[Development and pharmaceutical evaluation of hydrophobic cyclodextrin derivatives as modified-release drug carriers].
TLDR
The combination of CyD derivatives and pharmaceutical additives was also useful to modify the release rate of various drug molecules.Abstract:
Hydrophobic cyclodextrin (CyD) derivatives, such as 2,6-di-O-ethyl-beta-CyD (DE-beta-CyD), 2,3,6-tri-O-ethyl-beta-CyD (TE-beta-CyD), carboxymethylethyl-beta-CyDs (CME-beta-CyDs) with different degrees of substitution, 2,3,6-tri-O-acyl-beta-CyDs with different alkyl chains (C1-C12) were prepared and their chemical structures and physicochemical properties were elucidated. Furthermore, possible utilities of hydrophilic and hydrophobic CyD derivatives as modified-release drug carriers were evaluated on the basis of in vitro/in vivo correlations. The results obtained in this study are as follows: (1) Hydrophilic CyDs such as 2-hydroxypropyl-beta-CyD are useful as immediate-release type carriers for poorly water-soluble drugs such as nifedipine. (2) Hydrophobic CyDs such as ethylated and acylated beta-CyDs can be used as prolonged-release type carriers for water-soluble drugs such as diltiazem hydrochloride, buserelin acetate and molsidomine. (3) Enteric CME-beta-CyD derivatives are useful as delayed-release type carriers, and also as stabilizers for prostaglandin E and carmofur which are labile under alkaline conditions. (4) Various release rates can be obtained by combining hydrophilic and hydrophobic CyD derivatives in appropriate mixing ratios, e.g., double-layer tablets consisting of beta-CyD complex and DE-beta-CyD/CME-beta-CyD complexes released drugs rapidly at an initial stage, followed by slow release. The combination of CyD derivatives and pharmaceutical additives was also useful to modify the release rate of various drug molecules.read more
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Journal ArticleDOI
Cyclodextrin Drug Carrier Systems.
Journal ArticleDOI
Pharmaceutical applications of cyclodextrins. 2. In vivo drug delivery
TL;DR: This Review primarily focuses on newer findings concerning cyclodextrin derivatives which are likely to receive regulatory acceptance due to improved aqueous solubility and safety profiles as compared to the unmodified cyclodexypropyl-beta-cyclodextrins.
Journal ArticleDOI
Cyclodextrin-based controlled drug release system.
Fumitoshi Hirayama,Kaneto Uekama +1 more
TL;DR: In an oral drug delivery system (DDS), the hydrophilic and ionizable CDs can serve as potent drug carriers in the immediate release- and delayed release-formulations, respectively, while the release rate of water-soluble drugs can be retarded by hydrophobic CDs.
Journal ArticleDOI
Improving the dissolution and bioavailability of nifedipine using solid dispersions and solubilizers.
TL;DR: The aim of the present work was to improve the therapeutic efficacy of NF via incorporation into different types of carriers, and to investigate their in vitro dissolution and bioavailability in rabbits.
Journal ArticleDOI
Peracylated β-Cyclodextrins as Novel Sustained-release Carriers for a Water-soluble Drug, Molsidomine
TL;DR: The present results suggest that perbutanoyl‐β‐CyD is particularly useful in modifying the release rate of water‐soluble drugs as a novel slow‐release carrier.