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As Drug Delivery
System
•Cyclodextrins (CDs) are cyclic
oligosaccharides containing at least 6
pyranose units attached
•Cyclodextrins by α-(1,
(CDs), with 4) glucosidic
lipophilic inner
cavities and hydrophilic outer surfaces,
are capable of interacting with a large
variety of guest molecules to form
inclusion complexes
•The 3 natural CDs, α-, β-, and γ-CDs
(with 6, 7, or 8 glucose units
respectively), differ in their ring size
Type Cavity Molecular Solubility
of CD Diameter Å Weight (g/100 mL)
α- cyclodextrin α- CD
β- cyclodextrin β- CD
γ- cyclodextrin γ- CD
Hydroxyethyl-β-CD HE -β-CD
Hydroxypropyl-β-CD HP-β-CD
Sulfobutylether-β-CD SBE-β-CD
Methyl-β-CD M-β-CD
Dimethyl-β-CD DM-β–CD (DIMEB)
Randomly dimethylated -β-CD RDM-β-CD
Randomly methylated-β-CD RM-β−CD (RAMEB)
Carboxymethyl - β –CD CM-β-CD
Carboxymethyl ethyl- β-CD CME-β-CD
Diethyl-β-CD DE-β-CD
Tri-O-methyl-β- CD TRIMEB
Tri-O-ethyl–β-CD TE-β-CD
Tri-O-butyryl–β-CD TB-β-CD
Tri-O-valeryl–β-CD TV-β-CD
Di-O-hexanoyl–β-CD DH-β-CD
Glucosyl-β-CD G1-β-CD
Maltosyl-β-CD G2 -β-CD
2-hydroxy-3-trimethyl-ammoniopropyl-
HTMAPCD
β-CD
tudy of CD Complexation and Dilution Effects
number of substituted hydroxyls per
glucopyranose unit of CD ring. Since the
number of reactive hydroxyls per mole of
glucopyranose unit is 3, the maximum
numbers of substituents possible for α-, β-,
and γ-CDs are 18, 21, and 24, respectively.
Average molar degree of substitution
(MS): the average number of moles of the
substituting agent, eg, hydroxypropyl, per
mole of glucopyranose. It may not
necessarily describe the extent to which the
reactive sites are substituted when the
substituting agent itself has reactive sites, or
when new reactive sites are generated
during the substitution reaction. Thus the
value of MS can be more than 3 for each
glycopyranose unit of substituted CDs, or
Degree of polymerization (DP): the ratio of
MS to DS (MS/DS). If no additional reactive
sites are produced during the substitution, MS
and DS are equal and the DP becomes 1.
CD Drug(s) Ref.
α-CD Praziquantel 75