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},
created = {2015-12-14T19:51:29.000Z},
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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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The purpose of this study was to explore the\nfeasibility of preparing BA solid dispersions (BA-SDs) with hydrophilic\npolymers to enhance the aqueous solubility of BA. Melt-quenched solid\ndispersions (MQ-SDs) of BA were prepared at various ratios with the\nhydrophilic polymers including Soluplus, HPMCAS-HF, Kollidon VA64,\nKollidon K90, and Eudragit RLPO. BA was found to be miscible in all\npolymers at a 1:4 (w/w) ratio by modulated differential scanning\ncalorimetry (MDSC). BA/Soluplus MQ-SD exhibited the highest solubility\nin simulated body fluids followed by BA/Kollidon VA64 MQ-SD. The MQ-SDs\nof BA/Soluplus, BA/HPMCAS-HF, and BA/Kollidon VA64 were found to be\namorphous as indicated by X-ray powder diffraction (XRPD) studies.\nFourier transform infra-red (FT-IR) studies indicated molecular\ninteractions between BA and Soluplus. Our preliminary screening of\npolymers indicates that Soluplus and Kollidon VA64 exhibit the greatest\npotential to form BA-SDs.","bibtype":"article","author":"Yu, Meiki and Ocando, Joseph E and Trombetta, Louis and Chatterjee, Parnali","journal":"AAPS PHARMSCITECH","number":"2","bibtex":"@article{\n title = {Molecular Interaction Studies of Amorphous Solid Dispersions of the Antimelanoma Agent Betulinic Acid},\n type = {article},\n year = {2015},\n identifiers = {[object Object]},\n keywords = {betulinic acid; DSC; FT-IR; HPLC; SEM; solid dispe},\n pages = {384-397},\n volume = {16},\n month = {4},\n publisher = {SPRINGER},\n city = {233 SPRING ST, NEW YORK, NY 10013 USA},\n id = {1466671f-6948-3327-a2bf-73a7fde0a220},\n created = {2015-12-14T19:51:29.000Z},\n file_attached = {false},\n profile_id = {3187ec9d-0fcc-3ba2-91e0-3075df9b18c3},\n group_id = {d75e47fd-ff52-3a4b-bf1e-6ebc7e454352},\n last_modified = {2017-03-14T12:30:08.401Z},\n read = {false},\n starred = {false},\n authored = {false},\n confirmed = {true},\n hidden = {false},\n citation_key = {ISI:000351612500017},\n source_type = {article},\n user_context = {Article},\n private_publication = {false},\n abstract = {Betulinic acid (BA), a novel natural product with antimelanoma activity,\nhas poor aqueous solubility (< 0.1 mu g/mL) and therefore exhibits poor\nbioavailability. The purpose of this study was to explore the\nfeasibility of preparing BA solid dispersions (BA-SDs) with hydrophilic\npolymers to enhance the aqueous solubility of BA. Melt-quenched solid\ndispersions (MQ-SDs) of BA were prepared at various ratios with the\nhydrophilic polymers including Soluplus, HPMCAS-HF, Kollidon VA64,\nKollidon K90, and Eudragit RLPO. BA was found to be miscible in all\npolymers at a 1:4 (w/w) ratio by modulated differential scanning\ncalorimetry (MDSC). BA/Soluplus MQ-SD exhibited the highest solubility\nin simulated body fluids followed by BA/Kollidon VA64 MQ-SD. The MQ-SDs\nof BA/Soluplus, BA/HPMCAS-HF, and BA/Kollidon VA64 were found to be\namorphous as indicated by X-ray powder diffraction (XRPD) studies.\nFourier transform infra-red (FT-IR) studies indicated molecular\ninteractions between BA and Soluplus. Our preliminary screening of\npolymers indicates that Soluplus and Kollidon VA64 exhibit the greatest\npotential to form BA-SDs.},\n bibtype = {article},\n author = {Yu, Meiki and Ocando, Joseph E and Trombetta, Louis and Chatterjee, Parnali},\n journal = {AAPS PHARMSCITECH},\n number = {2}\n}","author_short":["Yu, M.","Ocando, J., E.","Trombetta, L.","Chatterjee, P."],"bibbaseid":"yu-ocando-trombetta-chatterjee-molecularinteractionstudiesofamorphoussoliddispersionsoftheantimelanomaagentbetulinicacid-2015","role":"author","urls":{},"keyword":["betulinic acid; DSC; FT-IR; HPLC; SEM; solid dispe"],"downloads":0},"search_terms":["molecular","interaction","studies","amorphous","solid","dispersions","antimelanoma","agent","betulinic","acid","yu","ocando","trombetta","chatterjee"],"keywords":["betulinic acid; dsc; ft-ir; hplc; sem; solid dispe"],"authorIDs":[]}