Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin

Jin Xie,1,* Yijing Luo,1,* Yang Liu,1 Yueqin Ma,1,2 Pengfei Yue,1,* Ming Yang1 1Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China; 2Department of Pharmaceutics, 94th Hospital of People’s Liberatio...

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Main Authors: Xie J, Luo Y, Liu Y, Ma Y, Yue P, Yang M
Format: Article
Language:English
Published: Dove Medical Press 2019-01-01
Series:International Journal of Nanomedicine
Subjects:
Online Access:https://www.dovepress.com/novel-redispersible-nanosuspensions-stabilized-by-co-processed-nanocry-peer-reviewed-article-IJN
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author Xie J
Luo Y
Liu Y
Ma Y
Yue P
Yang M
author_facet Xie J
Luo Y
Liu Y
Ma Y
Yue P
Yang M
author_sort Xie J
collection DOAJ
description Jin Xie,1,* Yijing Luo,1,* Yang Liu,1 Yueqin Ma,1,2 Pengfei Yue,1,* Ming Yang1 1Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China; 2Department of Pharmaceutics, 94th Hospital of People’s Liberation Army, Nanchang, China *These authors contributed equally to this work Background: To improve the dissolution and bioavailability of poorly soluble drugs, novel nanosuspensions using co-processed nanocrystalline cellulose–sodium carboxymethyl starch (NCCS) as a synergetic stabilizer were first designed.Methods: Co-processed NCCS was prepared by means of homogenization. Poorly soluble baicalin (BCA) was used as a model drug. BCA nanosuspension (BCA-NS/NCCS) using co-processed NCCS as a dispersant was prepared via homogenization and further converted into the dried BCA nanosuspension particle (BCA-NP/NCCS) via spray drying. The influence of NCCS on the dispersion efficiency of BCA-NS/NCCS was investigated. Morphology and crystal characteristic of NCCS and BCA-NP were analyzed. The dissolution and bioavailability evaluation were performed to investigate the feasibility of NCCS as a stabilizer for BCA-NS/NCCS and BCA-NP.Results: The optimum 50% concentration of NCCS (nanocrystalline cellulose [NCC]:sodium carboxymethyl starch [SCS]=60:40) could be mostly beneficial for formation and stability of BCA-NS/NCCS. NCCS could completely prevent aggregation of BCA-NP during spray drying and enhance the redispersibility as well as dissolution of spray-dried BCA-NP, which might be attributed to “brick–concrete”-based barrier effect of NCCS and the swelling capacity of superdisintegrant SCS. The crystal state of NCC and BCA presented in BCA-NP/NCCS remained unchanged during the homogenization. The BCA-NP/NCCS exhibited a fast dissolution rate and significantly enhanced bioavailability of BCA. The AUC(0–∞) of the BCA-NP/NCCS (8,773.38±718.18 µg/L·h) was 2.01 times (P<0.05) as high as that of the crude BCA (4,354.61±451.28 µg/L·h).Conclusion: This study demonstrated that novel surfactant-free nanosuspensions could be prepared using co-processed NCCS as a synergetic stabilizer and also provided a feasible strategy to improve the dissolution and oral bioavailability of poorly soluble drug. Keywords: nanocrystalline cellulose, Pickering nanosuspensions, nanocrystals, solid particles stabilizer, oral bioavailability
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spelling doaj.art-6ae0daa6d7ef48859f5fff41446cab952022-12-21T23:00:20ZengDove Medical PressInternational Journal of Nanomedicine1178-20132019-01-01Volume 1435336943392Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalinXie JLuo YLiu YMa YYue PYang MJin Xie,1,* Yijing Luo,1,* Yang Liu,1 Yueqin Ma,1,2 Pengfei Yue,1,* Ming Yang1 1Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China; 2Department of Pharmaceutics, 94th Hospital of People’s Liberation Army, Nanchang, China *These authors contributed equally to this work Background: To improve the dissolution and bioavailability of poorly soluble drugs, novel nanosuspensions using co-processed nanocrystalline cellulose–sodium carboxymethyl starch (NCCS) as a synergetic stabilizer were first designed.Methods: Co-processed NCCS was prepared by means of homogenization. Poorly soluble baicalin (BCA) was used as a model drug. BCA nanosuspension (BCA-NS/NCCS) using co-processed NCCS as a dispersant was prepared via homogenization and further converted into the dried BCA nanosuspension particle (BCA-NP/NCCS) via spray drying. The influence of NCCS on the dispersion efficiency of BCA-NS/NCCS was investigated. Morphology and crystal characteristic of NCCS and BCA-NP were analyzed. The dissolution and bioavailability evaluation were performed to investigate the feasibility of NCCS as a stabilizer for BCA-NS/NCCS and BCA-NP.Results: The optimum 50% concentration of NCCS (nanocrystalline cellulose [NCC]:sodium carboxymethyl starch [SCS]=60:40) could be mostly beneficial for formation and stability of BCA-NS/NCCS. NCCS could completely prevent aggregation of BCA-NP during spray drying and enhance the redispersibility as well as dissolution of spray-dried BCA-NP, which might be attributed to “brick–concrete”-based barrier effect of NCCS and the swelling capacity of superdisintegrant SCS. The crystal state of NCC and BCA presented in BCA-NP/NCCS remained unchanged during the homogenization. The BCA-NP/NCCS exhibited a fast dissolution rate and significantly enhanced bioavailability of BCA. The AUC(0–∞) of the BCA-NP/NCCS (8,773.38±718.18 µg/L·h) was 2.01 times (P<0.05) as high as that of the crude BCA (4,354.61±451.28 µg/L·h).Conclusion: This study demonstrated that novel surfactant-free nanosuspensions could be prepared using co-processed NCCS as a synergetic stabilizer and also provided a feasible strategy to improve the dissolution and oral bioavailability of poorly soluble drug. Keywords: nanocrystalline cellulose, Pickering nanosuspensions, nanocrystals, solid particles stabilizer, oral bioavailabilityhttps://www.dovepress.com/novel-redispersible-nanosuspensions-stabilized-by-co-processed-nanocry-peer-reviewed-article-IJNnanocrystalline cellulosenanosuspensionsnanocrystalssolid particles stabilizersodium carboxymethyl starch
spellingShingle Xie J
Luo Y
Liu Y
Ma Y
Yue P
Yang M
Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
International Journal of Nanomedicine
nanocrystalline cellulose
nanosuspensions
nanocrystals
solid particles stabilizer
sodium carboxymethyl starch
title Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
title_full Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
title_fullStr Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
title_full_unstemmed Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
title_short Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
title_sort novel redispersible nanosuspensions stabilized by co processed nanocrystalline cellulose ndash sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
topic nanocrystalline cellulose
nanosuspensions
nanocrystals
solid particles stabilizer
sodium carboxymethyl starch
url https://www.dovepress.com/novel-redispersible-nanosuspensions-stabilized-by-co-processed-nanocry-peer-reviewed-article-IJN
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