Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization
Il-Woo Jung, Hyo-Kyung HanCollege of Pharmacy, Dongguk University-Seoul, Ilsan-Donggu, Goyang, Republic of KoreaAbstract: In this work, we aimed to develop chitosan-coated mucoadhesive liposomes ­containing risedronate to improve intestinal drug absorption. Liposomes containing risedronate...
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Dove Medical Press
2014
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oai:doaj.org-article:2fe75986b298483888cb65de8f4b7f142021-12-02T05:36:19ZEffective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization1178-2013https://doaj.org/article/2fe75986b298483888cb65de8f4b7f142014-05-01T00:00:00Zhttp://www.dovepress.com/effective-mucoadhesive-liposomal-delivery-system-for-risedronate-prepa-a16788https://doaj.org/toc/1178-2013 Il-Woo Jung, Hyo-Kyung HanCollege of Pharmacy, Dongguk University-Seoul, Ilsan-Donggu, Goyang, Republic of KoreaAbstract: 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, chitosanJung IWHan HKDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 2299-2306 (2014) |
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Medicine (General) R5-920 |
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Medicine (General) R5-920 Jung IW Han HK Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| description |
Il-Woo Jung, Hyo-Kyung HanCollege of Pharmacy, Dongguk University-Seoul, Ilsan-Donggu, Goyang, Republic of KoreaAbstract: 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 |
| format |
article |
| author |
Jung IW Han HK |
| author_facet |
Jung IW Han HK |
| author_sort |
Jung IW |
| title |
Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| title_short |
Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| title_full |
Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| title_fullStr |
Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| title_full_unstemmed |
Effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| title_sort |
effective mucoadhesive liposomal delivery system for risedronate: preparation and in vitro/in vivo characterization |
| publisher |
Dove Medical Press |
| publishDate |
2014 |
| url |
https://doaj.org/article/2fe75986b298483888cb65de8f4b7f14 |
| work_keys_str_mv |
AT jungiw effectivemucoadhesiveliposomaldeliverysystemforrisedronatepreparationandinvitroinvivocharacterization AT hanhk effectivemucoadhesiveliposomaldeliverysystemforrisedronatepreparationandinvitroinvivocharacterization |
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1718400286593122304 |