Improved solubility and corneal permeation of PEGylated curcumin complex used for the treatment of ophthalmic bacterial infections

Abstract

Naturally occurring curcumin can be used for the treatment of corneal bacterial infections with its limitation of poor solubility. Aim of the present study was to enhance solubility and permeation of curcumin for the treatment of corneal bacterial infections. For increasing solubility, curcumin and polyethylene glycol (PEG 6000) complex (1:3) was prepared by fusion melting method. Phase solubility studies were used for the calculation of Gibbs free energy of curcumin. Central composite rotatable design (CCRD) was applied for optimization of Curcumin (CUR), PEGylated Curcumin (PEG-CUR), penetration enhancer cremophore (CR). Optimized ointments were further evaluated by mucous permeation, membrane permeability and cell toxicity studies by Transwell cell, ussing chamber and Caco-2 cells respectively. Antibacterial test was also performed by agar well diffusion method. Solubility of PEG-CUR was increased up to 93±3.2% as compared to pure curcumin and content uniformity was in the range of 95–110%. Curcumin permeation from PEG-CUR ointment was increased up to 12 folds. No toxicity of Caco-2 cells for PEG-CUR even after 24h was observed. Activity index of pure CUR, PEG-CUR ointment with or without CR against S. aureus and P. aeruginosa was 97±2.3, 96±1.6, 95±2.5% respectively. Ointment with solubility enhanced PEG-CUR and cremophore can be used as a promising tool for the treatment of corneal bacterial infections.

Development and Evaluation of an Innovative Approach Using Niosomes Based Polymeric Microneedles to Deliver Dual Antioxidant Drugs

“…Jss for different formulations was in the order: M4 (containing 7% PEG 400) > M2 (containing 7% PEG 400) > M1 (containing 5% PEG 400) > M3 (containing 5% PEG 400). The results indicate that using PVP and 7% PEG 400 together enhances skin permeation compared to using PVP and 5% PEG 400, which is in line with previous studies [73,74]. This improvement is attributed to the strong hydrophilic nature of PEG 400, which increases the solubilization of the drug and enhances partition to the aqueous phase [49].…”

Concomitant Effect of Quercetin and Its Copper Complex in the Development of Sustained-Release Nanoparticles of Polycaprolactone, Used for the Treatment of Skin Infection

“…The regression coefficient ( r ) and AIC values at various times PCL conc in the Higuchi model revealed that the drug release was diffusion-controlled, whereas no significant alteration was identified across all values (1) in the Weibull model. The Weibull model provided the best adjustment curve for Cu-Q-PCL-NPs because it had a higher α value and a lower AIC value , in comparison to Q-PCL-NPs. In the case of Cu-Q-PCL-NPs, the dissolution of Cu 2+ ions were high due to the low pH (5.5); therefore, the Cu-Q-PCL-NPs has a higher drug release than Q-PCL-NPs …”

Engineered Robust Hydrophobic/Hydrophilic Nanofibrous Scaffolds with Drug-Eluting, Antioxidant, and Antimicrobial Capacity

“…The kinetics of drug release from curcumin-loaded composites was studied in an aqueous PBS medium without any modification. According to the literature, the solubility of free curcumin in such medium is almost negligible (below 0.5 μg•ml −1 ), 57 such that modification of PBS medium with additives like Tween 80 and methanol is needed. 11 Here, the complexation of curcumin by its interaction with the hydrophilic carriers gives rise to an increased solubility of curcumin in pure aqueous PBS medium, as shown in the release profiles of Figure 6.…”