Development and evaluation of nitrendipine loaded solid lipid nanoparticles: Influence of wax and glyceride lipids on plasma pharmacokinetics

Kumar, Venishetty Vinay; Durairaj, Chandrasekar; Sistla, Ramakrishna; Veerabrahma, Kishan; Rao, Yi; Diwan, Prakash V.

doi:10.1016/j.ijpharm.2006.11.004

Cited by 178 publications

(81 citation statements)

References 16 publications

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“…18 SLNs prepared with CP have successfully enhanced the oral bioavailability of nitrendipine via lymphatic targeting. 25 Furthermore, CPbased SLNs exhibited high physical stability compared with mono-and triglycerides. 26 Preliminary studies investigated drug solubility in different system components.…”

Section: Resultsmentioning

confidence: 99%

Fabrication, appraisal, and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles

Elnaggar¹,

El-Massik²,

Abdallah³

2011

IJN

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Although sildenafil citrate (SC) is used extensively for erectile dysfunction, oral delivery of SC encounters many obstacles. Furthermore, the physicochemical characteristics of this amphoteric drug are challenging for delivery system formulation and transdermal permeation. This article concerns the assessment of the potential of nanomedicine for improving SC delivery and transdermal permeation. SC-loaded nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) were fabricated using a modified high-shear homogenization technique. Nanoparticle optimization steps included particle size analysis, entrapment efficiency (EE) determination, freeze-drying and reconstitution, differential scanning calorimetry, in vitro release, stability study and high-performance liquid chromatography analysis. Transdermal permeation of the nanocarriers compared with SC suspension across human skin was assessed using a modified Franz diffusion cell assembly. Results revealed that SLNs and NLCs could be optimized in the nanometric range (180 and 100 nm, respectively) with excellent EE (96.7% and 97.5%, respectively). Nanoparticles have significantly enhanced in vitro release and transdermal permeation of SC compared with its suspensions. Furthermore, transdermal permeation of SC exhibited higher initial release from both SLN and NLC formulations followed by controlled release, with promising implications for faster onset and longer drug duration. Nanomedicines prepared exhibited excellent physical stability for the study period. Solid nanoparticles optimized in this study successfully improved SC characteristics, paving the way for an efficient topical Viagra ® product.

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Section: Resultsmentioning

confidence: 99%

Fabrication, appraisal, and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles

Elnaggar¹,

El-Massik²,

Abdallah³

2011

IJN

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“…Then, the plasma was separated from the blood using a cooling centrifuge (Sigma, Germany) at 4° using 15 000 rpm for 15 min. The separated plasma samples were stored at −70° until analysis [32,33] .…”

Section: Application Of Methods In Pharmacokineticsmentioning

confidence: 99%

Statistical Optimization of Extraction Process for the Quantification of Valsartan in Rabbit Plasma by a HPLC Method

Reddy¹

2017

ijps

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This article describes a high performance liquid chromatography method for determination of valsartan in rabbit plasma. The method was statistically optimized, developed and validated as per United States of Food and Drug Administration guidelines. The solvent deproteination technique was opted for the extraction of valsartan from rabbit plasma. Full factorial design was used for the optimization of an extraction method. The main effect of deproteinating agent, volume of deproteinating agent, speed of centrifugation and time of centrifugation was found to be significant at P<0.0001 on all the responses. After deproteinization, the drug was analysed on a C 18 column using 20 mM ammonium formate:acetonitrile (58:42 v/v) as the mobile phase with a flow rate of 0.9 ml/min. The standard calibration curve was constructed in the concentration range of 75 ng/ml to 4.0 µg/ml and linearity was found to be 0.9989. Losartan was used as the internal standard. The retention time of valsartan and the internal standard was found to be 11.394 and 6.343 min, respectively. No interference peak was perceived. From the accuracy results, the relative error was found between 0.99 and 13.01% and relative standard deviation was between 1.43 and 12.19%. The percent relative standard deviation of intra-day and inter-day precision was found to be less than 15%. Limit of detection and limit of quantitation were found to be 22.00 and 66.67 ng/ml, respectively. From pharmacokinetic applications, the peak plasma concentration (C max ) of valsartan oral suspension was found to be 1092.67±39.62 ng/ml at 0.67±1.24 h. The half-life and area under the curve were found to be 19.92±10.28 h and 8393.35±131.14 ng/ml, respectively. The high performance liquid chromatography method was successfully demonstrated as rapid and sensitive method which can be used as an alternative for the analysis of valsartan in plasma samples.

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“…Drug entrapment efficiencies were determined by separating free GP from the GP nanoparticles (GPNP) using a Centrisart I centrifugal ultrafiltration unit (Supleco, Bellefonte, PA) with a filter membrane (molecular weight cutoff 10 kDa) as described elsewhere, 22 and then measuring the GP in nanoparticle-containing supernatants using inductively coupled plasma-mass spectroscopy. About 1 mL of the formulation solution was put in the outside chamber and in the recovery chamber at the top.…”

Section: Encapsulation Efficiencymentioning

confidence: 99%

Enhancement of anticancer efficacy using modified lipophilic nanoparticle drug encapsulation

Wong¹,

Lee²,

Zhang³

et al. 2012

IJN

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Background: Development of anticancer drugs is challenging. Indeed, much research effort has been spent in the development of new drugs to improve clinical outcomes with minimal toxicity. We have previously reported that a formulation of lipid gold porphyrin nanoparticles reduced systemic drug toxicity when compared with free gold porphyrin. In this study, we investigated the delivery and treatment efficiency of PEG surface-modified lipid nanoparticles as a carrier platform. Methods: We encapsulated antitumor drugs into PEG-modified lipid nanoparticles and these were characterized by size, zeta potential, and encapsulation efficiency. The delivery efficiency into tumor tissue was evaluated using a biodistribution study. To evaluate antitumor efficacy, gold porphyrin or camptothecin (a DNA topoisomerase I inhibitor) were encapsulated and compared using an in vivo neuroblastoma (N2A) model. Results: We showed that drug encapsulation into PEG-modified lipid nanoparticles enhanced the preferential uptake in tumor tissue. Furthermore, higher tumor killing efficiency was observed in response to treatment with PEG-modified lipid nanoparticles encapsulating gold porphyrin or camptothecin when compared with free gold porphyrin or free camptothecin. The in vivo antitumor effect was further confirmed by study of tumor inhibition and positive apoptosis activity. Surface modification of lipophilic nanoparticles with PEG increased the efficiency of drug delivery into tumor tissue and subsequently more effective antitumor activity. Conclusion: This specific design of a chemotherapeutic agent using nanotechnology is important in the development of a safe and effective drug in cancer therapy.

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Development and evaluation of nitrendipine loaded solid lipid nanoparticles: Influence of wax and glyceride lipids on plasma pharmacokinetics

Cited by 178 publications

References 16 publications

Fabrication, appraisal, and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles

Fabrication, appraisal, and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles

Statistical Optimization of Extraction Process for the Quantification of Valsartan in Rabbit Plasma by a HPLC Method

Enhancement of anticancer efficacy using modified lipophilic nanoparticle drug encapsulation

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