Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement
Raloxifene (RXF) is a hormone-like medication used for treating postmenopausal osteoporosis and estrogen-dependent breast cancer, yet associated with bad low bioavailability due to poor solubility. This study was intended to develop cyclodextrin/chitosan nanoparticles (ccNPs) for oral delivery of RX...
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2018-06-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1999-4923/10/3/76 |
| _version_ | 1811305010314608640 |
|---|---|
| author | Zaihua Wang Yan Li |
| author_facet | Zaihua Wang Yan Li |
| author_sort | Zaihua Wang |
| collection | DOAJ |
| description | Raloxifene (RXF) is a hormone-like medication used for treating postmenopausal osteoporosis and estrogen-dependent breast cancer, yet associated with bad low bioavailability due to poor solubility. This study was intended to develop cyclodextrin/chitosan nanoparticles (ccNPs) for oral delivery of RXF in order to enhance the oral bioavailability. RXF-loaded ccNPs (RXF-ccNPs) were prepared by cyclodextrin inclusion followed by complexation with chitosan. RXF-ccNPs were fully characterized by particle size, morphology and in vitro drug release. The oral delivery efficacy and transepithelial transport potential were evaluated by pharmacokinetics, in situ single-pass intestinal perfusion, cellular uptake and ex vivo imaging. The resulting RXF-ccNPs were around 165 nm in particle size with a narrow distribution. The oral bioavailability of RXF was enhanced by 2.6 folds through ccNPs compared to RXF suspensions in rats. It was shown that RXF-ccNPs could improve the intestinal permeability of RXF, increase the cellular uptake of RXF and facilitate its transport across the absorptive epithelia. The results indicate that our developed ccNPs based on sulfobutylether-β-cyclodextrin and oligochitosan are a promising vehicle to orally deliver poorly water-soluble drugs over and above RXF. |
| first_indexed | 2024-04-13T08:17:41Z |
| format | Article |
| id | doaj.art-16032bc8ecd5469b9c77a49e760488fe |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-13T08:17:41Z |
| publishDate | 2018-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-16032bc8ecd5469b9c77a49e760488fe2022-12-22T02:54:43ZengMDPI AGPharmaceutics1999-49232018-06-011037610.3390/pharmaceutics10030076pharmaceutics10030076Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability EnhancementZaihua Wang0Yan Li1Guangzhou Guocaoxiafang Biotechnology Co. Ltd., No. 3 Luoxuan 4th Road, Guangzhou International Biotech Island, Guangzhou 510320, ChinaDepartment of Pharmacy, School of Pharmacy, No. 601 West Huangpu Avenue, Jinan University, Guangzhou 510632, ChinaRaloxifene (RXF) is a hormone-like medication used for treating postmenopausal osteoporosis and estrogen-dependent breast cancer, yet associated with bad low bioavailability due to poor solubility. This study was intended to develop cyclodextrin/chitosan nanoparticles (ccNPs) for oral delivery of RXF in order to enhance the oral bioavailability. RXF-loaded ccNPs (RXF-ccNPs) were prepared by cyclodextrin inclusion followed by complexation with chitosan. RXF-ccNPs were fully characterized by particle size, morphology and in vitro drug release. The oral delivery efficacy and transepithelial transport potential were evaluated by pharmacokinetics, in situ single-pass intestinal perfusion, cellular uptake and ex vivo imaging. The resulting RXF-ccNPs were around 165 nm in particle size with a narrow distribution. The oral bioavailability of RXF was enhanced by 2.6 folds through ccNPs compared to RXF suspensions in rats. It was shown that RXF-ccNPs could improve the intestinal permeability of RXF, increase the cellular uptake of RXF and facilitate its transport across the absorptive epithelia. The results indicate that our developed ccNPs based on sulfobutylether-β-cyclodextrin and oligochitosan are a promising vehicle to orally deliver poorly water-soluble drugs over and above RXF.http://www.mdpi.com/1999-4923/10/3/76raloxifenebioavailabilitynanoparticlescyclodextrinchitosanelectrostatic complexation |
| spellingShingle | Zaihua Wang Yan Li Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement Pharmaceutics raloxifene bioavailability nanoparticles cyclodextrin chitosan electrostatic complexation |
| title | Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement |
| title_full | Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement |
| title_fullStr | Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement |
| title_full_unstemmed | Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement |
| title_short | Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement |
| title_sort | raloxifene sbe β cd inclusion complexes formulated into nanoparticles with chitosan to overcome the absorption barrier for bioavailability enhancement |
| topic | raloxifene bioavailability nanoparticles cyclodextrin chitosan electrostatic complexation |
| url | http://www.mdpi.com/1999-4923/10/3/76 |
| work_keys_str_mv | AT zaihuawang raloxifenesbebcdinclusioncomplexesformulatedintonanoparticleswithchitosantoovercometheabsorptionbarrierforbioavailabilityenhancement AT yanli raloxifenesbebcdinclusioncomplexesformulatedintonanoparticleswithchitosantoovercometheabsorptionbarrierforbioavailabilityenhancement |