Disposition Kinetics and Oral Bioavailability of Vincamine-Loaded Polyalkyl Cyanoacrylate Nanoparticles

Maincent, Philippe; Verge, Roger Le; Sado, P. A.; Couvreur, P.; Devissaguet, Jean‐Philippe

doi:10.1002/jps.2600751009

Cited by 115 publications

(27 citation statements)

References 11 publications

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“…8 Maincent et al were the first to demonstrate that nanoparticles could improve the oral bioavailability of drugs in 1984. 9,10 After oral administration, the nanoparticles could control the release of drugs, reduce gastrointestinal mucosal irritation, and ensure their stability in the gastrointestinal tract. 11 Lecithin nanoparticles (LNs) were reported to be able to increase antitumor effects of docetaxel after intravenous injection with good biocompatibility.…”

Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Cao²,

Hu³

et al. 2012

IJN

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Abstract:The aim of this research work was to investigate the potential of lecithin nanoparticles (LNs) in improving the oral bioavailability of docetaxel. Docetaxel-loaded LNs (DTXLNs) were prepared from oil-in-water emulsions and characterized in terms of morphology, size, zeta potential, and encapsulation efficiency. The in vitro release of docetaxel from the nanoparticles was studied by using dialysis bag method. Caco-2 cell monolayer was used for the in vitro permeation study of DTX-LNs. Bioavailability studies were conducted in rats and different pharmacokinetic parameters were evaluated after oral administration of DTX-LNs. The results showed that DTX-LNs had a mean diameter of 360 ± 8 nm and exhibited spherical shape with smooth surface under transmission electron microscopy. The DTX-LNs showed a sustained-release profile, with about 80% of docetaxel released within 72 hours. The apical to basolateral transport of docetaxel across the Caco-2 cell monolayer from the DTX-LNs was 2.14 times compared to that of the docetaxel solution (0.15 × 10 −5 ± 0.016 × 10 −5 cm/second versus 0.07 × 10 −5 ± 0.003 × 10 −5 cm/second). The oral bioavailability of the DTX-LNs was 3.65 times that of docetaxel solution (8.75% versus 2.40%). These results indicate that DTX-LNs were valuable as an oral drug delivery system to enhance the absorption of docetaxel.

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Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Cao²,

Hu³

et al. 2012

IJN

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“…The pharmacokinetic studies showed that the PK of CEF encapsulated in liposomes made with BS was superior to the aqueous solution of CEF and conventional liposomes resulting in a higher AUC0-, Cmax, Tmax, t½ and F. Although at this stage the ultimate fate and the mechanisms of absorption of liposomes with NaDC after oral administration have not been completely determined yet, the enhancement must be the result of a combination of positive effects before, on and through the intestinal epithelial membrane. Starting with better protection against hydrolytic degradation in the GIT environment, the prolonged life time increased the number of vesicles arriving in the intestine (54). Earlier results in literature showed that increased oral bioavailability was supported by the accumulation of vesicles at the brushboarder membrane of enterocytes followed by an improved drug transport through the intestinal membrane facilitating the absorption into the systemic circulation (54).…”

Section: Discussionmentioning

confidence: 99%

“…Starting with better protection against hydrolytic degradation in the GIT environment, the prolonged life time increased the number of vesicles arriving in the intestine (54). Earlier results in literature showed that increased oral bioavailability was supported by the accumulation of vesicles at the brushboarder membrane of enterocytes followed by an improved drug transport through the intestinal membrane facilitating the absorption into the systemic circulation (54). Drug formulations can be absorbed by biomembranes through multiple passive or active pathways using paracellular or transcellular transport.…”

Section: Discussionmentioning

confidence: 99%

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

et al. 2017

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-PURPOSE: Liposomes have been studied as a colloidal carrier in drug delivery systems, especially for oral administration. However, their low structural integrity in the gut is still a major shortcoming. Membrane disruptive effects of physiological bile salts in the small intestine result in premature drug release prior to intestinal absorption. Thus, we analyzed the stabilizing effect of sodium deoxycholate when incorporated into nano-sized liposomes. METHOD: Cefotaxime-loaded liposomes were prepared with different sodium deoxycholate concentrations (3.75-30 mM) by rotary film evaporation followed by nanosize reduction. The physical integrity of liposomes was evaluated by monitoring cefotaxime leakage, particle sizes in different simulated physiological media. The oral bioavailability and pharmacokinetics of cefotaxime was assessed in rats (n = 6 per group) after single dose of drug-encapsulated in liposomes containing bile salt, drug in conventional liposomes, and cefotaxime solution (oral and intravenous). RESULTS: Simulated gastric fluid with low pH showed less effect on the stability of liposomes in comparison to media containing physiological bile salts. Liposomes containing 15 mM sodium deoxycholate were most stable in size and retained the majority of encapsulated cefotaxime even in fed state of simulated intestinal fluid being the most destructive media. Pharmacokinetics data showed an increase in Cmax and AUC0-inf in the following order: cefotaxime solution < conventional liposomes < liposomes made with bile salts. The total oral bioavailability of cefotaxime in liposomes containing bile salt was found to be 5-times higher compared to cefotaxime solution and twice as much as in conventional liposomes. CONCLUSION: Incorporation of bile salts, initially used as membrane permeation enhancer, also acted as a stabilizer against physiological bile salts. The nanosized liposomes containing sodium deoxycholate were able to reduce the leakage of encapsulated cefotaxime in the gut due to the improved vesicle stability and to enhance the oral bioavailability of acid-labile drugs up to 5-fold.

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“…There is a number of mechanisms explaining the bioavailability enhancement of drugs when they are encapsulated into vesicles and/or in nano-particles system following oral administration. One of the mechanism could be due to accumulation of its nanoparicles at brush-boarder membrane of enterocytes and subsequently the gradient of drug concentration was increased across the intestinal epithelium which facilitates the absorption of a significant amount of drug into the systemic circulation (25,26). In addition, another potential mechanisms may explain the absorption of particulate at intestine following the oral administration (27,28).…”

Section: Discussionmentioning

confidence: 99%

Cefotaxime pharmacokinetics after oral application in the form of 3α,7α-dihydroxy-12-keto-5β-cholanate microvesicles in rat

Goločorbin-Kon

Mikov

Arafat

et al. 2009

Eur. J. Drug Metabol. Pharmacokinet.

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The aim of ths study was to investigate the pharmacokinetics of cefotaxime sodium (CEF) pharmacokinetics after oral application in the form of sodium 3alpha,7alpha-dihydroxy-12-keto-5beta-cholanate (MKC) microvesicles (MV) in rat. Thirty Male Wister rats were divided into six groups (n=5 per group). Groups were treated orally with: (i) CEF (15 mg/kg) saline solution (15 mg/kg); (ii) CEF (15 mg/kg) saline solution with MKC (2 mg/kg); (iii) CEF saline solution mixed with blank microvesicles; (iv) CEF (15 mg/kg) encapsulated in microvesicles with saline solution; (v) CEF saline solution (15 mg/kg) mixed with blank MKC microvesicules; (vi) CEF (15 mg/kg) encapsulated in MKC microvesicules with saline solution. Data were analyzed using noncompartmental model. CEF oral bioavailability was increased twofold when coadministered with MKC and when encapsulated in microvesicles and ninefold when encapsulated in MKC microvesicles compared to the same CEF dose administered orally as saline solution. The increased bioavailability of CEF resulting from CEF encapsulation in microvesicules with MKC suggests that this formulation can extend the application of CEF from parenteral only to oral application.

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Disposition Kinetics and Oral Bioavailability of Vincamine-Loaded Polyalkyl Cyanoacrylate Nanoparticles

Cited by 115 publications

References 11 publications

Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

Cefotaxime pharmacokinetics after oral application in the form of 3α,7α-dihydroxy-12-keto-5β-cholanate microvesicles in rat

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