Abstract:Grape seed extract (GSE) displays strong antioxidant activity, but its instability creates barriers to its applications. Herein, three HP-β-CD/GSE inclusion complexes with host–guest ratios of 1:0.5, 1:1, and 1:2 were successfully prepared by co-precipitation method to improve stability. Successful embedding of GSE in the HP-β-CD cavity was confirmed by fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM) analys… Show more
“…The FT-IR spectra of HP-β-CD consisted of the prominent absorption band of the 1034 cm −1 (C-C stretching vibrations), 1085 cm −1 (C-O stretching vibrations), 1158 cm −1 (symmetric C-O-C stretching vibrations), 1654 cm −1 (H-OH bending vibrations), 2973 cm −1 (symmetric and a symmetric C-H stretching vibrations in CH 2 and CH 3 groups in in hydroxypropyl parts) and 3411 cm −1 (OH stretching vibrations). Furthermore, in the range of 1200–1500 cm −1 there are bands associated with bending vibrations of C-H and O-H bonds [ 29 , 30 , 31 , 32 , 33 ].…”
Section: Resultsmentioning
confidence: 99%
“…The formation of the complex carries the limitations of bending and stretching vibrations of the guest molecules. The literature often indicates changes in the intensity of the mentioned bands and/or their shifts in the recorded absorption spectra [ 31 , 34 , 35 ]. The broad band corresponding from OH bonds (3411 cm −1 ) in HP-β-CD consistently appears in the tedizolid/HP-β-CD complex.…”
Section: Resultsmentioning
confidence: 99%
“…However, it should be noted that it is broaden and shifted towards shorter wavelengths. According to literature, it may be related to the formation of hydrogen bonds between tedizolid and cyclodextrin [ 29 , 30 , 31 ]. The numerous bands present in the spectrum of pure tedizolid in the range of 950–1200 cm −1 in the complex have largely been obscured by the characteristic absorption peaks of HP-β-CD (C-C (1034 cm −1 ), C-O (1084 cm −1 ) and C-O-C (1158 cm −1 ) stretching vibrations).…”
Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-β-cyclodextrin (tedizolid/HP-β-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives.
“…The FT-IR spectra of HP-β-CD consisted of the prominent absorption band of the 1034 cm −1 (C-C stretching vibrations), 1085 cm −1 (C-O stretching vibrations), 1158 cm −1 (symmetric C-O-C stretching vibrations), 1654 cm −1 (H-OH bending vibrations), 2973 cm −1 (symmetric and a symmetric C-H stretching vibrations in CH 2 and CH 3 groups in in hydroxypropyl parts) and 3411 cm −1 (OH stretching vibrations). Furthermore, in the range of 1200–1500 cm −1 there are bands associated with bending vibrations of C-H and O-H bonds [ 29 , 30 , 31 , 32 , 33 ].…”
Section: Resultsmentioning
confidence: 99%
“…The formation of the complex carries the limitations of bending and stretching vibrations of the guest molecules. The literature often indicates changes in the intensity of the mentioned bands and/or their shifts in the recorded absorption spectra [ 31 , 34 , 35 ]. The broad band corresponding from OH bonds (3411 cm −1 ) in HP-β-CD consistently appears in the tedizolid/HP-β-CD complex.…”
Section: Resultsmentioning
confidence: 99%
“…However, it should be noted that it is broaden and shifted towards shorter wavelengths. According to literature, it may be related to the formation of hydrogen bonds between tedizolid and cyclodextrin [ 29 , 30 , 31 ]. The numerous bands present in the spectrum of pure tedizolid in the range of 950–1200 cm −1 in the complex have largely been obscured by the characteristic absorption peaks of HP-β-CD (C-C (1034 cm −1 ), C-O (1084 cm −1 ) and C-O-C (1158 cm −1 ) stretching vibrations).…”
Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-β-cyclodextrin (tedizolid/HP-β-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives.
“…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.…”
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.
“…In the present study, an extraction and encapsulation of components of propolis in a combinatorial liposome–cyclodextrin system is performed. The particular properties of both carriers that were taken in advantage are: The ability of the cyclodextrins to enclose polyphenols and enhance their permeability through the skin [ 38 , 39 ] as well as the ability of the liposomes to encapsulate large quantities of components of various degrees of polarities, for topical transport of components and control of their release rate [ 40 , 41 , 42 ].…”
Propolis is a resinous substance produced by bees that exhibits antimicrobial, immunostimulatory and antioxidant activity. Its use is common in functional foods, cosmetics and traditional medicine despite the fact that it demonstrates low extraction yields and inconsistency in non-toxic solvents. In this work, a new encapsulation and delivery system consisting of liposomes and cyclodextrins incorporating propolis polyphenols has been developed and characterized. The antioxidant, antimutagenic and antiaging properties of the system under normal and UVB-induced oxidative stress conditions were investigated in cultured skin cells and/or reconstituted skin model. Furthermore, the transcript accumulation for an array of genes involved in many skin-related processes was studied. The system exhibits significant polyphenol encapsulation efficiency, physicochemical stability as well as controlled release rate in appropriate conditions. The delivery system can retain the anti-mutagenic, anti-oxidative and anti-ageing effects of propolis polyphenols to levels similar and comparable to those of propolis methanolic extracts, making the system ideal for applications where non-toxic solvents are required and controlled release of the polyphenol content is desired.
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