Abstract:This study aims at modifying curcumin to curcumin pyrazole and complexing it with HPβCD employing a simple protocol to improve curcumin's chemical–physical properties and biological activities.
“…In vitro cytotoxicity study is commonly employed to evaluate the potential of samples to induce cell death. 39 The results displayed in Fig. 8 showed that the in vitro cytotoxicity of samples was improved with the increase of sample concentration.…”
Cannabidiol (CBD), a natural phenolic compound, has many promising biological activities, but its use in food or other fields is restricted owing to inferior water solubility. So hydroxypropyl-β-cyclodextrin (HP-β-CD) was...
“…In vitro cytotoxicity study is commonly employed to evaluate the potential of samples to induce cell death. 39 The results displayed in Fig. 8 showed that the in vitro cytotoxicity of samples was improved with the increase of sample concentration.…”
Cannabidiol (CBD), a natural phenolic compound, has many promising biological activities, but its use in food or other fields is restricted owing to inferior water solubility. So hydroxypropyl-β-cyclodextrin (HP-β-CD) was...
“…Large irregular particles of commercial nimodipine (Nim) are depictable in Figure 5 [ 29 ], while spherical shells with circular holes of hydroxypropyl-β-cyclodextrin, (Hp-β-CD), with a particle ranging from 25 to 100 μm, are shown in Figure 5 [ 30 ]. For methyl-β-cyclodextrin, Me-β-CD, fragments of spherical shells are presented in Figure 5 [ 31 ].…”
The aim of the present study was to manufacture new orally disintegrating tablets containing nimodipine–hydroxypropyl-β-cyclodextrin and nimodipine–methyl-β-cyclodextrin inclusion complexes. For obtaining a better quality of the manufactured tablets, three methods of the preparation of inclusion complexes, in a 1:1 molar ratio, were used comparatively; namely, a solid-state kneading method and two liquid state coprecipitation and lyophilization techniques. The physical and chemical properties of the obtained inclusion complexes, as well as their physical mixtures, were investigated using Fourier transformed infrared spectroscopy, scanning electron microscopy, X-ray diffraction analyses, and differential scanning calorimetry. The results showed that the lyophilization method can be successfully used for a better complexation. Finally, the formulation and precompression studies for tablets for oral dispersion, containing Nim–HP-β-CD and Nim–Me-β-CD inclusion complexes, were successfully assessed.
“…In both physical mixtures, curcumin peak was broadened and shifted to slightly lower wavelength (3441 cm −1 ) suggestive of slight hydrogen bond formation. However, in the spectra of the improved SD/P4 and 6, the complete absence of curcumin peak along with other identifying peaks in the 1700–1500 cm −1 region, along with the shift of HPβCD peaks to lower wavelength (3398 cm −1 ), might indicate possible formation of inclusion complex, 80 , 81 possibly through hydrogen bond formation with –OH of curcumin. Figure 4 FT-IR spectra of ( A ) curcumin, ( B ) lecithin, ( C ) cholesterol, ( D ) SA, ( E ) PLX 188, ( F ) HPβCYD, ( G ) SD/P4 improved physical mixture, ( H ) SD/P6 improved physical mixture, ( I ) improved SD/P4 formulation and ( J ) improved SD/P6 formulation.…”
“…Again, we can notice the absence of curcumin peak, which when considered together with the shift and intensive broadening of HPβCD peak, further indicate the possible formation of inclusion complex. 80 , 81 …”
“…In both physical mixtures, curcumin peak was broadened and shifted to slightly lower wavelength (3441 cm −1 ) suggestive of slight hydrogen bond formation. However, in the spectra of the improved SD/P4 and 6, the complete absence of curcumin peak along with other identifying peaks in the 1700-1500 cm −1 region, along with the shift of HPβCD peaks to lower wavelength (3398 cm −1 ), might indicate possible formation of inclusion complex, 80,81 possibly through hydrogen bond formation with -OH of curcumin.…”
Purpose
The goal was to directly deliver curcumin, a natural polyphenolic anticancer and anti-inflammatory compound, to the lung tissues with minimal systemic exposure through the fabrication of proliposomes, overcoming its poor aqueous solubility and oral bioavailability.
Methods
Nano-spray drying was employed to prepare proliposomes using hydroxypropyl beta-cyclodextrin as a carrier. Lecithin and cholesterol were used as lipids, stearylamine and Poloxamer 188 were added as positive charge inducer and a surfactant, respectively. Different characterization parameters were evaluated like percentage yield, entrapment efficiency, drug loading, aerodynamic particle size, in vitro release besides morphological examination. Cytotoxicity studies on cell line A549 lung tumor cells as well as in vivo lung pharmacokinetic studies were also carried.
Results
The optimized formulations showed superior aerosolization properties coupled their enhanced ability to reach deep lung tissues with a high % of fine particle fraction. Cytotoxicity studies using MTT assay demonstrated enhanced growth inhibitory effect on lung tumor cells A549 and significant reduction of proinflammatory cytokines such as tumor necrosis factor-α, interleukin-6 and interleukin-10 compared to the pure drug. Results of lung pharmacokinetic tests confirmed the superiority of proliposomal curcumin over curcumin powder in both, the rate and extent of lung tissue absorption, as well as the mean residence time within the lung tissues.
Conclusion
The pulmonary delivery of curcumin-loaded proliposomes as dry powder provides a direct approach to lung tissues targeting while avoiding the limitations of the oral route and offering a non-invasive alternative to the parenteral one.
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