Hydrophilic-hydrophobic polymer blend for modulation of crystalline changes and molecular interactions in solid dispersion.
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.
Pharmaceutical Engineering Laboratory, Biomedical Engineering Department, International University, Vietnam National University, Ho Chi Minh City, Viet Nam.
Hai
H
Van Ngo
Pharmaceutical Engineering Laboratory, Biomedical Engineering Department, International University, Vietnam National University, Ho Chi Minh City, Viet Nam.
Phuc Kien
PK
Nguyen
Pharmaceutical Engineering Laboratory, Biomedical Engineering Department, International University, Vietnam National University, Ho Chi Minh City, Viet Nam.
Toi
T
Van Vo
School of Medicine, Deakin University, Waurn Ponds, Victoria, Australia.
Wei
W
Duan
Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, Viet Nam.
Van-Thanh
VT
Tran
School of Medicine, Deakin University, Waurn Ponds, Victoria, Australia. Electronic address: phuong.tran1@deakin.edu.au.
Phuong Ha-Lien
PH
Tran
Pharmaceutical Engineering Laboratory, Biomedical Engineering Department, International University, Vietnam National University, Ho Chi Minh City, Viet Nam. Electronic address: ttdthao@hcmiu.edu.vn.
Thao Truong-Dinh
TT
Tran
D002626:Chemistry, Pharmaceutical / Q000379:methods; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry*; D006860:Hydrogen Bonding; D057927:Hydrophobic and Hydrophilic Interactions; D065347:Hypromellose Derivatives / Q000737:chemistry*; D017275:Isradipine / Q000008:administration & dosage / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction; D015028:Zein / Q000737:chemistry*
D004337:Drug Carriers; D011108:Polymers; D065347:Hypromellose Derivatives; D015028:Zein; D017275:Isradipine
Drug crystal; Hydrophilic-hydrophobic polymer; Molecular interaction; Solid dispersion