Enhanced Ocular Drug Delivery of Dexamethasone Using Chitosan-Coated Soluplus® Based Mixed Micellar System

Abstract

Background: This study introduces a novel dexamethasone (DEX) mixed micellar system (DEX-MM) using Soluplus® and Pluronic F-127 (PF127) to enhance ocular drug delivery. The enhancement of ocular application properties was achieved by creating a chitosan-coated DEX-MM (DEX-CMM), which promotes better adherence to the ocular surface, thereby improving drug absorption;

Methods: Using the solvent evaporation method, a formulation was developed with a Soluplus® to drug ratio of 1:10, enhanced with 0.25% PF127. After dispersing in water, 1% chitosan (CS) was added. The stability and integrity of DEX within the micelles were verified using attenuated total reflection-fourier transform infrared spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC). Additionally, in vitro and ex vivo drug release studies were conducted;

Results: DEX-CMM (F6) demonstrated a particle size of 151.9±1 nm and a polydispersity index (PDI) of 0.168±0.003, suggesting uniformity and high electrostatic stability with a zeta potential of +35.96±2.13 mV. The non-Fickian drug release mechanism indicated prolonged drug retention. Comparative analyses showed DEXCMM outperforming a standard DEX suspension in drug release and ocular tissue permeation, with flux measurements significantly higher than the DEX suspension;

Conclusion: The study confirmed the efficacy of DEX-CMM in enhancing drug delivery to ocular tissues, evidenced by improved permeability. Safety evaluations using the HET-CAM test demonstrated that DEX-CMM was non-irritant, supporting its potential for effective ocular drug delivery.

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Materials

Low molecular weight chitosan (STBH6262), and Pluronic F-127 (BCCB3537) were purchased from Sigma-Aldrich® (Missouri, USA). Dexamethasone (AB115220) was purchased from ABCR GmbH (Karlsruhe, Germany). Soluplus® (402932-23-4) was a gift from BASF Pharma (New Jersey, USA). Glacial acetic acid and ethanol was purchased from Honeywell®, (Raunheim, Germany). Acetonitrile HPLC grade was purchased from Sisco Research Laboratories Pvt Ltd (Mumbai, India).

Adwan, S.; Al-Akayleh, F.; Qasmieh, M.; Obeidi, T. Enhanced Ocular Drug Delivery of Dexamethasone Using Chitosan-Coated Soluplus® Based Mixed Micellar System. Preprints 2024, 2024091939. https://doi.org/10.20944/preprints202409.1939.v1