Oral delivery of camptothecin using cyclodextrin/poly(anhydride) nanoparticles
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
MetadataShow full item record
AbstractCamptothecin (CPT), a molecule that shows powerful anticancer activity, is still not used in clinic due to its high hydrophobicity and poor active form's stability. In order to solve these drawbacks, the combination between poly(anhydride) nanoparticles and cyclodextrins was evaluated. CPT-loaded nanoparticles, prepared in the presence of 2-hydroxypropyl-β-cyclodextrin, (HPCD-NP) displayed a mean size close to 170nm and a payload of 50μg per mg (25 times higher than the one of the control nanoparticles). CPT was not released from nanoparticles under gastric conditions. However, under intestinal conditions, about 50% of the drug content was released as a burst, whereas the remained drug was released following a zero-order kinetic. Pharmacokinetic studies revealed that the CPT plasma levels, from orally administered nanoparticles, were high and sustained up to 48h. The CPT oral bioavailability was 7-fold higher than the value obtained with the control, whereas its clearance was significantly lower than for the aqueous suspension. These observations may be directly related to a prolonged residence time of nanoparticles in close contact with the intestinal epithelium, the presence of the cyclodextrin that decreases the CPT transformation into its inactive form and the generation of an acidic microenvironment during the degradation of the poly(anhydride) that would prevent the transformation of the active lactone into the inactive carboxylate conformation.
CitationHuarte, J., Espuelas, S., Lai, Y., He, B., Tang, JZ., Irache., JM. (2016) 'Oral delivery of camptothecin using cyclodextrin/poly(anhydride) nanoparticles', International Journal of Pharmaceutics, 506 (1-2) pp. 116-28
JournalInternational Journal of Pharmaceutics
The following license files are associated with this item:
- Increased oral bioavailability of paclitaxel by its encapsulation through complex formation with cyclodextrins in poly(anhydride) nanoparticles.
- Authors: Agüeros M, Zabaleta V, Espuelas S, Campanero MA, Irache JM
- Issue date: 2010 Jul 1
- Cyclodextrin/poly(anhydride) nanoparticles as drug carriers for the oral delivery of atovaquone.
- Authors: Calvo J, Lavandera JL, Agüeros M, Irache JM
- Issue date: 2011 Dec
- Comparative evaluation of polymeric and amphiphilic cyclodextrin nanoparticles for effective camptothecin delivery.
- Authors: Cirpanli Y, Bilensoy E, Lale Doğan A, Caliş S
- Issue date: 2009 Sep
- Antitumoral activity of camptothecin-loaded nanoparticles in 9L rat glioma model.
- Authors: Cırpanlı Y, Allard E, Passirani C, Bilensoy E, Lemaire L, Calış S, Benoit JP
- Issue date: 2011 Jan 17
- Bioadhesive properties and biodistribution of cyclodextrin-poly(anhydride) nanoparticles.
- Authors: Agüeros M, Areses P, Campanero MA, Salman H, Quincoces G, Peñuelas I, Irache JM
- Issue date: 2009 Jun 28