Preparation of casein–chitosan microspheres containing diltiazem hydrochloride by an aqueous coacervation technique

Bayomi, Mohsen A.; Al‐Suwayeh, Saleh A.; El-Helw, Abdulrahim M.; Mesnad, A.F.

doi:10.1016/s0031-6865(98)00020-x

Cited by 81 publications

(40 citation statements)

References 15 publications

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“…Static angle of repose was measured according to the fixed funnel and free standing cone method [18]. A funnel with the end of the stem cut perpendicular to the axis of symmetry is secured with its tip 2 cm height, H, above a graph paper placed on a flat horizontal surface.…”

Section: Flow Properties Of Ccammentioning

confidence: 99%

Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

Zhou

Chen

2008

Front. Mater. Sci. China

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In this study, chitosan/cellulose acetate microspheres (CCAM) were prepared by W/O/W emulsification and solvent evaporation as a drug delivery system. The microspheres were spherical, free-flowing and non-aggregated. The CCAM had good flow and suspension ability. The loading efficiency of different model drugs increased with the increasing hydrophobicity of the drug. The loading efficiency of 6-mercaptopurine (6-MP) was more than 30% whereas that of ranitidine hydrochloride (RT) or acetaminophen (ACP) was only 10%. The pH values of solution affected the swelling ability of CCAM and the relative humidity had little effect on the characteristics of CCAM when it was not more than 75%. The CCAM system had a good effect on the controlled release of different model drugs. However, the release rate became slower with the increase of the hydrophobicity of drugs. The release rate of CCAM loaded with hydrophilic RT was almost 60% during 48 h and the release rate of CCAM loaded with hydrophobic drug of 6-MP was not more than 30%. In the meantime, the CCAM system was degradable in vitro and the degradation rate was faster in lysozyme solution than that in the medium of PBS. So the CCAM system was a degradable promising drug delivery system especially for hydrophobic drugs.

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Section: Flow Properties Of Ccammentioning

confidence: 99%

Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

Zhou

Chen

2008

Front. Mater. Sci. China

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“…However, the release of some drugs is reduced with an increase in drug content in the microspheres [34][35] . In these conditions, factors such as swelling, porosity, and drug solubility are determiners of drug release.…”

Section: In Vitrmentioning

confidence: 99%

Effect of crosslinking agents on chitosan microspheres in controlled release of diclofenac sodium

et al. 2005

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Abstract:In this work chitosan microspheres were prepared by the simple coacervation method and crosslinked using epichlorhydrin or glutaraldehyde for the controlled release of diclofenac sodium. The effects of the crosslinking agents on chitosan microspheres over a 12-hour period were assessed with regard to swelling, hydrolysis, porosity, crosslinking, impregnation of diclofenac sodium (DS), and consequently to the release of DS in buffer solutions, simulating the gastrointestinal tract. The degree of swelling varied with the pH for glutaraldehyde chitosan microspheres (GCM) and epichlorhydrin chitosan microspheres (ECM). Partial acid and basic hydrolysis affected the swelling behavior of the GCM matrix. Release kinetics of diclofenac sodium from these matrices were investigated at pH 1.2, 6.8 and 9.0, simulating the gastrointestinal tract conditions. The results indicated that the release mechanism deviated slightly from Fickian transport.

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“…43 Results also showed that RIVA release increased by increasing the loading drug amount. Bayomi et al 45 also reported that diltiazem release was faster from chitosan microspheres of higher drug content. The RIVA release from liposomes followed zero-order kinetics, which meant that drug release was independent on the initial drug concentration inside liposomes.…”

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confidence: 95%

Potential therapeutic effect of nanobased formulation of rivastigmine on rat model of Alzheimer's disease

Ismail¹,

ElMeshad²,

Salem³

2013

IJN

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Background:To sustain the effect of rivastigmine, a hydrophilic cholinesterase inhibitor, nanobased formulations were prepared. The efficacy of the prepared rivastigmine liposomes (RLs) in comparison to rivastigmine solution (RS) was assessed in an aluminium chloride (AlCl 3 )-induced Alzheimer's model. Methods: Liposomes were prepared by lipid hydration (F1) and heating (F2) methods. Rats were treated with either RS or RLs (1 mg/kg/day) concomitantly with AlCl 3 (50 mg/kg/day). Results:The study showed that the F1 method produced smaller liposomes (67.51 ± 14.2 nm) than F2 (528.7 ± 15.5 nm), but both entrapped the same amount of the drug (92.1% ± 1.4%). After 6 hours, 74.2% ± 1.5% and 60.8% ± 2.3% of rivastigmine were released from F1 and F2, respectively. Both RLs and RS improved the deterioration of spatial memory induced by AlCl 3 , with RLs having a superior effect. Further biochemical measurements proved that RS and RLs were able to lower plasma C-reactive protein, homocysteine and asymmetric dimethylarginine levels. RS significantly attenuated acetylcholinesterase (AChE) activity, whereas Na + / K + -adenosine triphosphatase (ATPase) activity was enhanced compared to the AlCl 3 -treated animals; however, RLs succeeded in normalization of AChE and NaGene-expression profile showed that cotreatment with RS to AlCl 3 -treated rats succeeded in exerting significant decreases in BACE1, AChE, and IL1B gene expression. Normalization of the expression of the aforementioned genes was achieved by coadministration of RLs to AlCl 3 -treated rats. The profound therapeutic effect of RLs over RS was evidenced by nearly preventing amyloid plaque formation, as shown in the histopathological examination of rat brain. Conclusion: RLs could be a potential drug-delivery system for ameliorating Alzheimer's disease.

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Preparation of casein–chitosan microspheres containing diltiazem hydrochloride by an aqueous coacervation technique

Cited by 81 publications

References 15 publications

Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

Effect of crosslinking agents on chitosan microspheres in controlled release of diclofenac sodium

Potential therapeutic effect of nanobased formulation of rivastigmine on rat model of Alzheimer's disease

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Preparation of casein–chitosan microspheres containing diltiazem hydrochloride by an aqueous coacervation technique

Cited by 81 publications

References 15 publications

Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

Effect of crosslinking agents on chitosan microspheres in controlled release of diclofenac sodium

Potential therapeutic effect of nanobased formulation of rivastigmine on rat model of Alzheimer&#39;s disease

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Potential therapeutic effect of nanobased formulation of rivastigmine on rat model of Alzheimer's disease