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Colloidal anticancer drugs bioavailabilities in oral administration models
V Moutardier1, F Tosini, P Vlieghe
1Departement de Chirurgie Oncologique, Centre Regional de Lutte contre le Cancer, Institut Paoli Calmettes, 232 Bd de Sainte Marguerite, Marseille 13009, France.
International Journal of Pharmaceutics
|June 24, 2003
Summary
Polymerised core liposomes show potential for oral anticancer drug delivery, enhancing permeation of 5-fluorouracil and methotrexate. Patient treatment history, like radiation, impacts drug absorption in the colon.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Gastroenterology
Background:
- Liposomes are utilized for drug delivery.
- Polymerised core liposomes offer potential advantages over classical liposomes.
- Gastrointestinal degradation and drug release are key considerations for oral liposomal formulations.
Purpose of the Study:
- To evaluate drug release and gastrointestinal degradation of polymerised core liposomes.
- To assess the encapsulation and permeation of vincristine, 5-fluorouracil (5-FU), and methotrexate (MTX) using liposomes.
- To investigate the impact of patient treatment history on drug bioavailability in the human colon.
Main Methods:
- Liposomes with a polymerised core were prepared.
- Drug encapsulation and release studies were conducted.
- In vitro studies used Caco-2 and TC7 cell lines.
- Ex vivo studies utilized 150 human colon tissue sections.
Main Results:
- Polymerised core liposomes exhibited slightly reduced drug release and GI degradation compared to classical liposomes.
- Liposomal formulation enhanced permeation of 5-FU and MTX within therapeutic ranges.
- Pre-operative radiation in patients increased drug tissue uptake in the excised human colon model.
- Prior chemotherapy modified transmucosal ion transport.
Conclusions:
- Liposomal encapsulation of anticancer drugs has variable effects on permeation.
- Oral anticancer treatment design should consider patient history, including radiation and chemotherapy.
- Nutritional and pharmacological factors are crucial for optimising oral anticancer therapies.