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Published on: February 9, 2019
Fisetin-loaded nanocochleates: formulation, characterisation, in vitro anticancer testing, bioavailability and
Chellampillai Bothiraja1, Bhagwat D Yojana, Atmaram P Pawar
1Bharati Vidyapeeth University, Poona College of Pharmacy , Paud Road, Erandwane, Pune-411038, Maharashtra , India pounbothi@yahoo.com.
Background:
The natural flavonoid fisetin has shown anticancer properties but its in vivo administration remains challenging due its poor aqueous solubility and extensive in vivo metabolism. This juncture demands an effective, controlled release and safe formulation of fisetin would be a significant advance for the treatment of cancer.
Objectives:
Nanocochleates are unique lipid-based supramolecular assemblies composed of a negatively charged phospholipid and a divalent cation. The aim was to develop and evaluate fisetin-loaded nanocochleates to improve its therapeutic efficacy. Using the trapping method, fisetin-loaded dimyristoylphosphatidylcholine liposomal vesicles were converted into nanocochleates by the action of Ca(2+) ions. These nanocochleates were further evaluated for physicochemical, in vitro anticancer and haemolysis, pharmacokinetics and tissue distribution study in mice.
Results:
Stable rolled-up layers as well as elongated structure of nanocochleates possessing particle size and encapsulation efficiency (EE) of 275 + 4 nm and 84.31 ± 2.52%, respectively were obtained. Nanocochleates demonstrated safety and a sustained release of fisetin at physiological pH. A 1.3-fold improvement in vitro anticancer towards human breast cancer MCF-7 cells was observed. Pharmacokinetics studies in mice revealed that nanocochleates injected intraperitonially showed a 141-fold higher relative bioavailability. Moreover, a low tissue distribution was observed.
Conclusion:
Developed nanocochleates markedly improved anticancer efficacy, bioavailability and safety of fisetin. The nanocochleates technology would facilitate the administration of this flavonoid in the clinical setting.
Areas Covered:
In this research article, we focused on lipid-based supramolecular assembly 'nanocochleates' composed of negatively charged phospholipids and divalent cation as drug carrier for systemic delivery system and discussed their formulations, optimisation, characterization, in vitro and in vivo performance.
Insights
This study developed fisetin-loaded nanocochleates, improving the anticancer flavonoid
Area of Science:
- Nanotechnology
- Drug Delivery Systems
- Cancer Therapeutics
Background:
- Fisetin, a natural flavonoid, exhibits anticancer properties but faces challenges in administration due to poor solubility and metabolism.
- Effective, controlled-release, and safe fisetin formulations are crucial for advancing cancer treatment.
Purpose of the Study:
- To develop and evaluate fisetin-loaded nanocochleates to enhance fisetin's therapeutic efficacy.
- To improve the bioavailability and anticancer activity of fisetin through nanocochleate formulation.
Main Methods:
- Fisetin-loaded liposomal vesicles were converted into nanocochleates using Ca(2+) ions.
- Characterization included physicochemical properties, in vitro anticancer activity, haemolysis, pharmacokinetics, and tissue distribution studies in mice.
Main Results:
- Nanocochleates with a particle size of 275 ± 4 nm and 84.31 ± 2.52% encapsulation efficiency were successfully prepared.
- Fisetin nanocochleates demonstrated sustained release, improved in vitro anticancer activity by 1.3-fold against MCF-7 cells, and a 141-fold increase in relative bioavailability.
- The formulation exhibited safety with low tissue distribution.
Conclusions:
- The developed fisetin nanocochleates significantly enhanced anticancer efficacy, bioavailability, and safety.
- Nanocochleate technology offers a promising approach for the clinical administration of fisetin for cancer treatment.
