Abstract
Amorphous solid dispersion (ASD) is one of the most versatile supersaturating drug delivery systems to improve the dissolution rate and oral bioavailability of poorly water-soluble drugs. PVP based ASD formulation of nimodipine (NMD) has been marketed and effectively used in clinic for nearly 30 years, yet the mechanism by which PVP maintains the supersaturation and subsequently improves the bioavailability of NMD was rarely investigated. In this research, we first studied the molecular interactions between NMD and PVP by solution NMR, using CDCl3 as the solvent, and the drug-polymer Flory-Huggins interaction parameter. No strong specific interaction between PVP and NMD was detected in the nonaqueous state. However, we observed that aqueous supersaturation of NMD could be significantly maintained by PVP, presumably due to the hydrophobic interactions between the hydrophobic moieties of PVP and NMD in aqueous medium. This hypothesis was supported by dynamic light scattering (DLS) and supersaturation experiments in the presence of different surfactants. DLS revealed the formation of NMD/PVP aggregates when NMD was supersaturated, suggesting the formation of hydrophobic interactions between the drug and polymer. The addition of su...Continue Reading
References
Jan 1, 1996·Pharmaceutical Research·S D MithaniJ B Dressman
Jul 6, 2004·Journal of Pharmaceutical Sciences·Anand BalakrishnanJames E Polli
Sep 24, 2004·Langmuir : the ACS Journal of Surfaces and Colloids·Nirmesh JainMireille Turmine
Apr 3, 2007·Langmuir : the ACS Journal of Surfaces and Colloids·Tian WuLian Yu
Apr 18, 2009·Journal of Pharmaceutical Sciences·Joachim BrouwersPatrick Augustijns
Feb 4, 2010·Journal of Pharmaceutical Sciences·Feng QianMunir A Hussain
Jul 8, 2010·Journal of Pharmaceutical Sciences·Ye SunLian Yu
Jan 18, 2011·Advances in Colloid and Interface Science·Julia Maldonado-ValderramaAlan Mackie
May 1, 1985·Langmuir : the ACS Journal of Surfaces and Colloids·E D GoddardK P Ananthapadmanabhan
Aug 4, 2011·Expert Opinion on Drug Delivery·Abhishek SinghGuy Van den Mooter
Nov 14, 2012·Journal of Pharmaceutical Sciences·Leslie Z Benet
Jun 12, 2013·International Journal of Pharmaceutics·Chris Brough, R O Williams
Dec 24, 2014·Molecular Pharmaceutics·Yuejie ChenFeng Qian
Jan 9, 2015·Molecular Pharmaceutics·Jie ChenLynne S Taylor
Sep 15, 2015·International Journal of Clinical Pharmacology and Therapeutics·Masahiko Sato, Mamoru Narukawa
Feb 1, 2014·Acta Pharmaceutica Sinica. B·Yanbin Huang, Wei-Guo Dai
Dec 29, 2015·Molecular Pharmaceutics·Chengyu LiuFeng Qian
Jun 11, 2016·Pharmaceutical Research·Yuejie ChenFeng Qian
Jun 16, 2016·The AAPS Journal·Suhas G GumasteAbu T M Serajuddin
Jun 24, 2016·Molecular Pharmaceutics·Yuejie ChenFeng Qian
Aug 5, 2016·Journal of Pharmaceutical Sciences·Henrik PalmelundThomas Rades
Jan 31, 2018·Pharmaceutical Research·Zhen ChenFeng Qian
Citations
Dec 31, 2019·Drug Delivery·Andreas SchittnyMaxim Puchkov
Jun 11, 2019·Pharmaceutical Development and Technology·Chun TaoHongtao Song
Jun 2, 2020·Pharmaceutical Research·Shan WangFeng Qian
Jun 18, 2020·Pharmaceutics·Marius Monschke, Karl G Wagner
Aug 11, 2021·Pharmaceutics·Meng LiEcevit Bilgili
Nov 20, 2018·Molecular Pharmaceutics·Yuejie ChenFeng Qian
Dec 12, 2021·AAPS PharmSciTech·Qin ShiBai Ling