262
solubility and dissolution of EFA. Binary and ternary complexes
were prepared with EFA, NS, and PVP K30 for comparative reasons. Results obtained confirmed inclusion complexation and the
stability constant for ternary complex (1997 lit/mole) indicates
stable complex formation. Saturation solubility was 17-fold higher
with ternary complex in distilled water and about 4-fold in
simulated gastric fluid. In vitro dissolution was improved threefold
with ternary complex. Ternary nanosponge complexes were found
to have twofold increase in oral bioavailability of efavirenz as compared to plain drug [64].
Imiquimod (IMQ) is an antiproliferative medication, which
enhances both the innate and cellular immune responses by producing proinflammatory cytokines. IMQ can induce a cellmediated immune response and increase collagen breakdown. In
addition, IMQ can modify the expression of genes associated with
apoptosis and is clinically used for the treatment of neoplastic skin
diseases. IMQ is one of the emerging options for HS (hypertrophic
scar) prevention and therapy. β-CD nanosponges cross-linked with
pyromellitic dianhydrides (IMQ-CDNS) loaded with IMQ were
prepared and their antiproliferative action on HS fibroblasts was
evaluated. CDNS are soft and swellable and form stable nanohydrogel structure on contact with water, making them very suitable
for topical applications. The percentage of water uptake increases
with the pH of the external medium and reaches the best swelling
properties at pH values over 6 (mimics the pH of the skin in HS)
due to the presence of dissociated carboxylic groups of the pyromellitic acid network [65].
CDNS can incorporate and store the drug to a good extent.
IMQ loaded in CDNS can be released with prolonged- and
controlled- release kinetics. Loaded nanosponge IMQ–NS could
act as a drug reservoir dispersed in the hydrogel, able to slowly
deliver IMQ through the skin, favoring dermal accumulation. This
behavior could allow for a reduction in the number of applications,
enhancing patient compliance. Moreover, a decrease in the irritating effect on skin might be obtained. These results might pave the
way to develop an innovative topical nanomedicine formulation for
the prevention and treatment of hypertrophic scars (Fig. 5) [66].
Many diseases and infections can be transmitted from one individual to another during sexual contact (sexually transmitted diseases, STDs). These diseases are caused by a myriad of pathogens
such as bacteria, viruses, parasites, and fungi. In immunocompromised patients, they can cause mucosal, skin, or systemic infections
which are conventionally treated with antifungal agents such as
topically or orally administered azole drugs. However, prolonged
usage of such antifungal agents, such as fluconazole, can eventually
lead to reduced susceptibility and clinical response [67]. Econazole
nitrate (EN) is a commercially available imidazole antifungal used
2.4 Cyclodextrin
Nanosponges
for Antifungal Drugs
Maria Tannous et al.
solubility and dissolution of EFA. Binary and ternary complexes
were prepared with EFA, NS, and PVP K30 for comparative reasons. Results obtained confirmed inclusion complexation and the
stability constant for ternary complex (1997 lit/mole) indicates
stable complex formation. Saturation solubility was 17-fold higher
with ternary complex in distilled water and about 4-fold in
simulated gastric fluid. In vitro dissolution was improved threefold
with ternary complex. Ternary nanosponge complexes were found
to have twofold increase in oral bioavailability of efavirenz as compared to plain drug [64].
Imiquimod (IMQ) is an antiproliferative medication, which
enhances both the innate and cellular immune responses by producing proinflammatory cytokines. IMQ can induce a cellmediated immune response and increase collagen breakdown. In
addition, IMQ can modify the expression of genes associated with
apoptosis and is clinically used for the treatment of neoplastic skin
diseases. IMQ is one of the emerging options for HS (hypertrophic
scar) prevention and therapy. β-CD nanosponges cross-linked with
pyromellitic dianhydrides (IMQ-CDNS) loaded with IMQ were
prepared and their antiproliferative action on HS fibroblasts was
evaluated. CDNS are soft and swellable and form stable nanohydrogel structure on contact with water, making them very suitable
for topical applications. The percentage of water uptake increases
with the pH of the external medium and reaches the best swelling
properties at pH values over 6 (mimics the pH of the skin in HS)
due to the presence of dissociated carboxylic groups of the pyromellitic acid network [65].
CDNS can incorporate and store the drug to a good extent.
IMQ loaded in CDNS can be released with prolonged- and
controlled- release kinetics. Loaded nanosponge IMQ–NS could
act as a drug reservoir dispersed in the hydrogel, able to slowly
deliver IMQ through the skin, favoring dermal accumulation. This
behavior could allow for a reduction in the number of applications,
enhancing patient compliance. Moreover, a decrease in the irritating effect on skin might be obtained. These results might pave the
way to develop an innovative topical nanomedicine formulation for
the prevention and treatment of hypertrophic scars (Fig. 5) [66].
Many diseases and infections can be transmitted from one individual to another during sexual contact (sexually transmitted diseases, STDs). These diseases are caused by a myriad of pathogens
such as bacteria, viruses, parasites, and fungi. In immunocompromised patients, they can cause mucosal, skin, or systemic infections
which are conventionally treated with antifungal agents such as
topically or orally administered azole drugs. However, prolonged
usage of such antifungal agents, such as fluconazole, can eventually
lead to reduced susceptibility and clinical response [67]. Econazole
nitrate (EN) is a commercially available imidazole antifungal used
2.4 Cyclodextrin
Nanosponges
for Antifungal Drugs
Maria Tannous et al.