FORMULATION AND CHARACTERIZATION OF INCLUSION COMPLEXES USING HYDROXYPROPYL-β-CYCLODEXTRIN AND FLORFENICOL WITH CHITOSAN MICROPARTICLES

Rogel, Cristian; Mendoza, Néstor; Troncoso, José; González, Javier; Plessing, Carlos von

doi:10.4067/s0717-97072011000100011

Cited by 11 publications

(5 citation statements)

References 16 publications

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“…However, at pH 8, the effect of HP-β-CD on the dissolution of EB probably has more significance, because only a 15 % of the complexed drug was dissolved 60 minutes compared to the 1% dissolved without the presence of HP-β-CD. As it was previously mentioned, the amount of drug dissolved can have a significant effect on the bioavailability and factors like the amorphous character and improved wettability of the complex may help to develop new and more efficient delivery systems for the administration of EB in fish species 21 .…”

Section: 4-ft-ir Spectroscopymentioning

confidence: 99%

Preparation and Characterization of the Emamectin Benzoate/Hydroxypropyl-B-Cyclodextrin Inclusion Complex

Torres¹,

Villa²,

González³

et al. 2011

J. Chil. Chem. Soc.

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The objective of this study was to prepare an inclusion complex of the insecticide emamectin benzoate (EB) with hydroxypropyl-β-cyclodextrin (HP-β-CD) by co-evaporation and spray drying methods. The complexation of both compounds was evaluated on the aqueous and solid state using phase solubility diagrams, differential scanning calorimetry (DSC), X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). The aqueous solubility of the inclusion complexes at pH 8 had a 2-fold increase respect to the drug alone and dissolution profiles showed a rise in the dissolution rate. These results suggest that the use of HP-β-CD could be an interesting alternative to enhance the bioavailability of EB in salmons.Key Words: Emamectin benzoate, cyclodextrin, inclusion complex, salmon.e-mail: cvonples@udec.cl 1.-INTRODUCTIONEmamectin benzoate, (4′'R)-4″-deoxy-4″-(methylamino)avermectin b1 benzoate, is one of the most widely used compounds in the salmon industry. Chemically, is a semisynthetic derivative of avermectins (Figure 1), which shows insecticide properties against the sea lice (Lepeophteirus salmonis), an ectoparasite that infests farmed salmons [1][2][3] . Unfortunately, it has been demonstrated that the efficacy of anti-infective treatments in salmons and trouts is low because is very difficult to control the dosage in medicated foods, which results in high intra-inter variability in plasma concentrations of the agents used [4][5][6] Of the approaches considered for improvement of the accuracy in the administration of EB, Glover et al. demonstrated that the intraperitoneal injection of the drug in farmed salmons resulted in higher and more predictable concentrations, but there are constraints that have relation with the manipulation of individual specimens 7 . From a point of view of the drug, one of the factors that influence the bioavailability of active compounds in living systems are their physicochemical properties like the solubility, which is often the limiting step in the absorption process. EB is a compound that has an erratic bioavailability and poor water solubility, which depends on the pH of the aqueous medium. At pH higher than 7, the solubility is drastically reduced and this is a relevant issue, because the intestinal pH of some fish can reach values of 7 -9 8 . Actually, the salmon industry is concerned about the need for optimize the therapeutic regimes, and one way to achieve predictable drug concentrations in plasma and tissues (taking into account the low and pH dependent solubility of EB) after an oral dose of a drug is improving its aqueous solubility with the use of cyclodextrins [9][10][11][12] . Of all the cyclodextrins used, hydroxypropyl-β-cyclodextrin (HP-β-CD) has been the most studied, because of its toxicological profile and better aqueous solubility [13][14][15] . Since there is no evidence of previous research, the aim of this work is to study the possibility of form an inclusion complex of EB and HP-β-CD, characterizing the...

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Section: 4-ft-ir Spectroscopymentioning

confidence: 99%

Preparation and Characterization of the Emamectin Benzoate/Hydroxypropyl-B-Cyclodextrin Inclusion Complex

Torres¹,

Villa²,

González³

et al. 2011

J. Chil. Chem. Soc.

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“…From the results of the DSC thermogram, it can be seen that there was a decrease in the melting point of the inclusion complex due to the active substance glibenclamide being mixed with hydroxypropyl-βcyclodextrin. This indicates that there has been an interaction between glibenclamide and hydroxypropyl-β-cyclodextrin which has formed an inclusion complex [23].…”

Section: Fig 3: Differential Scanning Calorimetry Analysis Of (A) Gli...mentioning

confidence: 99%

Characterization and Dissolution Rate Studies of Inclusion Complex of Glibenclamide and Hydroxypropyl-Β-Cyclodextrin Using Co-Grinding Method

Fadhila¹,

HALIM²,

ASSYIFA³

2022

Int J App Pharm

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Objective: Glibenclamide belongs to the 2nd generation sulfonylurea group as an oral antidiabetic with low solubility in water and high bioavailability in systemic circulation (Biopharmaceutical Classification System class II). This study aimed to increase the solubility and dissolution rate of glibenclamide by preparing an inclusion complex of Glibenclamide and Hydroxypropyl-β-cyclodextrin. Methods: Inclusion complexes were prepared by the co-grinding method in two ratios 1:1 and 1:2 mol. Characterizations of inclusion complex were carried out by Scanning Electron Microscopy (SEM), Fourier Transform Infrared (FT-IR) spectroscopy, Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) analysis. Solubility test was carried out in CO2-free distilled water and dissolution rate was carried out in phosphate buffer pH 7.4. Results: The results of the SEM analysis showed changes in particle morphology. FT-IR spectroscopy shows a shift in wavenumber. DSC analysis showed a decrease in the melting point of the inclusion complex. XRD characterization results showed a decrease in the intensity of the inclusion complex. Solubility of inclusion complex of glibenclamide increased nine times 1:1 mol inclusion complex, twelve times 1:2 mol inclusion complex compared to intact glibenclamide. The dissolution of glibenclamide, inclusion complex 1:1, and inclusion complex 1:2 in phosphate buffer pH 7.4 medium at 60 min was 17.19%, 34.15% and 52.83% respectively. Conclusion: Based on the results of the study, it can be said that the glibenclamide inclusion complex with Hydroxypropyl-β-cyclodextrin successfully increases the solubility and dissolution rate of glibenclamide significantly.

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“…Chitosan is a biocompatible and biodegradable polymer, widely used in NPs for drug delivery. Three methods of complex preparation were used to obtain a ternary system of florfenicol (FF) with HP-β-CD and chitosan NPs [ 130 ]. In vitro studies showed that the FF solubility almost doubled, and a better dissolution profile was exhibited by the product prepared by spray-drying.…”

Section: Modern Drug-delivery Systemsmentioning

confidence: 99%

“…Drug release from FF microparticles was analysed in HCl of pH 1.2 (simulated gastric media), showing a better profile with dissolution greater than 80% after 15 min for FF/HP-β-CD/chitosan compared to FF alone (less than 10%) and FF/chitosan microparticles (not higher than 50%). The authors postulated that the retardant effect of chitosan could be explained by the slow diffusion of the drug through the more hydrophilic chitosan/HP-β-CD matrix layer around the lipophilic drug [ 130 ].…”

Section: Modern Drug-delivery Systemsmentioning

confidence: 99%

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

Boczar

Michalska

2022

Pharmaceutics

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Cyclodextrins (CDs) are a family of cyclic oligosaccharides, consisting of a macrocyclic ring of glucose subunits linked by α-1,4 glycosidic bonds. The shape of CD molecules is similar to a truncated cone with a hydrophobic inner cavity and a hydrophilic surface, which allows the formation of inclusion complexes with various molecules. This review article summarises over 200 reports published by the end of 2021 that discuss the complexation of CDs with antibiotics and antibacterial agents, including beta-lactams, tetracyclines, quinolones, macrolides, aminoglycosides, glycopeptides, polypeptides, nitroimidazoles, and oxazolidinones. The review focuses on drug-delivery applications such as improving solubility, modifying the drug-release profile, slowing down the degradation of the drug, improving biological membrane permeability, and enhancing antimicrobial activity. In addition to simple drug/CD combinations, ternary systems with additional auxiliary substances have been described, as well as more sophisticated drug-delivery systems including nanosponges, nanofibres, nanoparticles, microparticles, liposomes, hydrogels, and macromolecules. Depending on the desired properties of the drug product, an accelerated or prolonged dissolution profile can be achieved when combining CD with antibiotics or antimicrobial agents.

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FORMULATION AND CHARACTERIZATION OF INCLUSION COMPLEXES USING HYDROXYPROPYL-β-CYCLODEXTRIN AND FLORFENICOL WITH CHITOSAN MICROPARTICLES

Cited by 11 publications

References 16 publications

Preparation and Characterization of the Emamectin Benzoate/Hydroxypropyl-B-Cyclodextrin Inclusion Complex

Preparation and Characterization of the Emamectin Benzoate/Hydroxypropyl-B-Cyclodextrin Inclusion Complex

Characterization and Dissolution Rate Studies of Inclusion Complex of Glibenclamide and Hydroxypropyl-Β-Cyclodextrin Using Co-Grinding Method

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

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