Physicochemical characterization of spray dried ternary micro-complexes of cefuroxime axetil with hydroxypropyl-β-cyclodextrin

Shah, Manali; Pore, Yogesh; Dhawale, Shashikant C.; Burade, Kishorkumar; Kuchekar, Bhanudas S.

doi:10.1007/s10847-012-0211-z

Cited by 27 publications

(29 citation statements)

References 41 publications

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“…The in silico studies allowed to rank CA-CD systems by predicted affinities, thus to select the most favorable system. According to the published thermodynamic effect of complexation in the studies of CA-HPβCD (Ks = 382.7 M −1 ) [7] and CA-βCD (Ks = 339.7 M −1 ) [8], the predicted ranks 1 and 3, respectively, remain in agreement with experimental results. In the literature, good agreement of in silico predictions with experimental results was observed for Ibuprofen systems with β−, γ−, and HPβCD, where dG of binding was simulated with the MM-PBSA approach [30].…”

Section: Discussionsupporting

confidence: 75%

“…The CDs have proven their usability as solubilization agents in numerous pharmaceutical applications, including systems with β-lactam analogs. In the study of Shah et al, CA was complexed with hydroxypropyl-βCD (HPβCD), resulting in improved solubility [7]. A recent study on the CA-βCD system also showed an increase in the solubility of CA in the system relative to pure CA [8].…”

Section: Introductionmentioning

confidence: 99%

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Computer-Aided Design of Cefuroxime Axetil/Cyclodextrin System with Enhanced Solubility and Antimicrobial Activity

et al. 2019

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This study aimed to investigate changes in the solubility and antimicrobial efficacy of cefuroxime axetil (CA) when incorporated into cyclodextrin (CD). While choosing the CD, the validated in silico model was used. A theoretical model based on docking and molecular mechanics/generalized born surface area was validated using a curated dataset of API (active pharmaceutical ingredient)–CD stability constants. The library of commonly used cyclodextrins was virtually screened, indicating CA –hydroxypropyl-βCD (HPβCD) as the most thermodynamically favored system. Solid-state CA–HPβCD system was prepared and characterized by differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR), and X-ray diffraction (XRPD) methods. The dissolution profiles of the CA and its cyclodextrin system were evaluated. Microbiological activity of the CA–HPβCD inclusion system was studied based on changes in minimal inhibitory concentration (MIC) values and related to ones of the pure CA. The theoretical model was successfully validated, obtaining an average correlation with experimental data R = 0.7. The dissolution study showed significantly improved dissolution profiles of CA–HPβCD compared to CA. HPβCD increases the antimicrobial efficacy of CA up to 4-fold compared to pure CA.

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Section: Discussionsupporting

confidence: 75%

Section: Introductionmentioning

confidence: 99%

Computer-Aided Design of Cefuroxime Axetil/Cyclodextrin System with Enhanced Solubility and Antimicrobial Activity

et al. 2019

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“…Standard Gibbs free energy change (∆G) given by the change in enthalpy and entropy (Table-3 rable towards increasing the concentration of cyclodextrin [15,23]. DSC: DSC has become a powerful tool to investigate the interactions between host and guest.…”

Section: Resultsmentioning

confidence: 99%

in silico and Physico-Chemical Assessment of Effectiveness of Hydroxy/Amino Acids as Auxiliary Substances to Improve the Complexation Efficiency of ββ ββ β-Cyclodextrin Towards Bosentan

Pore¹,

Jadhav²

2017

Asian J. Chem.

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The effectiveness of certain hydroxy and amino acids as an auxiliary substance to improve the complexation efficiency of β-cyclodextrin towards bosentan, a poorly soluble endothelin receptor antagonist, were assessed to enhance its physico-chemical performance. The phase solubility studies conducted in distilled water demonstrated a better choice of L-arginine as an auxiliary substance to improve complexation efficiency and association constant (Ks) of β-cyclodextrin. As a complementary evidence, in silico calculations were performed to foresee the stability, possible interactions and geometry of bosentan monohydrate inside β-cyclodextrin cavity, optimizing L-arginine again as an auxiliary substance. Subsequently, the solution state thermodynamic investigations revealed entropy driven complexation process. The lyophilized complexes were characterized by FTIR, DSC, XRPD and SEM. The performance of ternary complex was found to be appreciating in overall assessment, indicating better effectiveness of L-arginine as an auxiliary substance in improving complexation efficiency of β-cyclodextrin towards bosentan monohydrate.

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“…Whereas its surface was modified after inclusion complexation preparation with carrier HPBCD & by spray drying method 38 .…”

Section: Semmentioning

confidence: 99%

Functionality Advancement of Poorly Soluble Drug by Comparative Study of Solubilizing Techniques with Molecular Simulation to in vivo evaluation

Mogal¹,

Derle²

2017

IJPTR

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:This study aimed at the functionality advancement of poorly soluble model drug i.e. Cefixime with HPBCD using comparative study of different solubility enhancement methods. CFX formulations with hydroxypropyl-β-cyclodextrin (HP-β-CD) prepared by different solubility enhancement methods viz.,physical mixture, kneading method, solvent evaporation, spray drying, lyophilization/freeze drying, microwave irradiation method and compared their solubility enhancement as well as dissolution. The optimized complexes characterized using ATR, 1H-NMR, ROSEY, XRD, SEM and DSC for confirming the complexation. In-vivo pharmacokinetic studies were performed using male wister rats (N=6) through oral route. Hydroxy propyl Beta cyclodextrin inclusion complexation prepared by spray drying method was found to be optimized for complexation with cefixime. Spray drying method was found to be better than other complexation techniques on basis of in-vitro dissolution studies. ATR, NMR, XRD, and DSC confirmed the formation of complex. The in silico anticipations for mode of incorporation were in agreeing with the experimental proton NMR measure. The bioavailability of cefixime was found to be enhanced more than3 times. In comparison to pure drug, statistically significant increase in the oral bioavailability was obtained with the HP-β-CD inclusion complex which was prepared by spray drying technique, with 347% increase in terms of Cmax. This comparative study gave idea about best suited method for solubility enhancement along with molecular docking and NMR studies for anticipating mode of inclusion & thus, ultimately, improving the oral bioavailability of CFX.

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Physicochemical characterization of spray dried ternary micro-complexes of cefuroxime axetil with hydroxypropyl-β-cyclodextrin

Cited by 27 publications

References 41 publications

Computer-Aided Design of Cefuroxime Axetil/Cyclodextrin System with Enhanced Solubility and Antimicrobial Activity

Computer-Aided Design of Cefuroxime Axetil/Cyclodextrin System with Enhanced Solubility and Antimicrobial Activity

in silico and Physico-Chemical Assessment of Effectiveness of Hydroxy/Amino Acids as Auxiliary Substances to Improve the Complexation Efficiency of ββ ββ β-Cyclodextrin Towards Bosentan

Functionality Advancement of Poorly Soluble Drug by Comparative Study of Solubilizing Techniques with Molecular Simulation to in vivo evaluation

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