Darifenacin Self-assembled Liquid Crystal Cubic Nanoparticles: a Sustained Release Approach for an Overnight Control of Overactive Bladder

• Published in: AAPS PharmSciTech Vol. 24; no. 5; p. 120
• Main Authors: Farag, Michael M., El-Sebaie, Wessam, Basalious, Emad B., El-Gazayerly, Omaima N.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 12.05.2023
• Subjects: Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract; Animals; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Delayed-Action Preparations; Drug Carriers - chemistry; Liquid Crystals - chemistry; Nanoparticles - chemistry; Particle Size; Pharmacology/Toxicology; Pharmacy; Rabbits; Research Article; Urinary Bladder, Overactive - drug therapy; cubic nanoparticles; Darifenacin; permeation; liquid crystal; self-assembled; ex vivo permeation
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-023-02575-y

The current study is regarding the development and characterization of Darifenacin-loaded self-assembled liquid crystal cubic nanoparticles (LCCN). An anhydrous approach was used for the preparation of these cubic nanoparticles using a hydrotropic agent (propylene glycol), with minimal energy input. Upon dispersion in aqueous medium, the system was successfully transformed to cubosomal nanoparticles counterpart as depicted by transmission electron micrographs. A Box-Behnken design was used to optimize formulation variables, namely A: amount of GMO, B: amount of Pluronic F127, C: amount of PG, and D: amount of HPMC. The design has generated 29 formulae which were tested regarding drug content uniformity, dispersibility in water, particle size, zeta potential, polydispersity index, and in vitro release behavior. The numerical optimization algorithms have generated an optimized formula with high desirability ≈ 1. The optimized formula displayed small particle size, good homogeneity, and zeta potential along with controlled in vitro release profile and ex vivo permeation through rabbit intestine. Thus, self-assembled LCCN might offer an alternative anhydrous approach for the preparation of cubosomal nanoparticles with controlled release profile for a possibly better control of overactive bladder syndrome which tremendously affect the overall life quality. Graphical Abstract