[Design Features in the Molecular-level Development of Solid Pharmaceutical Formulations Based on Supramolecular...

Area of Science:

• Materials Science
• Pharmaceutical Science
• Supramolecular Chemistry

Background:

• Cyclodextrin (CD) crystal structures possess internal cavities and inter-column spaces suitable for complex formation.
• Developing solid CD complexes can improve drug properties like solubility and stability.

Purpose of the Study:

• To develop novel solid cyclodextrin complexes for drug encapsulation and delivery.
• To investigate methods for incorporating guest drugs into CD structures.

Main Methods:

• Preparation of drug/[polyethylene glycol (PEG)/γ-cyclodextrin-polypseudoraxane (PPRX)] complexes using sealed-heating and solid-phase cogrinding/heating methods.
• Characterization of complex structure and drug molecular state using powder X-ray diffraction and solid-state NMR.

Main Results:

• Successful preparation of drug/(PEG/γ-CD-PPRX) complexes with drugs incorporated between CD columns.
• Demonstrated incorporation of various guest drugs based on molecular size and log P, following stoichiometric rules.
• Improved dissolution characteristics and thermal stability of incorporated drugs.

Conclusions:

• Solid CD complexes offer a promising platform for drug encapsulation and controlled release.
• The developed methods enable the formation of complexes with diverse drugs, including thermally unstable ones.
• These novel complexes exhibit unique structural and pharmaceutical properties beneficial for drug delivery systems.