Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose

Khawar Abbas; Muhammad Ajaz Hussain; Syed Nasir Abbas Bukhari; Muhammad Amin; Muhammad Zaman

doi:10.1016/j.jddst.2019.06.013

Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose

Khawar Abbas
, Muhammad Ajaz Hussain^*
, Syed Nasir Abbas Bukhari
, Muhammad Amin
, Muhammad Zaman

^*Corresponding author for this work

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

1 Scopus citations

Abstract

Present study deals with the synthesis of macromolecular prodrugs of aceclofenac (ACL) on to hydrophilic polysaccharide hydroxyethylcellulose (HEC). ACL prodrugs synthesized were thoroughly characterized by spectroscopic techniques and found organo-soluble. The esterified prodrugs showed self-assembly behaviour at solvent interface of DMSO/water and appeared as nanoparticles of 200–550 nm diameter. The HEC-ACL conjugates showed significant inhibition (43%) in the levels of interleukin 6 (IL-6) which indicated its immunomodulatory potential. The conjugates showed 81% inhibition in edema created after carrageenan injection. HEC-aceclofenac conjugates appeared biocompatible in cell viability studies. Bioavailability studies revealed that ACL from the conjugate shows plasma half-life of 7.90 h which is significantly higher than unmodified ACL (3.93 h). Moreover, t_max of 4.0 h with peak plasma concentration (C_max) of 8.27 μg mL⁻¹ for ACL from conjugate indicated its enhanced bioavailability.

Original language	English
Pages (from-to)	856-862
Number of pages	7
Journal	Journal of Drug Delivery Science and Technology
Volume	52
DOIs	https://doi.org/10.1016/j.jddst.2019.06.013
State	Published - Aug 2019
Externally published	Yes

Bibliographical note

Publisher Copyright:
© 2019 Elsevier B.V.

Keywords

Aceclofenac
Bioavailability
Hydroxyethylcellulose
Immunomodulatory potential
Prodrug

ASJC Scopus subject areas

Pharmaceutical Science

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10.1016/j.jddst.2019.06.013

Cite this

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title = "Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose",

abstract = "Present study deals with the synthesis of macromolecular prodrugs of aceclofenac (ACL) on to hydrophilic polysaccharide hydroxyethylcellulose (HEC). ACL prodrugs synthesized were thoroughly characterized by spectroscopic techniques and found organo-soluble. The esterified prodrugs showed self-assembly behaviour at solvent interface of DMSO/water and appeared as nanoparticles of 200–550 nm diameter. The HEC-ACL conjugates showed significant inhibition (43\%) in the levels of interleukin 6 (IL-6) which indicated its immunomodulatory potential. The conjugates showed 81\% inhibition in edema created after carrageenan injection. HEC-aceclofenac conjugates appeared biocompatible in cell viability studies. Bioavailability studies revealed that ACL from the conjugate shows plasma half-life of 7.90 h which is significantly higher than unmodified ACL (3.93 h). Moreover, tmax of 4.0 h with peak plasma concentration (Cmax) of 8.27 μg mL−1 for ACL from conjugate indicated its enhanced bioavailability.",

keywords = "Aceclofenac, Bioavailability, Hydroxyethylcellulose, Immunomodulatory potential, Prodrug",

author = "Khawar Abbas and Hussain, \{Muhammad Ajaz\} and \{Abbas Bukhari\}, \{Syed Nasir\} and Muhammad Amin and Muhammad Zaman",

note = "Publisher Copyright: {\textcopyright} 2019 Elsevier B.V.",

year = "2019",

month = aug,

doi = "10.1016/j.jddst.2019.06.013",

language = "English",

volume = "52",

pages = "856--862",

journal = "Journal of Drug Delivery Science and Technology",

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}

Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose. / Abbas, Khawar; Hussain, Muhammad Ajaz; Abbas Bukhari, Syed Nasir et al.
In: Journal of Drug Delivery Science and Technology, Vol. 52, 08.2019, p. 856-862.

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

TY - JOUR

T1 - Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose

AU - Abbas, Khawar

AU - Hussain, Muhammad Ajaz

AU - Abbas Bukhari, Syed Nasir

AU - Amin, Muhammad

AU - Zaman, Muhammad

PY - 2019/8

Y1 - 2019/8

N2 - Present study deals with the synthesis of macromolecular prodrugs of aceclofenac (ACL) on to hydrophilic polysaccharide hydroxyethylcellulose (HEC). ACL prodrugs synthesized were thoroughly characterized by spectroscopic techniques and found organo-soluble. The esterified prodrugs showed self-assembly behaviour at solvent interface of DMSO/water and appeared as nanoparticles of 200–550 nm diameter. The HEC-ACL conjugates showed significant inhibition (43%) in the levels of interleukin 6 (IL-6) which indicated its immunomodulatory potential. The conjugates showed 81% inhibition in edema created after carrageenan injection. HEC-aceclofenac conjugates appeared biocompatible in cell viability studies. Bioavailability studies revealed that ACL from the conjugate shows plasma half-life of 7.90 h which is significantly higher than unmodified ACL (3.93 h). Moreover, tmax of 4.0 h with peak plasma concentration (Cmax) of 8.27 μg mL−1 for ACL from conjugate indicated its enhanced bioavailability.

AB - Present study deals with the synthesis of macromolecular prodrugs of aceclofenac (ACL) on to hydrophilic polysaccharide hydroxyethylcellulose (HEC). ACL prodrugs synthesized were thoroughly characterized by spectroscopic techniques and found organo-soluble. The esterified prodrugs showed self-assembly behaviour at solvent interface of DMSO/water and appeared as nanoparticles of 200–550 nm diameter. The HEC-ACL conjugates showed significant inhibition (43%) in the levels of interleukin 6 (IL-6) which indicated its immunomodulatory potential. The conjugates showed 81% inhibition in edema created after carrageenan injection. HEC-aceclofenac conjugates appeared biocompatible in cell viability studies. Bioavailability studies revealed that ACL from the conjugate shows plasma half-life of 7.90 h which is significantly higher than unmodified ACL (3.93 h). Moreover, tmax of 4.0 h with peak plasma concentration (Cmax) of 8.27 μg mL−1 for ACL from conjugate indicated its enhanced bioavailability.

KW - Aceclofenac

KW - Bioavailability

KW - Hydroxyethylcellulose

KW - Immunomodulatory potential

KW - Prodrug

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DO - 10.1016/j.jddst.2019.06.013

M3 - Article

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SN - 1773-2247

VL - 52

SP - 856

EP - 862

JO - Journal of Drug Delivery Science and Technology

JF - Journal of Drug Delivery Science and Technology

ER -

Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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