The effect of physical barriers and properties on the oral absorption of particulates

Norris, Daniel A.

doi:10.1016/s0169-409x(98)00037-4

Cited by 229 publications

(122 citation statements)

References 96 publications

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“…Our earlier work with sodium borohydride reduced gold nanoparticles demonstrated that nasal administration of the same at 20 IU/Kg resulted in 50% reduction of BGL at the end of 3 h (11). The higher reduction in BGL following nasal administration of gold nanoparticles as compared to oral is attributed due to the differences in the anatomy and physiological particularities as depicted in Table I ( [40][41][42][43][44][45]. The serum insulin levels determined at the end of the 2 h were consistently higher for chitosan reduced gold nanoparticles as compared to insulin solution when administered by oral and nasal routes (Fig.…”

Section: Resultsmentioning

confidence: 93%

Chitosan Reduced Gold Nanoparticles as Novel Carriers for Transmucosal Delivery of Insulin

et al. 2007

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Purpose. Colloidal metallic systems have been recently investigated in the area of nanomedicine. Gold nanoparticles have found themselves useful for diagnostic and drug delivery applications. Herein we have reported a novel method for synthesis of gold nanoparticles using a natural, biocompatible and biodegradable polymer; chitosan. Use of chitosan serves dual purpose by acting as a reducing agent in the synthesis of gold nanoparticles and also promotes the penetration and uptake of peptide hormone insulin across the mucosa. To demonstrate the use of chitosan reduced gold nanoparticles as carriers for drug delivery, we report herein the transmucosal delivery of insulin loaded gold nanoparticles. Materials and Methods. Gold nanoparticles were prepared using different concentrations of chitosan (from 0.01% w/v up to 1% w/v). The gold nanoparticles were characterized for surface plasmon band, zeta potential, surface morphology, in vitro diffusion studies and fluorescence spectroscopy. The in vivo studies in diabetic male Wistar rats were carried out using insulin loaded chitosan reduced gold nanoparticles.Results. Varying concentrations of chitosan used for the synthesis of gold nanoparticles demonstrated that the nanoparticles obtained at higher chitosan concentrations (>0.1% w/v) were stable showing no signs of aggregation. The nanoparticles also showed long term stability in terms of aggregation for about 6 months. Insulin loading of 53% was obtained and found to be stable after loading. Blood glucose lowering at the end of 2 h following administration of insulin loaded gold nanoparticles to diabetic rats was found to be 30.41 and 20.27% for oral (50 IU/kg) and nasal (10 IU/kg), respectively. Serum gold level studies have demonstrated significant improvement in the uptake of chitosan reduced gold nanoparticles. Conclusions. The synthesis of gold nanoparticles using a biocompatible polymer, chitosan would improve its surface properties for binding of biomolecules. Our studies indicate that oral and nasal administration of insulin loaded chitosan reduced gold nanoparticles has led to improved pharmacodynamic activity. Thus, chitosan reduced gold nanoparticles loaded with insulin prove to be promising in controlling the postprandial hyperglycemia.

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Section: Resultsmentioning

confidence: 93%

Chitosan Reduced Gold Nanoparticles as Novel Carriers for Transmucosal Delivery of Insulin

et al. 2007

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“…Ethionamide-loaded nanoparticles may improve gastrointestinal (GI) intolerance due to its release from nanoparticles in blood and reticuloendothelial system (RES), and very less release in intestine. The nanoparticulate formulations have been known to increase the oral bioavailability of drugs due to their specialized uptake mechanisms and because they bypass hepatic first-pass metabolism (Desai et al, 1996;Florence, 1997;2005;Norris et al, 1998). Furthermore, ethionamide-loaded nanoparticles may improve the drug efficacy by keeping the drug concentration above minimum inhibitory concentration (MIC) for a longer period of time and enhance the bactericidal effect of drug.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and tissue distribution studies of orally administered nanoparticles encapsulated ethionamide used as potential drug delivery system in management of multi-drug resistant tuberculosis

et al. 2010

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“…Thirdly, the cellular lining of the gastrointestinal tract is composed of absorptive enterocytes interspersed with membranous epithelial (M) cells. M cells that cover lymphoid aggregates, such as Peyar's patches, take up microparticles by a combination of endocytosis or transcytosis (Norris et al 1998;Andrianov and Payne 1998). Fourth, the permeability of gut wall was enhanced by lipids present in the SLNs and thus increased the drug absorption (Constantinides and Wasan 2007).…”

Section: Discussionmentioning

confidence: 99%

Formulation of enrofloxacin SLNs and its pharmacokinetics in emu (Dromaius novaehollandiae) birds

Kumar¹,

Arivuchelvan²,

Jagadeeswaran³

et al. 2014

Appl Nanosci

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The study was conducted to formulate the enrofloxacin solid lipid nanoparticles (SLNs) with sustained release profile and improved pharmacological activity and evaluate the pharmacokinetic behaviour of enrofloxacin SLNs after oral routes of administration in emus. The SLNs were prepared using tripalmitin as lipid carrier, Tween 80 and Span 80 as surfactants and polyvinyl alcohol (PVA) as a stabilizer by a hot homogenization coupled with ultrasonication method. The prepared enrofloxacin SLNs formulations were characterized for further investigation in emu birds. The pharmacokinetics of native enrofloxacin was studied after i.v. and oral bolus administration at 10 mg/kg in emu birds and compared with the disposition kinetics of enrofloxacin SLNs. Enrofloxacin and its metabolite ciprofloxacin in plasma were estimated using HPLC and the pharmacokinetic parameters were calculated by a noncompartmental analysis. The results demonstrated that the particle size, polydispersity index, zeta potential, encapsulation efficiency and loading capacity of the SLNs were 154.72 ± 6.11 nm, 0.42 ± 0.11, -28.83 ± 0.60 mV, 59.66 ± 3.22 and 6.13 ± 0.32 %, respectively. AFM and TEM images showed spherical to circular particles with well-defined periphery. In vitro drug release exhibited biphasic pattern with an initial burst release of 18 % within 2 h followed by sustained release over 96 h. Pharmacokinetic results showed that the t 1/2b , AUC 0-? , V darea /F, MRT and bioavailability were 3.107, 1.894, 1.594, 2.993 and 1.895 times enhanced (p \ 0.01), while CL B and b were significantly (p \ 0.01) decreased by 1.958 and 3.056 times compared to the values of native enrofloxacin administered orally. The ratio of AUC 0-t cipro/AUC 0-t enro after administration of native enrofloxacin and enrofloxacin SLNs was less than 10 %. The t 1/2b and MRT of the metabolite were longer than those of the parent substance. The PK/PD results confirmed that the SLNs extended the enrofloxacin concentration upto 48 h against pathogens susceptible to 0.125 lg/mL in emus. The results indicated that SLNs might be a promising delivery system to prolong and enhance the pharmacological activity of enrofloxacin.

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The effect of physical barriers and properties on the oral absorption of particulates

Cited by 229 publications

References 96 publications

Chitosan Reduced Gold Nanoparticles as Novel Carriers for Transmucosal Delivery of Insulin

Chitosan Reduced Gold Nanoparticles as Novel Carriers for Transmucosal Delivery of Insulin

Pharmacokinetics and tissue distribution studies of orally administered nanoparticles encapsulated ethionamide used as potential drug delivery system in management of multi-drug resistant tuberculosis

Formulation of enrofloxacin SLNs and its pharmacokinetics in emu (Dromaius novaehollandiae) birds

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