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Cyclodextrin nanoparticle bound oral camptothecin for colorectal cancer: Formulation development and optimization

AuthorsÜnal, Sedat; Aktas, Yesim; Benito, Juan M. ; Bilensoy, Erem
KeywordsColorectal Cancer
Oral Administration
Issue Date2020
CitationInternational journal of pharmaceutics 584 (2020)
AbstractChemotherapeutic drugs for colorectal cancer (CRC) which is currently the third most lethal cancer globally, are administered intravenously (iv) due to their low oral bioavailability resulting from their physicochemical properties. Non-selective biodistribution and difficulties of parenteral administration reduce treatment efficacy. The aim of this work is to develop cyclodextrin (CD) based cationic nanoparticles (NPs) for CRC treatment with model drug camptothecin (CPT) that can be administered orally, protecting CPT through gastrointestinal tract (GIT), accumulating at mucus layer and providing an effective local treatment for the tumor area. NPs using two different amphiphilic CDs were prepared and coated with polyethylenimine (PEI) or chitosan (CS) to obtain positively charged surface for all formulations. Pre-formulation studies resulted in optimal formulation, CPT loaded Poly-ß-CD-C6 NPs, with 135 nm diameter and zeta potential of + 40 mV. In vitro release study was designed to represent gastrointestinal pH and transit time revealing 52% of encapsulated CPT successfully delivered all the way to simulated colon. CPT bound to Poly-ß-CD-C6 NPs exhibited higher cytotoxicity on HT-29 cells compared to equivalent CPT in solution. Caco-2 cell permeability studies showed 276% increase in CPT permeability and significantly higher mucosal penetration in cationic CD nanoparticle form.
Publisher version (URL)http://dx.doi.org/10.1016/j.ijpharm.2020.119468
Identifiersdoi: 10.1016/j.ijpharm.2020.119468
issn: 1873-3476
Appears in Collections:(IIQ) Artículos
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