Phase transited asymmetric membrane floating nanoparticles: a means for better management of poorly water-soluble drugs.

Abstract

Purpose: Effective remedy to gastrointestinal (GI) side effects caused by poorly water-soluble drugs remains a challenge. Researching for novel techniques to reduce these side effects and increase patient adherence to medical treatment is of interest. The current study aims to develop an innovative nano-sized gastro-retentive drug delivery for better management of poorly water-soluble drugs.

Method: A non-disintegrating ibuprofen-asymmetric membrane floating nanoparticle (Ibuprofen-AMFNP) was prepared by phase inversion technique to increase the gastric residence of the drug. Powder characterization, solubility, in vitro buoyancy, effect on in vivo inflammatory markers, and polymer diffusibility studies were conducted on the prepared formulation. All UV-spectrophotometric analysis was accomplished through a fiber optic system.

Results: The prepared Ibuprofen-AMFNPs were in the nano range of 114.45 nm ±1.31 nm. The formulation was buoyant for 12 h in the dissolution media indicating increased gastric residence, had better solubility and powder characteristics compared to the pure drug. Scanning electron microscopy revealed an outer non-porous and inner porous asymmetric membrane. Ibuprofen-AMFNP followed Higuchi drug release kinetics (p=0.9925) and had a Fickian diffusion release mechanism (n=0.05). Polymer diffusibility study showed that the 24 h stored formulation had faster drug release with no lag time (-923.08 nm/h) compared to a fresh formulation (2526.32 nm/h). The prepared nano-formulation showed a higher percentage of anti-inflammatory (85.144%) effect compared to the pure drug (78.336%).

Conclusion: Ibuprofen-AMFNP is envisioned to help reduce drug-related GI side effects, improve drug delivery, and thereby increase patient adherence to medical treatment.