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Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization

Authors Jung IW, Han HK

Received 22 January 2014

Accepted for publication 23 March 2014

Published 12 May 2014 Volume 2014:9(1) Pages 2299—2306

DOI https://doi.org/10.2147/IJN.S61181

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Il-Woo Jung, Hyo-Kyung Han

College of Pharmacy, Dongguk University-Seoul, Ilsan-Donggu, Goyang, Republic of Korea

Abstract: In this work, we aimed to develop chitosan-coated mucoadhesive liposomes ­containing risedronate to improve intestinal drug absorption. Liposomes containing risedronate were prepared with 1,2-distearoryl-sn-glycero-3-phosphocholine and distearoryl-sn-glycero-3-[phospho-rac-(1-glycerol)] using the freeze-drying method, with subsequent coating of the anionic surfaces of the liposomes with chitosan. The in vitro characteristics of the chitosan-coated liposomes were investigated, including their stability, mucoadhesiveness, and Caco-2 cell permeability. This formulation was stable in simulated gastric and intestinal fluids, with the percentage of drug remaining in the liposomes being more than 90% after 24 hours of incubation. Chitosan-coated liposomes also showed strong mucoadhesive properties, implying potential electrostatic interaction with the mucous layer in the gastrointestinal tract. Compared with the untreated drug, chitosan-coated liposomes significantly enhanced the cellular uptake of risedronate, resulting in an approximately 2.1–2.6-fold increase in Caco-2 cells. Further, the chitosan-coated liposomes increased the oral exposure of risedronate by three-fold in rats. Taken together, the results of this study suggest that chitosan-coated liposomes containing risedronate should be effective for improving the bioavailability of risedronate.

Keywords: cellular uptake, bioavailability, mucoadhesiveness, liposome, chitosan

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