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Effect of Hydrophilic Polymers on Complexation Efficiency of Cyclodextrins in Enhancing Solubility and Release of Diflunisal.
Polymers (Basel). 2020 Jul 15; 12(7)P

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 of βCD and HPβCD. 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.

Authors+Show Affiliations

Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.Department of Toxicology and Pharmacology, College of Pharmacy, Umm Al Qura University, Makkah 21955, Saudi Arabia.Department of Toxicology in Comprehensive Specialized Clinics Security Forces, Jeddah 21442, Saudi Arabia.Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.University College of Pharmacy, University of the Punjab, Lahore 54590, Pakistan.Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.Institute of Industrial Biotechnology, Government College University, Lahore 54590, Pakistan.Department of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden, Penang 11800, Malaysia.Department of Clinical Pharmacy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32679660

Citation

Bashir, Mehreen, et al. "Effect of Hydrophilic Polymers On Complexation Efficiency of Cyclodextrins in Enhancing Solubility and Release of Diflunisal." Polymers, vol. 12, no. 7, 2020.
Bashir M, Syed HK, Asghar S, et al. Effect of Hydrophilic Polymers on Complexation Efficiency of Cyclodextrins in Enhancing Solubility and Release of Diflunisal. Polymers. 2020;12(7).
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 Efficiency of Cyclodextrins in Enhancing Solubility and Release of Diflunisal. Polymers, 12(7). https://doi.org/10.3390/polym12071564
Bashir M, et al. Effect of Hydrophilic Polymers On Complexation Efficiency of Cyclodextrins in Enhancing Solubility and Release of Diflunisal. Polymers. 2020 Jul 15;12(7) PubMed PMID: 32679660.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of Hydrophilic Polymers on Complexation Efficiency 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, Y1 - 2020/07/15/ PY - 2020/06/10/received PY - 2020/07/04/revised PY - 2020/07/07/accepted PY - 2020/7/19/entrez PY - 2020/7/19/pubmed PY - 2020/7/19/medline KW - complexation KW - diflunisal KW - dissolution rate KW - hydrophilic polymers KW - hydroxypropyl β-cyclodextrin KW - β-cyclodextrin JF - Polymers VL - 12 IS - 7 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 of βCD and HPβCD. 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. SN - 2073-4360 UR - https://www.unboundmedicine.com/medline/citation/32679660/Effect_of_Hydrophilic_Polymers_on_Complexation_Efficiency_of_Cyclodextrins_in_Enhancing_Solubility_and_Release_of_Diflunisal_ L2 - https://www.mdpi.com/resolver?pii=polym12071564 DB - PRIME DP - Unbound Medicine ER -
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