Cocrystal formulations: A case study of topical formulations consisting of ferulic acid cocrystals

[Display omitted] Renaissance of cocrystals as alternative solid forms for fine-tuning physicochemical properties of active pharmaceutical ingredients (APIs) has paved way for development of marketable cocrystals. The current literature reveals established strategies for the design, synthesis and ch...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2020-04, Vol.149, p.95-104
Main Authors: Aitipamula, Srinivasulu, Das, Surajit
Format: Article
Language:English
Subjects:
Cocrystals
Ferulic acid
Permeability
Pharmaceutical
Physicochemical properties
Stability
Topical formulations
X-ray diffraction
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Summary:[Display omitted] Renaissance of cocrystals as alternative solid forms for fine-tuning physicochemical properties of active pharmaceutical ingredients (APIs) has paved way for development of marketable cocrystals. The current literature reveals established strategies for the design, synthesis and characterization of cocrystals. However, barring a few isolated case studies, strategies for development of cocrystal formulations have been underdeveloped. Herein we report topical formulations of an antioxidant, ferulic acid (FA), which contain the active in its cocrystal form. Cocrystals of FA with the coformers relevant to skin care such as urea, nicotinamide (NA) and isonicotinamide (INA) have been prepared and oleogel formulations of these have been developed. The cocrystal with urea and an anhydrous cocrystal with INA have been identified for the first time in this study. The novel cocrystals were structurally characterized by single crystal X-ray diffraction. Solubility and stability studies have revealed higher solubility of the cocrystals with NA and INA than the parent active and greater stability of FA in formulations that contained the cocrystals with INA and urea than the corresponding formulations containing physical mixtures or parent active. In vitro membrane permeation tests have ascertained sustained release profile of active from the formulation that contained the FA•INA cocrystal. The higher solubility, greater stability and sustained active release profile of the FA•INA cocrystal formulation make it a promising topical formulation of FA.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2020.01.021