Effect of hydrophilic polymers on complexation effciency of cyclodextrins in enhancing solubility and release of diflunisal

Mehreen Bashir; Haroon Khalid Syed; Sajid Asghar; Muhammad Irfan; Waleed Hassan Almalki; Salah Ali Menshawi; Ikram Ullah Khan; Pervaiz A. Shah; Ikrima Khalid; Junaid Ahmad; Umar Farooq Gohar; Kok Khiang Peh; Muhammad Shahid Iqbal

doi:10.3390/polym12071564

Effect of hydrophilic polymers on complexation effciency of cyclodextrins in enhancing solubility and release of diflunisal

Mehreen Bashir
, Haroon Khalid Syed
, Sajid Asghar
, Muhammad Irfan
, Waleed Hassan Almalki
, Salah Ali Menshawi
, Ikram Ullah Khan
, Pervaiz A. Shah
, Ikrima Khalid
, Junaid Ahmad
, Umar Farooq Gohar
, Kok Khiang Peh
, Muhammad Shahid Iqbal

Clinical Pharmacy

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

22 Scopus citations

Abstract

The effects of three hydrophilic polymers, namely, carboxymethyl cellulose sodium (CMC-Na), polyvinyl alcohol (PVA) and poloxamer-188 (PXM-188) on the solubility and dissolution of diflunisal (DIF) in complexation with β-cyclodextrin (βCD) or hydroxypropyl β-cyclodextrin (HPβCD), were investigated. The kneading method was used at different drug to cyclodextrin weight ratios. Increases in solubility and drug release were observed with the DIF/βCD and DIF/HPβCD complexes. The addition of hydrophilic polymers at 2.5, 5.0 and 10.0% w/w markedly improved the complexation and solubilizing efficiency ofβCDandHPβCD. Fourier-transform infrared (FTIR) showed that DIF was successfully included into the cyclodextrin cavity. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) confirmed stronger drug amorphization and entrapment in the molecular cage of cyclodextrins. The addition of PVA, CMC-Na or PXM-188 reduced further the intensity of the DIF endothermic peak. Most of the sharp and intense peaks of DIF disappeared with the addition of hydrophilic polymers. In conclusion, PXM-188 at a weight ratio of 10.0% w/w was the best candidate in enhancing the solubility, stability and release of DIF.

Original language	English
Article number	1564
Journal	Polymers
Volume	12
Issue number	7
DOIs	https://doi.org/10.3390/polym12071564
State	Published - 1 Jul 2020

Keywords

Complexation
Diflunisal
Dissolution rate
Hydrophilic polymers
Hydroxypropyl ß-cyclodextrin
ß-cyclodextrin

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10.3390/polym12071564

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Bashir, M., Syed, H. K., Asghar, S., Irfan, M., Almalki, W. H., Menshawi, S. A., Khan, I. U., Shah, P. A., Khalid, I., Ahmad, J., Gohar, U. F., Peh, K. K., & Iqbal, M. S. (2020). Effect of hydrophilic polymers on complexation effciency of cyclodextrins in enhancing solubility and release of diflunisal. Polymers, 12(7), Article 1564. https://doi.org/10.3390/polym12071564

@article{2ea3493a91c74865ba0511d6f80c3475,

title = "Effect of hydrophilic polymers on complexation effciency of cyclodextrins in enhancing solubility and release of diflunisal",

abstract = "The effects of three hydrophilic polymers, namely, carboxymethyl cellulose sodium (CMC-Na), polyvinyl alcohol (PVA) and poloxamer-188 (PXM-188) on the solubility and dissolution of diflunisal (DIF) in complexation with β-cyclodextrin (βCD) or hydroxypropyl β-cyclodextrin (HPβCD), were investigated. The kneading method was used at different drug to cyclodextrin weight ratios. Increases in solubility and drug release were observed with the DIF/βCD and DIF/HPβCD complexes. The addition of hydrophilic polymers at 2.5, 5.0 and 10.0\% w/w markedly improved the complexation and solubilizing efficiency ofβCDandHPβCD. Fourier-transform infrared (FTIR) showed that DIF was successfully included into the cyclodextrin cavity. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) confirmed stronger drug amorphization and entrapment in the molecular cage of cyclodextrins. The addition of PVA, CMC-Na or PXM-188 reduced further the intensity of the DIF endothermic peak. Most of the sharp and intense peaks of DIF disappeared with the addition of hydrophilic polymers. In conclusion, PXM-188 at a weight ratio of 10.0\% w/w was the best candidate in enhancing the solubility, stability and release of DIF.",

keywords = "Complexation, Diflunisal, Dissolution rate, Hydrophilic polymers, Hydroxypropyl {\ss}-cyclodextrin, {\ss}-cyclodextrin",

author = "Mehreen Bashir and Syed, \{Haroon Khalid\} and Sajid Asghar and Muhammad Irfan and Almalki, \{Waleed Hassan\} and Menshawi, \{Salah Ali\} and Khan, \{Ikram Ullah\} and Shah, \{Pervaiz A.\} and Ikrima Khalid and Junaid Ahmad and Gohar, \{Umar Farooq\} and Peh, \{Kok Khiang\} and Iqbal, \{Muhammad Shahid\}",

note = "Publisher Copyright: {\textcopyright} 2020 by the authors.",

year = "2020",

month = jul,

day = "1",

doi = "10.3390/polym12071564",

language = "English",

volume = "12",

journal = "Polymers",

issn = "2073-4360",

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TY - JOUR

T1 - Effect of hydrophilic polymers on complexation effciency of cyclodextrins in enhancing solubility and release of diflunisal

AU - Bashir, Mehreen

AU - Syed, Haroon Khalid

AU - Asghar, Sajid

AU - Irfan, Muhammad

AU - Almalki, Waleed Hassan

AU - Menshawi, Salah Ali

AU - Khan, Ikram Ullah

AU - Shah, Pervaiz A.

AU - Khalid, Ikrima

AU - Ahmad, Junaid

AU - Gohar, Umar Farooq

AU - Peh, Kok Khiang

AU - Iqbal, Muhammad Shahid

PY - 2020/7/1

Y1 - 2020/7/1

N2 - The effects of three hydrophilic polymers, namely, carboxymethyl cellulose sodium (CMC-Na), polyvinyl alcohol (PVA) and poloxamer-188 (PXM-188) on the solubility and dissolution of diflunisal (DIF) in complexation with β-cyclodextrin (βCD) or hydroxypropyl β-cyclodextrin (HPβCD), were investigated. The kneading method was used at different drug to cyclodextrin weight ratios. Increases in solubility and drug release were observed with the DIF/βCD and DIF/HPβCD complexes. The addition of hydrophilic polymers at 2.5, 5.0 and 10.0% w/w markedly improved the complexation and solubilizing efficiency ofβCDandHPβCD. Fourier-transform infrared (FTIR) showed that DIF was successfully included into the cyclodextrin cavity. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) confirmed stronger drug amorphization and entrapment in the molecular cage of cyclodextrins. The addition of PVA, CMC-Na or PXM-188 reduced further the intensity of the DIF endothermic peak. Most of the sharp and intense peaks of DIF disappeared with the addition of hydrophilic polymers. In conclusion, PXM-188 at a weight ratio of 10.0% w/w was the best candidate in enhancing the solubility, stability and release of DIF.

AB - The effects of three hydrophilic polymers, namely, carboxymethyl cellulose sodium (CMC-Na), polyvinyl alcohol (PVA) and poloxamer-188 (PXM-188) on the solubility and dissolution of diflunisal (DIF) in complexation with β-cyclodextrin (βCD) or hydroxypropyl β-cyclodextrin (HPβCD), were investigated. The kneading method was used at different drug to cyclodextrin weight ratios. Increases in solubility and drug release were observed with the DIF/βCD and DIF/HPβCD complexes. The addition of hydrophilic polymers at 2.5, 5.0 and 10.0% w/w markedly improved the complexation and solubilizing efficiency ofβCDandHPβCD. Fourier-transform infrared (FTIR) showed that DIF was successfully included into the cyclodextrin cavity. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) confirmed stronger drug amorphization and entrapment in the molecular cage of cyclodextrins. The addition of PVA, CMC-Na or PXM-188 reduced further the intensity of the DIF endothermic peak. Most of the sharp and intense peaks of DIF disappeared with the addition of hydrophilic polymers. In conclusion, PXM-188 at a weight ratio of 10.0% w/w was the best candidate in enhancing the solubility, stability and release of DIF.

KW - Complexation

KW - Diflunisal

KW - Dissolution rate

KW - Hydrophilic polymers

KW - Hydroxypropyl ß-cyclodextrin

KW - ß-cyclodextrin

UR - https://www.scopus.com/pages/publications/85088321714

U2 - 10.3390/polym12071564

DO - 10.3390/polym12071564

M3 - Article

AN - SCOPUS:85088321714

SN - 2073-4360

VL - 12

JO - Polymers

JF - Polymers

IS - 7

M1 - 1564

ER -

Effect of hydrophilic polymers on complexation effciency of cyclodextrins in enhancing solubility and release of diflunisal

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Keywords

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