Extended release and enhanced bioavailability of moxifloxacin conjugated with hydrophilic cellulose ethers

Nazia S. Abbas; Muhammad Amin; Muhammad A. Hussain; Kevin J. Edgar; Muhammad N. Tahir; Wolfgang Tremel

doi:10.1016/j.carbpol.2015.10.052

Extended release and enhanced bioavailability of moxifloxacin conjugated with hydrophilic cellulose ethers

Nazia S. Abbas
, Muhammad Amin
, Muhammad A. Hussain^*
, Kevin J. Edgar
, Muhammad N. Tahir
, Wolfgang Tremel

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

Abstract

Macromolecular prodrugs (MPDs) of moxifloxacin were fabricated based on hydroxypropylcellulose (HPC) and hydroxyethylcellulose (HEC). UV/Vis spectrophotometry was employed to determine covalently loaded drug content (DC) of each conjugate. The degree of substitution (DS) of moxifloxacin attained ranged from 0.27 to 0.38 (HPC) and 0.19 to 0.26 (HEC) per anhydroglucose unit (AGU), respectively. Transmission electron microscopic analyses showed that HPC-moxifloxacin conjugates self-assembled into nanowires of ∼30 nm diameters while HEC-moxifloxacin conjugates self-assembled into nanoparticles of 150-350 nm. In vitro drug release studies revealed that 15 and 49% moxifloxacin release occurred from the HPC-moxifloxacin conjugate after 6 h at pH 1.2 and 7.4, respectively. Similarly, moxifloxacin release from HEC-moxifloxacin conjugates was 15 and 39% at pH 1.2 and 7.4, respectively. Bioavailability and pharmacokinetic studies in rabbits showed that both HPC- and HEC-conjugates exhibited significantly enhanced moxifloxacin plasma half-life, over 24 h, confirming sustained release and enhanced bioavailability (AUC 2.0-2.1 times higher) of moxifloxacin.

Original language	English
Pages (from-to)	1297-1306
Number of pages	10
Journal	Carbohydrate Polymers
Volume	136
DOIs	https://doi.org/10.1016/j.carbpol.2015.10.052
State	Published - 20 Jan 2016
Externally published	Yes

Bibliographical note

Funding Information:
N. S. Abbas appreciates financial support of Higher Education Commission of Pakistan under the “Indigenous 5000 PhD fellowships program”. N.S. Abbas and M. Amin acknowledge Higher Education Commission of Pakistan for financial support under the IRSIP program as well. We acknowledge Ashland Inc, Covington, KY, USA for their generous gift of HEC. We also acknowledge STANDPHARM Pakistan (Pvt) Ltd. Lahore for a generous gift of moxifloxacin.

Publisher Copyright:
© 2015 Elsevier Ltd. All Rights Reserved.

Keywords

Hydroxyethylcellulose
Hydroxypropylcellulose
Moxifloxacin
Nano-assembly
Pharmacokinetics
Prodrugs

ASJC Scopus subject areas

Organic Chemistry
Polymers and Plastics
Materials Chemistry

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10.1016/j.carbpol.2015.10.052

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@article{0eefaad72cdf4768b93861751a08180e,

title = "Extended release and enhanced bioavailability of moxifloxacin conjugated with hydrophilic cellulose ethers",

abstract = "Macromolecular prodrugs (MPDs) of moxifloxacin were fabricated based on hydroxypropylcellulose (HPC) and hydroxyethylcellulose (HEC). UV/Vis spectrophotometry was employed to determine covalently loaded drug content (DC) of each conjugate. The degree of substitution (DS) of moxifloxacin attained ranged from 0.27 to 0.38 (HPC) and 0.19 to 0.26 (HEC) per anhydroglucose unit (AGU), respectively. Transmission electron microscopic analyses showed that HPC-moxifloxacin conjugates self-assembled into nanowires of ∼30 nm diameters while HEC-moxifloxacin conjugates self-assembled into nanoparticles of 150-350 nm. In vitro drug release studies revealed that 15 and 49\% moxifloxacin release occurred from the HPC-moxifloxacin conjugate after 6 h at pH 1.2 and 7.4, respectively. Similarly, moxifloxacin release from HEC-moxifloxacin conjugates was 15 and 39\% at pH 1.2 and 7.4, respectively. Bioavailability and pharmacokinetic studies in rabbits showed that both HPC- and HEC-conjugates exhibited significantly enhanced moxifloxacin plasma half-life, over 24 h, confirming sustained release and enhanced bioavailability (AUC 2.0-2.1 times higher) of moxifloxacin.",

keywords = "Hydroxyethylcellulose, Hydroxypropylcellulose, Moxifloxacin, Nano-assembly, Pharmacokinetics, Prodrugs",

author = "Abbas, \{Nazia S.\} and Muhammad Amin and Hussain, \{Muhammad A.\} and Edgar, \{Kevin J.\} and Tahir, \{Muhammad N.\} and Wolfgang Tremel",

note = "Funding Information: N. S. Abbas appreciates financial support of Higher Education Commission of Pakistan under the “Indigenous 5000 PhD fellowships program”. N.S. Abbas and M. Amin acknowledge Higher Education Commission of Pakistan for financial support under the IRSIP program as well. We acknowledge Ashland Inc, Covington, KY, USA for their generous gift of HEC. We also acknowledge STANDPHARM Pakistan (Pvt) Ltd. Lahore for a generous gift of moxifloxacin. Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd. All Rights Reserved.",

year = "2016",

month = jan,

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doi = "10.1016/j.carbpol.2015.10.052",

language = "English",

volume = "136",

pages = "1297--1306",

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TY - JOUR

T1 - Extended release and enhanced bioavailability of moxifloxacin conjugated with hydrophilic cellulose ethers

AU - Abbas, Nazia S.

AU - Amin, Muhammad

AU - Hussain, Muhammad A.

AU - Edgar, Kevin J.

AU - Tahir, Muhammad N.

AU - Tremel, Wolfgang

N1 - Funding Information: N. S. Abbas appreciates financial support of Higher Education Commission of Pakistan under the “Indigenous 5000 PhD fellowships program”. N.S. Abbas and M. Amin acknowledge Higher Education Commission of Pakistan for financial support under the IRSIP program as well. We acknowledge Ashland Inc, Covington, KY, USA for their generous gift of HEC. We also acknowledge STANDPHARM Pakistan (Pvt) Ltd. Lahore for a generous gift of moxifloxacin. Publisher Copyright: © 2015 Elsevier Ltd. All Rights Reserved.

PY - 2016/1/20

Y1 - 2016/1/20

N2 - Macromolecular prodrugs (MPDs) of moxifloxacin were fabricated based on hydroxypropylcellulose (HPC) and hydroxyethylcellulose (HEC). UV/Vis spectrophotometry was employed to determine covalently loaded drug content (DC) of each conjugate. The degree of substitution (DS) of moxifloxacin attained ranged from 0.27 to 0.38 (HPC) and 0.19 to 0.26 (HEC) per anhydroglucose unit (AGU), respectively. Transmission electron microscopic analyses showed that HPC-moxifloxacin conjugates self-assembled into nanowires of ∼30 nm diameters while HEC-moxifloxacin conjugates self-assembled into nanoparticles of 150-350 nm. In vitro drug release studies revealed that 15 and 49% moxifloxacin release occurred from the HPC-moxifloxacin conjugate after 6 h at pH 1.2 and 7.4, respectively. Similarly, moxifloxacin release from HEC-moxifloxacin conjugates was 15 and 39% at pH 1.2 and 7.4, respectively. Bioavailability and pharmacokinetic studies in rabbits showed that both HPC- and HEC-conjugates exhibited significantly enhanced moxifloxacin plasma half-life, over 24 h, confirming sustained release and enhanced bioavailability (AUC 2.0-2.1 times higher) of moxifloxacin.

AB - Macromolecular prodrugs (MPDs) of moxifloxacin were fabricated based on hydroxypropylcellulose (HPC) and hydroxyethylcellulose (HEC). UV/Vis spectrophotometry was employed to determine covalently loaded drug content (DC) of each conjugate. The degree of substitution (DS) of moxifloxacin attained ranged from 0.27 to 0.38 (HPC) and 0.19 to 0.26 (HEC) per anhydroglucose unit (AGU), respectively. Transmission electron microscopic analyses showed that HPC-moxifloxacin conjugates self-assembled into nanowires of ∼30 nm diameters while HEC-moxifloxacin conjugates self-assembled into nanoparticles of 150-350 nm. In vitro drug release studies revealed that 15 and 49% moxifloxacin release occurred from the HPC-moxifloxacin conjugate after 6 h at pH 1.2 and 7.4, respectively. Similarly, moxifloxacin release from HEC-moxifloxacin conjugates was 15 and 39% at pH 1.2 and 7.4, respectively. Bioavailability and pharmacokinetic studies in rabbits showed that both HPC- and HEC-conjugates exhibited significantly enhanced moxifloxacin plasma half-life, over 24 h, confirming sustained release and enhanced bioavailability (AUC 2.0-2.1 times higher) of moxifloxacin.

KW - Hydroxyethylcellulose

KW - Hydroxypropylcellulose

KW - Moxifloxacin

KW - Nano-assembly

KW - Pharmacokinetics

KW - Prodrugs

UR - https://www.scopus.com/pages/publications/84945917501

U2 - 10.1016/j.carbpol.2015.10.052

DO - 10.1016/j.carbpol.2015.10.052

M3 - Article

C2 - 26572474

AN - SCOPUS:84945917501

SN - 0144-8617

VL - 136

SP - 1297

EP - 1306

JO - Carbohydrate Polymers

JF - Carbohydrate Polymers

ER -

Extended release and enhanced bioavailability of moxifloxacin conjugated with hydrophilic cellulose ethers

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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