Surfactant effects on the physical characteristics of Amphotericin B-containing nanostructured lipid carriers

Tan, See Wei; Billa, Nashiru; Roberts, Clive J.; Burley, J.

doi:10.1016/j.colsurfa.2010.09.030

Cited by 95 publications

(47 citation statements)

References 22 publications

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“…The three types of SLNs (containing AmB, PAR, or SSZ) were prepared as previously described (5,17). Briefly, 50 mg of drug (AmB, PAR, or SSZ) and 120 mg of lecithin were initially dissolved in a 40-mL mixture of chloroform and methanol at a 1:1 ratio, along with 200 mg each of cocoa butter and beeswax.…”

Section: Preparation Of Slnsmentioning

confidence: 99%

“…In a previous work, we have successfully developed an AmB-containing SLN formulation, subjected the same to extensive characterization (17)(18)(19) and we have performed a pilot GI transit study of the formulation in fasted rats (5). In the present paper, we describe the pharmacokinetics of AmB as a consequence of food status and the GI transit of AmBcontaining SLNs using an indirect estimation method (20)(21)(22).…”

Section: Introductionmentioning

confidence: 99%

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Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

et al. 2015

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Abstract. Amphotericin B (AmB) is poorly absorbed from the gastrointestinal tract. Recent studies have suggested enhanced drug absorption from solid lipid nanoparticles (SLN). Little is known of the fate of AmB absorption within the gastrointestinal tract, and no gastrointestinal transit study has yet been performed on AmB-containing nano-formulations. We aimed to investigate the effect of food on the gastrointestinal transit properties of an AmB-containing SLN in rats. Three SLNs containing AmB, paracetamol, or sulfasalazine were formulated using cocoa butter and beeswax as lipid matrices and simultaneously administered orally to Sprague-Dawley rats. Paracetamol and sulfapyridine were used as marker drugs for estimating gastric emptying and cecal arrival, respectively. The pharmacokinetic data generated for paracetamol and sulfapyridine were used in estimating the absorption of the AmB SLNs in the small and large intestines, respectively. A delayed rate of AmB absorption was observed in the fed state; however, the extent of absorption was not affected by food. Specifically, the percentages of AmB absorption during the fasted state in the stomach, small intestine, and colon were not significantly different from absorption within the respective regions in the fed state. In both states, however, absorption was highest in the colon and appeared to be a combination of absorption from the small intestine plus absorption proper within the colon. The study suggests that AmB SLN, irrespective of food status, is slowly but predominantly taken up by the lymph, making the small intestine the most favorable site for the delivery of the AmB SLNs.

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Section: Preparation Of Slnsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

et al. 2015

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“…From a stability standpoint, sufficient electrical potential (4AE30 mV) must be retained by nanoparticles in order to induce static repulsion on reproach (Tan et al, 2010). Herein stearylamine, a surface charge modifier, has been utilized to assess its influence on z-potential of SLNs.…”

Section: Characterization Of Sln Dispersionmentioning

confidence: 99%

“…z-potential measurements were run at an electric field strength of 25 V/m. Results are presented as mean AE standard deviation (SD) from three replicate determinations (Shegokar et al, 2010;Tan et al, 2010;Zhang et al, 2010).…”

Section: Physico-chemical Characterization Of Sln Dispersionmentioning

confidence: 99%

Novel surface modified solid lipid nanoparticles as intranasal carriers for ropinirole hydrochloride: application of factorial design approach

et al. 2013

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Present investigation deals with intranasal delivery of ropinirole hydrochloride (ROPI HCl), loaded in solid lipid nanoparticles (SLNs). Prime objectives of this experiment are avoidance of hepatic first pass metabolism and to improve therapeutic efficacy in the treatment of Parkinson's disease. SLNs were fabricated by emulsification-solvent diffusion technique. A 3 2 -factorial design approach has been employed to assess the influence of two independent variables, namely Pluronic F-68 and stearylamine concentration on particle size, z-potential and entrapment efficiency of prepared SLNs. Prepared samples were further evaluated for in vitro drug diffusion, ex vivo drug permeation, histopathological and stability studies. Differential scanning calorimetry analysis revealed the encapsulation of amorphous form of drug into lipid matrix, while scanning electron microscopy studies indicated the spherical shape. Fabricated SLNs had shown no severe signs of damage on integrity of nasal mucosa. Release pattern of prepared drug-loaded sample was best fitted to zero-order kinetic model with non-Fickian super case II diffusion mechanism. In vivo pharmacodynamic studies were carried out to compare therapeutic efficacy of prepared nasal formulation against marketed oral formulation.Results of analysis of variance demonstrated the significance of suggested model. Threedimensional response surface plots and regression equations confirmed the corresponding influence of selected independent variables on measured responses. Our findings suggested the feasibility of investigated system for intranasal administration.

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“…AmB is currently administered intravenously due its poor aqueous solubility characteristics, which makes oral delivery challenging. In earlier studies, we have successfully formulated and exhaustively characterised an oral AmB-containing solid lipid nanoformulation with the aim of improving its oral bioavailability (Amekyeh et al, 2015;Tan et al, 2014;Tan et al, 2010).…”

mentioning

confidence: 99%

Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry

Amekyeh

Billa

Roberts

2017

International Journal of Pharmaceutics

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Oral delivery of pharmaceuticals requires that they retain their physical and chemical attributes during transit within the gastrointestinal (GI) tract, for the manifestation of desired therapeutic profiles. Solid lipid nanoparticles (SLNs) are used as carriers to improve the absorption of hydrophobic drugs. In this study, we examine the stability of amphotericin B (AmB) and 5 paracetamol (PAR) SLNs in simulated GI fluids during gastric emptying. On contact with the simulated fluids, the particles increased in size due to ingress of the dissolution media into the particles. Simulated gastric emptying revealed that the formulations had mean sizes < 350 nm and neutral surface charges, both of which are optimal for intestinal absorption of SLNs. There was ingress of the fluids into the SLNs, followed by diffusion of the dissolved drug, whose rate 10 depended on the solubility of the loaded-drug in the particular medium. Time-of-flight secondary ion mass spectrometry analyses indicated that drug loading followed the core-shell model and that the AmB SLNs have a more drug-enriched core than the PAR SLNs do. The AmB SLNs are therefore a very suitable carrier of AmB for oral delivery. The stability of the SLNs in the simulated GI media indicates their suitability for oral delivery.

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Surfactant effects on the physical characteristics of Amphotericin B-containing nanostructured lipid carriers

Cited by 95 publications

References 22 publications

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

Novel surface modified solid lipid nanoparticles as intranasal carriers for ropinirole hydrochloride: application of factorial design approach

Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry

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