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Area of Science:

  • Materials Science
  • Pharmaceutical Science
  • Nanotechnology

Background:

  • Improving drug solubility and release is crucial for enhancing active pharmaceutical ingredient (API) uptake.
  • Higher energy polymorphs can improve drug dissolution and bioavailability.
  • Nanocellulose materials offer a high surface area for modifications to influence API crystallization.

Purpose of the Study:

  • To utilize cellulose nanocrystals (CNCs) to create organogels for promoting the crystallization of specific API polymorphs.
  • To investigate the influence of CNC-based organogels on the polymorphic forms of selected sulfonamide drugs.
  • To optimize the composition and preparation of CNC-organogels for heterogeneous crystallization.

Main Methods:

  • Oxidation of CNCs and subsequent mixing with octadecylamine (ODA) surfactant in dimethylsulfoxide (DMSO) to form organogels.
  • Incorporation of APIs (sulfamethoxazole, sulfapyridine, sulfamerazine) into the gel mixture prior to gelation.
  • Analysis of the crystalline forms of APIs recovered from the CNC organogels using techniques like X-ray diffraction (XRD).

Main Results:

  • Sulfamethoxazole was recovered in an amorphous state from the CNC organogels.
  • Sulfapyridine crystallized into a mixture of polymorphs (forms I, III, and IV), differing from its as-received form.
  • Sulfamerazine crystallized into polymorphs I and II, also distinct from its original crystalline form.

Conclusions:

  • Cellulose nanocrystal organogels can effectively induce heterogeneous crystallization of APIs into desired polymorphic forms.
  • This approach demonstrates potential for the rational design of nanocellulose-based systems for controlling pharmaceutical crystallization.
  • The developed organogel system shows promise for improving drug solubility and bioavailability through tailored polymorph selection.