Molecular Interaction Studies of Amorphous Solid Dispersions of the Antimelanoma Agent Betulinic Acid. Yu, M., Ocando, J., E., Trombetta, L., & Chatterjee, P. AAPS PHARMSCITECH, 16(2):384-397, SPRINGER, 4, 2015.
abstract   bibtex   
Betulinic acid (BA), a novel natural product with antimelanoma activity, has poor aqueous solubility (< 0.1 mu g/mL) and therefore exhibits poor bioavailability. The purpose of this study was to explore the feasibility of preparing BA solid dispersions (BA-SDs) with hydrophilic polymers to enhance the aqueous solubility of BA. Melt-quenched solid dispersions (MQ-SDs) of BA were prepared at various ratios with the hydrophilic polymers including Soluplus, HPMCAS-HF, Kollidon VA64, Kollidon K90, and Eudragit RLPO. BA was found to be miscible in all polymers at a 1:4 (w/w) ratio by modulated differential scanning calorimetry (MDSC). BA/Soluplus MQ-SD exhibited the highest solubility in simulated body fluids followed by BA/Kollidon VA64 MQ-SD. The MQ-SDs of BA/Soluplus, BA/HPMCAS-HF, and BA/Kollidon VA64 were found to be amorphous as indicated by X-ray powder diffraction (XRPD) studies. Fourier transform infra-red (FT-IR) studies indicated molecular interactions between BA and Soluplus. Our preliminary screening of polymers indicates that Soluplus and Kollidon VA64 exhibit the greatest potential to form BA-SDs.
@article{
 title = {Molecular Interaction Studies of Amorphous Solid Dispersions of the Antimelanoma Agent Betulinic Acid},
 type = {article},
 year = {2015},
 identifiers = {[object Object]},
 keywords = {betulinic acid; DSC; FT-IR; HPLC; SEM; solid dispe},
 pages = {384-397},
 volume = {16},
 month = {4},
 publisher = {SPRINGER},
 city = {233 SPRING ST, NEW YORK, NY 10013 USA},
 id = {1466671f-6948-3327-a2bf-73a7fde0a220},
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 last_modified = {2017-03-14T12:30:08.401Z},
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 abstract = {Betulinic acid (BA), a novel natural product with antimelanoma activity,
has poor aqueous solubility (< 0.1 mu g/mL) and therefore exhibits poor
bioavailability. The purpose of this study was to explore the
feasibility of preparing BA solid dispersions (BA-SDs) with hydrophilic
polymers to enhance the aqueous solubility of BA. Melt-quenched solid
dispersions (MQ-SDs) of BA were prepared at various ratios with the
hydrophilic polymers including Soluplus, HPMCAS-HF, Kollidon VA64,
Kollidon K90, and Eudragit RLPO. BA was found to be miscible in all
polymers at a 1:4 (w/w) ratio by modulated differential scanning
calorimetry (MDSC). BA/Soluplus MQ-SD exhibited the highest solubility
in simulated body fluids followed by BA/Kollidon VA64 MQ-SD. The MQ-SDs
of BA/Soluplus, BA/HPMCAS-HF, and BA/Kollidon VA64 were found to be
amorphous as indicated by X-ray powder diffraction (XRPD) studies.
Fourier transform infra-red (FT-IR) studies indicated molecular
interactions between BA and Soluplus. Our preliminary screening of
polymers indicates that Soluplus and Kollidon VA64 exhibit the greatest
potential to form BA-SDs.},
 bibtype = {article},
 author = {Yu, Meiki and Ocando, Joseph E and Trombetta, Louis and Chatterjee, Parnali},
 journal = {AAPS PHARMSCITECH},
 number = {2}
}

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