Effect of β-cyclodextrin and hydroxypropyl β-cyclodextrin complexation on physicochemical properties and antimicrobial activity of cefdinir

Aleem, Omair; Kuchekar, Bhanudas S.; Pore, Yogesh; Late, Sameer

doi:10.1016/j.jpba.2008.02.006

Cited by 112 publications

(70 citation statements)

References 15 publications

(13 reference statements)

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“…In FD sample it can be observed that the OME absorption band at 1625.99 cm -1 has disappeared, appearing a band at 1647.81 cm -1 (Fig. 3e), which is characteristic of HPβCD and corresponds to the elongation of the H-O-H bonds [20]. The intensity of the band at 1203.31 cm -1 is also significantly decreased.…”

Section: Infrared Spectroscopy (Ir)mentioning

confidence: 91%

Stability and enzymatic studies with omeprazole:hydroxypropyl-β-cyclodextrin

Ramos

Salústio

Serralheiro

et al. 2010

J Incl Phenom Macrocycl Chem

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Omeprazole (OME) exhibits low stability to light, heat and humidity. In stress conditions OME stability should improve under inclusion complex form with hydroxypropyl-β-cyclodextrin (HPβCD). Stability of OME, its physical mixture (PM) with HPβCD and OME:HPβCD inclusion complex was assessed during 60 days. The inclusion complexes were prepared by kneading and freezedrying techniques and characterized by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). A molecular modelling was also held to predict the most probable tridimensional conformation of inclusion complex OME:HPβCD. The inhibitory activity of free and complexed OME on selected enzymes, namely, papain (protease model of the proton pump) and acetylcholinesterase (enzyme present in cholinergic neurons and also involved in Alzheimer's disease) was compared. The results obtained show that HPβCD do not protect against OME degradation, in any prepared powder, in the presence of light, heat and humidity. This may indicate that the reactive group of OME is not included in the HPβCD cavity. This fact is supported by molecular modelling data, which demonstrated that 2-pyridylmethyl group of OME is not included into the cyclodextrin cavity. In relation to enzymatic assays it was observed that free OME and OME in the binary systems showed identical inhibitory activity on papain and acethylcolinesterase, concluding that HPβCD do not affect OME activity on these two enzymes.

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Section: Infrared Spectroscopy (Ir)mentioning

confidence: 91%

Stability and enzymatic studies with omeprazole:hydroxypropyl-β-cyclodextrin

Ramos

Salústio

Serralheiro

et al. 2010

J Incl Phenom Macrocycl Chem

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“…NM (1667 mg) was added and kneaded for 60 min with successive addition of ethanol-water mixture to obtain the desired paste consistency. The formed complex was dried in vacuum oven for 24 h at 50 o C. Dried product was scraped, passed through a 60# mesh sieve and stored in a desiccator until further use [14,16,17].…”

Section: Kneading Methodsmentioning

confidence: 99%

Enhancement of Aqueous Solubility and Oral Bioavailability of Nelfinavir by Complexation with β- Cyclodextrin

Kumari¹,

Bhawar²,

Musmade³

et al. 2015

Trop. J. Pharm Res

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“…However, CFX-HPBCD spray dried has shown significant and highest zone of inhibition against both the microorganisms as compared to pure CFX alone and other binary systems. The greater antimicrobial activity of CFX-HPBCD spray dried may be due to the ability of HPBCD to release the drug readily from the inclusion complexation 43 . In-Vivo absorption study in wistar rats:…”

Section: Antimicrobial Studiesmentioning

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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Effect of β-cyclodextrin and hydroxypropyl β-cyclodextrin complexation on physicochemical properties and antimicrobial activity of cefdinir

Cited by 112 publications

References 15 publications

Stability and enzymatic studies with omeprazole:hydroxypropyl-β-cyclodextrin

Stability and enzymatic studies with omeprazole:hydroxypropyl-β-cyclodextrin

Enhancement of Aqueous Solubility and Oral Bioavailability of Nelfinavir by Complexation with β- Cyclodextrin

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

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