology
- Materials Science
- Oncology
Background:
- Cancer remains a leading cause of mortality worldwide, necessitating novel therapeutic strategies.
- Isoginkgetin (IGG), a biflavone, shows promise as an anticancer agent by modulating cell cycle and inhibiting tumor infiltration.
- Poor solubility, absorbability, and bioavailability limit IGG's clinical application.
Purpose of the Study:
- To formulate Isoginkgetin (IGG) into mixed nanomicelles to enhance its physicochemical properties and therapeutic efficacy.
- To evaluate the in vitro and in vivo performance of IGG-loaded nanomicelles.
Main Methods:
- Optimization of formulation conditions for IGG-loaded TPGS/Soluplus mixed nanomicelles.
- Characterization of nanomicelles, including particle size, entrapment efficiency, and drug loading.
- Assessment of physicochemical stability, in vitro cytotoxicity, and in vivo metabolism and bioavailability.
Main Results:
- Successfully prepared stable IGG-loaded nanomicelles (62.34 ± 1.10 nm) with high entrapment efficiency (96.92 ± 0.66%) and drug loading (2.42 ± 0.02%).
- Nanomicelles exhibited significantly enhanced cytotoxicity compared to free IGG.
- Metabolism studies revealed increased systemic distribution and bioavailability of IGG when formulated as nanomicelles, with metabolites detected in plasma, bile, urine, and feces.
Conclusions:
- Formulation of IGG into mixed nanomicelles significantly improves its stability, solubility, cytotoxicity, and bioavailability.
- This nanomicellar formulation offers a promising new approach for developing effective anticancer drugs based on Isoginkgetin.
