FORMULATION, OPTIMIZATION AND EVALUATION OF MEBENDAZOLE NANOSUSPENSION: AN APPROACH TO ENHANCE DISSOLUTION

Objectives

The objective of this study is to develop a mebendazole (MBZ) nanosuspension designed as an immediate-release dosage form to improve solubility and bioavailability.

Material and Methods

MBZ, classified as a BCS Class II drug, demonstrates low bioavailability (<10%) due to its limited solubility (0.035 mg/mL). The wet-media milling technique was utilised to reduce particle size, which subsequently increased surface area and dissolution rate. Polyvinyl alcohol (PVA) has been chosen as the stabiliser to improve formulation stability and inhibit particle aggregation. A comprehensive factorial design was employed to optimise critical process parameters, resulting in a nanosuspension characterised by an optimized mean particle size and a polydispersity index (PDI).

Results:

The optimised formulation exhibited an 8.72-fold enhancement in solubility and achieved over 98% drug release within 60 minutes in vitro, markedly surpassing both pure MBZ and existing marketed formulations. The formulation demonstrated a high entrapment efficiency of 96.21% and a drug content of 97.53%, thereby ensuring optimal drug loading. The successful conversion of MBZ into the amorphous form was confirmed through differential scanning calorimetry (DSC). The freeze-drying process enhanced dissolution properties while preserving formulation integrity, stability, and long-term viability. The solubility of the nanosuspension exhibited a significant increase in both aqueous and acidic media, effectively addressing the dissolution-limited absorption of MBZ.

Conclusions:

The findings indicate that nanosuspension technology represents a viable approach for enhancing the dissolution of poorly soluble drugs. The research highlights the potential use of nanosuspensions in drug delivery, especially for BCS Class II compounds, providing an effective formulation strategy to improve pharmacokinetic performance, stability, safety, and therapeutic results.