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Hydrophilic-hydrophobic polymer blend for modulation of crystalline changes and molecular interactions in solid dispersion

Van Ngo, Hai, Nguyen, Phuc Kien, Van Vo, Toi, Duan, Wei, Tran, Van-Thanh, Tran, Phuong Ha-Lien and Tran, Thao Truong-Dinh 2016, Hydrophilic-hydrophobic polymer blend for modulation of crystalline changes and molecular interactions in solid dispersion, International journal of pharmaceutics, vol. 513, no. 1-2, pp. 148-152, doi: 10.1016/j.ijpharm.2016.09.017.

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Title Hydrophilic-hydrophobic polymer blend for modulation of crystalline changes and molecular interactions in solid dispersion
Author(s) Van Ngo, Hai
Nguyen, Phuc Kien
Van Vo, Toi
Duan, Wei
Tran, Van-Thanh
Tran, Phuong Ha-Lien
Tran, Thao Truong-Dinh
Journal name International journal of pharmaceutics
Volume number 513
Issue number 1-2
Start page 148
End page 152
Total pages 5
Publisher Elsevier
Place of publication Amsterdam, The Netherlands
Publication date 2016-11-20
ISSN 0378-5173
1873-3476
Keyword(s) Drug crystal
Hydrophilic-hydrophobic polymer
Molecular interaction
Solid dispersion
Science & Technology
Life Sciences & Biomedicine
Pharmacology & Pharmacy
WATER-SOLUBLE DRUG
ORAL DELIVERY
SWELLABLE POLYMER
MELTING METHOD
DISSOLUTION
FORMULATION
ISRADIPINE
PHARMACOKINETICS
BIOAVAILABILITY
STRATEGIES
Summary This research study aimed to develop a new strategy for using a polymer blend in solid dispersion (SD) for dissolution enhancement of poorly water-soluble drugs. SDs with different blends of hydrophilic-hydrophobic polymers (zein/hydroxypropyl methylcellulose - zein/HPMC) were prepared using spray drying to modulate the drug crystal and polymer-drug interactions in SDs. Physicochemical characterizations, including power X-ray diffraction and Fourier transform infrared spectroscopy, were performed to elucidate the roles of the blends in SDs. Although hydrophobic polymers played a key role in changing the model drug from a crystal to an amorphous state, the dissolution rate was limited due to the wetting property. Fortunately, the hydrophilic-hydrophobic blend not only reduced the drug crystallinity but also resulted in a hydrogen bonding interaction between the drugs and the polymer for a dissolution rate improvement. This work may contribute to a new generation of solid dispersion using a blend of hydrophilic-hydrophobic polymers for an effective dissolution enhancement of poorly water-soluble drugs.
Language eng
DOI 10.1016/j.ijpharm.2016.09.017
Field of Research 111502 Clinical Pharmacology and Therapeutics
1115 Pharmacology And Pharmaceutical Sciences
Socio Economic Objective 0 Not Applicable
HERDC Research category C1 Refereed article in a scholarly journal
ERA Research output type C Journal article
Copyright notice ©2016, Elsevier B.V.
Persistent URL http://hdl.handle.net/10536/DRO/DU:30086870

Document type: Journal Article
Collection: School of Medicine
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