5
Curcumin (CRM) is a bright yellow chemical compound produced by Curcuma longa plants. It is the principal curcuminoid of
turmeric (Curcuma longa), a member of the ginger family,
Zingiberaceae. CRM has a surprisingly wide range of beneficial
properties, including anti-inflammatory, antioxidant, chemopreventive and chemotherapeutic activity, but its low aqueous solubility, physical instability and low bioavailability make it difficult to
study [23].
Quercetin, (QUE) a plant flavonol from the flavonoid group
of polyphenols, is found in many fruits, vegetables, leaves and
grains; red onions and kale are common foods containing appreciable content of QUE [24]. It has a bitter flavor and is used as an
ingredient in dietary supplements, beverages and foods. Due to its
antioxidant properties, QUE has been considered as a potent molecule against cancer, while recently it is considered protective agent
against early inflammatory stages of Alzheimer’s disease. Its low
solubility, and thus limited bioavailability, is the primary reason for
formulating the molecule into a 2-HP-β-CD inclusion complex.
2 Materials
1. Use purified water and analytical grade guest molecules.
2. Store all guest molecules at room temperature (unless indicated
otherwise).
3. Prepare ammonium hydroxide solution by diluting 20 mL of
ammonia solution (25% v/v concentrated solution) to a final
volume of 100 mL with purified water and mix gently. The concentration of the obtained NH 4 OH solution is 5% v/v. This
solution is used for all preparations described below.
4. Use 2-HP-β-CD as the host molecule and drug carrier for solubility amelioration through a neutralization and freeze-drying
procedure in the following preparations.
3 Methods
1. Accurately weigh 60 mg of IRB and 408 mg of 2-HP-β-CD
and transfer them in a 100 mL beaker.
2. Suspend with 50 mL of water.
3. Add small amounts of ammonium hydroxide solution 5% v/v
under continuous stirring and pH monitoring until complete
dissolution. The optimum pH value is approximately 10.5 for
the complexation to take place (see Notes 1–3).
4. When complete dissolution is achieved (visual observation to
obtain clear colorless solution) fix the volume at 60 mL with
purified water.
3.1 Steps to Follow
for the Preparation
of Solid-State
Irbesartan–2-HP-β-CD
Inclusion Complex
[25, 26]
Neutralization and Freeze-Drying Technique to Prepare Drug: CD Complexes
Curcumin (CRM) is a bright yellow chemical compound produced by Curcuma longa plants. It is the principal curcuminoid of
turmeric (Curcuma longa), a member of the ginger family,
Zingiberaceae. CRM has a surprisingly wide range of beneficial
properties, including anti-inflammatory, antioxidant, chemopreventive and chemotherapeutic activity, but its low aqueous solubility, physical instability and low bioavailability make it difficult to
study [23].
Quercetin, (QUE) a plant flavonol from the flavonoid group
of polyphenols, is found in many fruits, vegetables, leaves and
grains; red onions and kale are common foods containing appreciable content of QUE [24]. It has a bitter flavor and is used as an
ingredient in dietary supplements, beverages and foods. Due to its
antioxidant properties, QUE has been considered as a potent molecule against cancer, while recently it is considered protective agent
against early inflammatory stages of Alzheimer’s disease. Its low
solubility, and thus limited bioavailability, is the primary reason for
formulating the molecule into a 2-HP-β-CD inclusion complex.
2 Materials
1. Use purified water and analytical grade guest molecules.
2. Store all guest molecules at room temperature (unless indicated
otherwise).
3. Prepare ammonium hydroxide solution by diluting 20 mL of
ammonia solution (25% v/v concentrated solution) to a final
volume of 100 mL with purified water and mix gently. The concentration of the obtained NH 4 OH solution is 5% v/v. This
solution is used for all preparations described below.
4. Use 2-HP-β-CD as the host molecule and drug carrier for solubility amelioration through a neutralization and freeze-drying
procedure in the following preparations.
3 Methods
1. Accurately weigh 60 mg of IRB and 408 mg of 2-HP-β-CD
and transfer them in a 100 mL beaker.
2. Suspend with 50 mL of water.
3. Add small amounts of ammonium hydroxide solution 5% v/v
under continuous stirring and pH monitoring until complete
dissolution. The optimum pH value is approximately 10.5 for
the complexation to take place (see Notes 1–3).
4. When complete dissolution is achieved (visual observation to
obtain clear colorless solution) fix the volume at 60 mL with
purified water.
3.1 Steps to Follow
for the Preparation
of Solid-State
Irbesartan–2-HP-β-CD
Inclusion Complex
[25, 26]
Neutralization and Freeze-Drying Technique to Prepare Drug: CD Complexes