Enhancing intestinal drug solubilisation using lipid-based delivery systems

Porter, Christopher John; Pouton, Colin W.; Cuiné, Jean; Charman, William N.

doi:10.1016/j.addr.2007.10.014

Cited by 619 publications

(357 citation statements)

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“…Self nanoemulsifying drug delivery systems (SNEDDS) are isotropic mixtures of drug, lipids and surfactants, usually with one or more hydrophilic co-solvents or co-emulsifiers that form fine oil in water nanoemulsions upon mild agitation in an aqueous medium with a droplet sizes ranging 20-200 nm (Mou et al, 2008;Porter et al, 2008). In the gastrointestinal tract environment (fluids 100 and motility) this systems spontaneously emulsify (Nazzal et al, 2002;Devani et al, 2004;Patel et al, 2007).…”

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confidence: 99%

Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil

Villar

Naveros

Campmany

et al. 2012

International Journal of Pharmaceutics

140

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Self nanoemulsifying drug delivery systems of gemfibrozil were developed under Quality by Design approach for improvement of dissolution and oral absorption. Preliminary screening was performed to select proper components combination. Box-Behnken experimental design was employed as statistical tool to optimize the formulation variables, X1 (Cremophor® EL), X2 (Capmul® MCM -C8), and X3 (lemon essential oil). Systems were assessed for visual characteristics (emulsification efficacy), turbidity, droplet size, polydispersity index and drug release. Different pH media were also assayed for optimization. Following optimization, the values of formulation components (X1, X2, and X3) were 32. 43%, 29.73% and 21.62 %, respectively (16.22% of gemfibrozil). Transmission electron microscopy demonstrated spherical droplet morphology. SNEEDS release study was compared to commercial tablets. Optimized SNEDDS formulation of gemfibrozil showed a significant increase in dissolution rate compared to conventional tablets. Both formulations followed Weibull mathematical model release with a significant difference in td parameter in favour of the SNEDDS. Equally amodelistic parameters were calculated being the dissolution efficiency significantly higher for SNEDDS, confirming that the developed SNEDDS formulation was superior to commercial formulation with respect to in vitro dissolution profile. This paper provides an overview of the SNEDDS of the gemfibrozil as a promising alternative to improve oral absorption. She is an expert in nanotechnology (colloids and nanoparticles) with a wide experience. She has extensive curriculum of published paper about this subject Jose Luis Arias Mediano Ph. D. Professor reseracher, Pharmacy and Pharmaceutical Technology , University of Granada jlarias@ugr.es He is an expert in nanotechnology (colloids and nanoparticles) with a wide experience in this type of investigation. Also is reviewer in specialized pharmaceutical journal. He is an expert in nanotechnology (colloids and nanoparticles) with a wide experience in this type of investigation. Also is reviewer of Pharmaceutical science journals. IJP AUTHOR CHECKLISTDear Author, It frequently happens that on receipt of an article for publication, we find that certain elements of the manuscript, or related information, is missing. This is regrettable of course since it means there will be a delay in processing the article while we obtain the missing details.In order to avoid such delays in the publication of your article, if accepted, could you please run through the list of items below and make sure you have completed the items. Overall Manuscript Electronic artwork format? ---------------------------------------------------TIFF

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mentioning

confidence: 99%

Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil

Villar

Naveros

Campmany

et al. 2012

International Journal of Pharmaceutics

140

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“…[4] The increased concentration of bile provides an emulsifying environment rich in micelles, into which lipids, the lipid digestion products and any available drug are solubilized. [4,12,[15][16][17] In the duodenum, pancreatic lipase then hydrolyses the remaining triglycerides to monoglycerides (MAGs), DAGs, i.e., partial glycerides that have a better capacity for drug solubilization and emulsification than their triglyceride counterparts [18] and FFAs that may function as cosurfactants. [12] Since there is evidence that (mixtures of) MCTs, MAGs, and DAGs have a higher solubilization capacity than LCTs, controlled modification of SB and PKO may result in new derivatives with desirable properties for the delivery of poorly soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Enzymatically Modified Shea Butter and Palm Kernel Oil as Potential Lipid Drug Delivery Matrices

Obitte

Zorn

Oroz‐Guinea

et al. 2018

Euro J Lipid Sci & Tech

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Drug formulations based on lipids can enable a significantly better delivery of a pharmaceutically active substance and thus enhance their bioavailability. However, natural fats and oils usually have properties, which do not allow their direct use for drug delivery. Therefore, we have modified palm kernel oil (PKO) and shea butter (SB) via lipase-catalyzed transesterification using either glycerol -to create a diglyceride-enriched lipid -or using hexanoic acid via acidolysis -to alter their fatty

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“…[3] Rapid emulsification of these systems under mild agitation in vivo generates high surface area, and thereby, increases the rate and extent of absorption and results in more reproducible blood time profiles. [4] In addition, lymphatic uptake of the drugs is enhanced due to the small globule size and surface charge associated with it. [5] Therefore, particle size, drug release and zeta potential were selected as optimization criteria.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Talele¹

2017

AJP

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Aim: The objective of the present study was to design self nanoemulsifying drug delivery system of quetiapine fumarate by optimizing particle size, zeta potential, and drug release using response surface methodology. Materials and Methods: Self-nanoemulsified drug delivery system formulations were prepared using Labrafac Lipophile WL as oil, Tween 80 as a surfactant, and Capryol 90 as a cosurfactant. Pseudo-ternary phase diagrams of oil, surfactant/co surfactant, and water were developed using the water titration method. Different Smix ratios were prepared, and the maximum ratio was selected for self-nanoemulsified drug delivery system (SNEDDS) formulation. D-optimal design for 3 factors at 3 levels each was employed systematically to optimize particle size, zeta potential, and drug release. Result and Discussion: The polynomial mathematical model generated for response and found to be significant. The optimized model predicted a particle size 54.42 nm, zeta potential −13.03 mv, and drug release 93.67% residual plots for particle size, zeta potential, and % drug release indicates points nearly closed to straight lines indicating good model. The signal-to-noise ratio effect was studied which causes r 2 value closer to 0.5. Conclusion: The quantitative effect of these factors at different levels was predicted using polynomial equation. Response methodology was then used to predict the levels of the factors A, B, and C required to obtaining an optimum formulation. A new formulation was prepared according to these levels. Signalto-noise ratio was studied. Observed response was in close agreement with the predicted values of the optimized formulation, thereby demonstrating the feasibility of the optimization procedure in developing SNEDDS of quetiapine fumarate.

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Enhancing intestinal drug solubilisation using lipid-based delivery systems

Cited by 619 publications

References 151 publications

Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil

Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil

Enzymatically Modified Shea Butter and Palm Kernel Oil as Potential Lipid Drug Delivery Matrices

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