Evaluation of carboxymethyl-β-cyclodextrin with acid function: Improvement of chemical stability, oral bioavailability and bitter taste of famotidine

Mady, Fatma M.; Aboutaleb, A.; Khaled, Khaled A.; Yamasaki, Keishi; Iohara, Daisuke; Taguchi, Kazuaki; Anraku, Makoto; Hirayama, Fumitoshi; Uekama, Kaneto; Otagiri, Masaki

doi:10.1016/j.ijpharm.2010.06.018

Cited by 50 publications

(34 citation statements)

References 31 publications

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“…Powder was also prepared for oral suspension, but after reconstitution its stability was limited to thirty days only and also had extremely bitter taste [12]. Hence, researchers also tried numerous techniques to mask its bitter taste [13]. Hydrophobic nature of famotidine reduces its water solubility and also exposure to gastric degradation contributes to its variable and poor oral bioavailability [14].…”

Section: Introductionmentioning

confidence: 99%

Fabrication, Characterization, and In Vivo Evaluation of Famotidine Loaded Solid Lipid Nanoparticles for Boosting Oral Bioavailability

Shafique

Khan

et al. 2017

Journal of Nanomaterials

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Famotidine as H 2 receptor has antagonistic effects on gastric secretion. Unfortunately, its hydrophobic nature contributes to its variable and poor oral bioavailability. In the current study efforts are being made to fabricate famotidine loaded solid lipid nanoparticles with narrow size distribution. Prepared nanoformulations were pharmaceutically evaluated to confirm the desired boosted oral bioavailability. Famotidine loaded nanoformulation (FFSe-4) showed particle size 111.9±1.3 nm, polydispersity index 0.464 ± 0.03, zeta potential −33.46 ± 2 mV, entrapment efficiency 84 ± 2.7%, and drug loading capacity 2.709 ± 0.13%. Drugexcipients compatibility was confirmed by Fourier transformed infrared spectroscopy. Scanning electron microscopy confirmed spherical shaped, nanosized particles. Differential scanning calorimetry and powder X-ray diffractometry confirmed the change in crystalline nature. Prepared nanoformulation was more stable at refrigerated temperature. In vitro study showed that drug release time is proportional to drug pay load and followed zero order kinetics. Release exponent ( > 0.5) confirmed non-Fickian-diffusion mechanism for drug release. In vivo pharmacokinetic studies showed 2.06-fold increase in oral bioavailability of famotidine dispersed in solid lipid nanoparticles compared to commercial product. These results authenticate solid lipid nanoparticles as drug delivery system and propose prolonged release with improved oral bioavailability for famotidine.

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Section: Introductionmentioning

confidence: 99%

Fabrication, Characterization, and In Vivo Evaluation of Famotidine Loaded Solid Lipid Nanoparticles for Boosting Oral Bioavailability

Shafique

Khan

et al. 2017

Journal of Nanomaterials

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“…[74] In another study, inclusion complexes of famotidine were formulated with carboxymethyl-β-cyclodextrin and pronounced enhancement effect on chemical stability in acidic environment of the drug. [75] Improvement in the chemical stability of Voriconazole was also observed by formulating inclusion complexes with cyclodextrin.…”

Section: Thermal Stabilitymentioning

confidence: 97%

“…[76] The formation of inclusion complexes of catechin with β-CD s showed the higher storage stability and provided more protection against temperature, oxygen, and light. [51] Sulfamethoxazole β-CD Enhance bioavailability and dissolution rate [67] Eslicarbazepine acetate β-CD Faster onset of action and higher bioavailability [69] Polylactic acid β-CD Improve the thermal expansion stability [72] Chimonanthus praecox β-CD Enhancement of antioxidant activity and thermal stability [73] Famotidine Carboxymethyl β-CD Improvement of chemical stability, oral bioavailability, and bitter taste [75] Astaxanthin HP-β-CD Storage stability and antioxidant activity [76] Catechin β-CD Protection of antioxidants, higher storage stability against temperature, oxygen, and light [51] α-tocopherol β-CD Higher antioxidant activity and better UV-light stability.…”

Section: Storage Stabilitymentioning

confidence: 99%

Untitled

Budhwar¹

2018

AJP

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Inclusion complexes have various applications in different fields of drug delivery and pharmaceutical industry due to their ability of complexation with guest molecules and enhancement of the physicochemical properties of guest molecules. Cyclodextrins and their derivatives have the ability to encapsulate the bioactive compounds into its cavity and protect these from the environmental conditions, improve the solubility, bioavailability, and other properties also. The aim of this review is to highlight the advantages of cyclodextrins in the enhancement of physicochemical properties of drugs (such as solubility, stability, bioavailability, permeability, and others), different methods for production and various characterization techniques used for evaluation of complexes. Applications of cyclodextrin complexes in pharmaceutical and other fields are also explained here with examples. Thus cyclodextrins, because of their continuing ability to find several novel applications in drug delivery, are expected to solve many problems accompanied with the delivery of different novel drugs through various delivery routes.

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“…[46][47][48] Cyclodextrin has been proven as a drug absorption enhancer as well. 49,50 Since daidzein is a typical poor hydrophilic and poor lipophilic drug with very low oral bioavailability, …”

Section: Dovepressmentioning

confidence: 99%

The comparison of different daidzein-PLGA nanoparticles in increasing its oral bioavailability

Ma¹,

Zhao²,

Li³

et al. 2012

IJN

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Abstract:The aim of this research was to increase the oral bioavailability of daidzein by the formulations of poly(lactic-co-glycolic) acid (PLGA) nanoparticles loaded with daidzein. Amongst the various traditional and novel techniques of preparing daidzein-loaded PLGA nanoparticles, daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles were selected. The average drug entrapment efficiency, particle size, and zeta potential of daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles were 81.9% ± 5%, 309.2 ± 14.0 nm, −32.14 ± 2.53 mV and 83.2% ± 7.2%, 323.2 ± 4.8 nm, −18.73 ± 1.68 mV, respectively. The morphological characterization of nanoparticles was observed with scanning electron microscopy by stereological method and the physicochemical state of nanoparticles was valued by differential scanning calorimetry. The in vitro drug-release profile of both nanoparticle formulations fitted the Weibull dynamic equation. Pharmacokinetic studies demonstrated that after oral administration of daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles to rats at a dose of 10 mg/kg, relative bioavailability was enhanced about 5.57-and 8.85-fold, respectively, compared to daidzein suspension as control. These results describe an effective strategy for oral delivery of daidzein-loaded PLGA nanoparticles and might provide a fresh approach to enhancing the bioavailability of drugs with poor lipophilic and poor hydrophilic properties.

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Evaluation of carboxymethyl-β-cyclodextrin with acid function: Improvement of chemical stability, oral bioavailability and bitter taste of famotidine

Cited by 50 publications

References 31 publications

Fabrication, Characterization, and In Vivo Evaluation of Famotidine Loaded Solid Lipid Nanoparticles for Boosting Oral Bioavailability

Fabrication, Characterization, and In Vivo Evaluation of Famotidine Loaded Solid Lipid Nanoparticles for Boosting Oral Bioavailability

Untitled

The comparison of different daidzein-PLGA nanoparticles in increasing its oral bioavailability

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