Preparation and characterization of vinpocetine loaded nanostructured lipid carriers (NLC) for improved oral bioavailability

Zhuang, Chun-Yang; Li, Ning; Wang, Mi; Zhang, Xiaoning; Pan, Weisan; Peng, Junjie; Pan, Yusheng; Tang, Xin

doi:10.1016/j.ijpharm.2010.05.005

Cited by 281 publications

(132 citation statements)

References 26 publications

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“…It would be more difficult for a drug to be released in the form of an ionic complex encapsulated in nanoparticles; therefore, the long-circulating effect was enhanced. Second, NLC are stealthy due to their special material and surface properties [12,46] , so they can escape from the phagocytosis of the reticuloendothelial system. Furthermore, the tight structure of the NLC, which is composed of both solid and liquid lipids, can protect a drug from enzyme degradation before release.…”

Section: Discussionmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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Aim: Breviscapine isolated from the Chinese herb Erigeron breviscapus (Vant) Hand-Mazz is widely used to treat cardiovascular and cerebrovascular diseases. The aim of this study was to improve the pharmacokinetic profiles of breviscapine using nanostructured lipid carrier based on an ionic complex formation. Methods: Breviscapine nanostructured lipid carrier (Bre-NLC) was prepared using the thin film homogenization method. The morphology of Bre-NLCs was determined using transmission electron microscopy. The mean particle size, polydispersity index, zeta-potential analysis and entrapment efficiency were analized. In vitro release was studied using the dialysis method. In vitro stability was studied in fresh plasma and liver slurry of rats. In vivo pharmacokinetics was analyzed in rats after intravenous injection of a dose equivalent to breviscapine (10 mg/kg). Results: The Bre-NLCs were spherical with a mean particle size of ~170 nm, a zeta potential of ~20 mV and a high entrapment efficiency of ~89%. Compared with a commercially available solution, a substantial decrease in the cumulative release of breviscapine was found for the Bre-NLCs. The NLC has a significantly protective effect against the liver enzyme degradation of breviscapine. After intravenous administration in rats, the Bre-NLCs exhibited a 32 times increase in the AUC 0-t and a 12 times increase in T 1/2 as compared to the commercially available breviscapine solution. Conclusion:The results demonstrate that the NLC has great potential to use as a novel sustained release system for breviscapine.

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Section: Discussionmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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“…Lipid nanoparticles with solid particle matrix are derived from o/w emulsions by simply replacing liquid lipid (oil) by a solid lipid. Carvedilol nanostructured lipid carriers (CAR-NLCs) have a solid matrix blended with a liquid lipid (oil) to form an unstructured matrix that improved the drug loading and reduced drug expulsion from the matrix during storage (Zhuang et al, 2010;Beloqui et al, 2013). Due to the differences in the structures of the solid and liquid lipids, formation of a perfect crystal is distorted.…”

Section: Introductionmentioning

confidence: 99%

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

et al. 2016

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The purpose of this study was to develop Carvedilol nanostructured lipid carriers (CAR-NLCs) using stearic acid and oleic acid as lipid, and to estimate the potential as oral delivery system for poorly water soluble drug. The particle-size analysis revealed that all the developed formulations were within the nanometer range. The EE and loading were found to be between 69.45-88.56% and 9.58-12.56%, respectively. The CAR-NLCopt showed spherical morphology with smooth surface under transmission electron microscope (TEM). The crystallization of the drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC) and revealed that the drug was in an amorphous state in the NLC matrix. The ex vivo gut permeation study showed many folds increment in the permeation of CAR-NLCs compared to Carvedilol suspension (CAR-S). The oral bioavailability study of CAR was carried out using Wistar rats and relative bioavailability of CAR-NLCopt was found to be 3.95 fold increased in comparison with CAR-S. In vivo antihypertensive study in Wistar rats showed significant reduction in mean systolic BP by CAR-NLCopt vis-à-vis CAR-S (p50.05) owing to the drug absorption through lymphatic pathways. In conclusion, the NLC formulation remarkably improved the oral bioavailability of CAR and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs. The promising findings in this investigation suggest the practicability of these systems for the enhancement of bioavailability of CAR.

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“…The surfactant and cosurfactant were selected based on their efficacy in formulating MEs for intravenous products as determined by our previous extensive research in related fields. [24][25][26] In our preliminary test, the best solubilization, microemulsifying effect, and resistance to infinite dilution were found for the MCT/S75/HS 15/PEG 400 combinations. The appropriate components and their ratio of surfactant phase (S75, HS 15), oil phase, and aqueous phase (5% PEG 400 aqueous solution) were determined by aqueous phase titration.…”

Section: Preparation Of Mesmentioning

confidence: 79%

Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics

Shi-lin¹,

Chen²,

Ye³

et al. 2013

IJN

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Preparation and characterization of vinpocetine loaded nanostructured lipid carriers (NLC) for improved oral bioavailability

Cited by 281 publications

References 26 publications

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics

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