Abstract

Owing to their unique structural features, non-lamellar liquid crystalline nanoparticles comprising cubosomes and hexosomes are attracting increasing attention as versatile investigative drug carriers. Background: Depending on their physiochemical characteristics, drug molecules on entrapment can modulate and reorganize structural features of cubosomes and hexosomes. Therefore, it is important to assess the effect of guest molecules on broader biophysical characteristics of non-lamellar liquid crystalline nanoparticles, since drug-induced architectural, morphological, and size modifications can affect the biological performance of cubosomes and hexosomes. Methods: We report on alterations in morphological, structural, and size characteristics of nanodispersions composed from binary mixtures of glycerol monooleate and vitamin E on thymoquinone (a molecule with wide therapeutic potentials) loading. Results: Thymoquinone loading was associated with a slight increase in the mean hydrodynamic nanoparticle size and led to structural transitions from an internal biphasic feature of coexisting inverse cubic Fd3m and hexagonal (H2) phases to an internal inverse cubic Fd3m phase (micellar cubosomes) or an internal inverse micellar (L2) phase (emulsified microemulsions, EMEs). We further report on the presence of “flower-like” vesicular populations in both native and drug-loaded nanodispersions. Conclusions: These nanodispersions have the potential to accommodate thymoquinone and may be considered as promising platforms for the development of thymoquinone nanomedicines.

Highlights

  • Nigella sativa, commonly known as black cumin, fennel flower, and kalonji, is an annual herbaceous plant with a rich religious and historical background [1,2,3]

  • We examine the effect of TQ loading on the structural and morphological features of non-lamellar liquid crystalline nanoparticles from a binary lipid mixture consisting of glycerol monooleate (GMO), which is the most investigated lipid with non-lamellar liquid crystalline phase forming propensity, and vitamin E (Vit E)

  • The interior organization of GMO/Vit E nano-self-assemblies stabilized with different concentrations of TPGS-PEG2000 (0.75–1.5 wt%) was studied by synchrotron small angle X-ray scattering (SAXS)

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Summary

Introduction

Commonly known as black cumin, fennel flower, and kalonji, is an annual herbaceous plant with a rich religious and historical background [1,2,3]. Despite its broad therapeutic potentials, there are major concerns and limitations (including low solubility in water, poor bioavailability, poor membrane penetration capacity, and lack of mechanistic understanding of the drug action) hindering the translational development of TQ-based formulations [4,5,9,10]. Overcoming these limitations might be achieved through the rational design of nanoparticulate formulations for TQ delivery [4,8,11,15,16,17,18]. We further report on TQ encapsulation efficiency and the effect of ageing on the mean nanoparticles sizes within 30 days of post-preparation of structurally optimized samples

Results and Discussion
Cryo-transmission
Effect
Materials
Encapsulation Efficiency
Concluding Remarks
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