Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

Singh, Bhupinder; Khurana, Lalit Kumar; Bandyopadhyay, Shantanu; Kapil, Rishi; Katare, O. P.

doi:10.3109/10717544.2011.604686

Cited by 103 publications

(49 citation statements)

References 40 publications

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“…Remarkable augmentation in the antimalarial activity of the drug can be rationally ascribed to the superior efficacy of the SNEDDS formulation, owing to significant improvement in the biopharmaceutical performance of the drug. Vital mechanistics through which SNEDDS may have helped in augmenting the oral drug absorption by circumnavigation of hepatic first-pass effect, inhibition of metabolism by gut cytochromes and of efflux by P-gp (Porter & Charman, 2001a;Porter et al, 2008;Singh et al, 2011b;Elgart et al, 2013;Singh et al, 2014;Beg et al, 2015b). Owing to enhanced oral drug absorption into the systemic circulation, more number of parasites were killed in case of the SNEDDS formulations, as is clearly evident from the percent parasitemia count in the blood smear till day ''8'' P.I.…”

Section: In Vivo Pharmacodynamic Studiesmentioning

confidence: 88%

“…Of late, the lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) have proved their worth as one of the highly promising systems for ameliorating the oral bioavailability of drugs, especially belonging to the BCS class II and IV categories (Singh et al, 2011b;Beg et al, 2015aBeg et al, , 2015b. These primarily constitute the isotropic mixtures of lipids, surfactants, cosurfactants and/or cosolvents, which upon spontaneous emulsification in presence of gastrointestinal fluid produce ultrafine oil-in-water nanoemulsion with particle size less than 100 nm (Singh et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

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Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

et al. 2016

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The current studies entail systematic development of self-nanoemulsifying drug delivery systems (SNEDDS) containing medium-chain triglycerides (MCTs) and long-chain triglycerides (LCTs) for augmenting the biopharmaceutical performance of artemether. Equilibrium solubility and pseudoternary phase diagram studies facilitated selection of Captex 355 and Ethyl oleate as MCTs and LCTs, and Cremophor RH 40 and Tween 80 as surfactants, while Transcutol HP as cosolvent for formulating the SNEDDS. Systematic optimization was performed employing the Box-Behnken design taking concentrations of lipid, surfactant and cosolvent as the critical material attributes (CMAs), while evaluating for globule size, emulsification time, dissolution efficiency and permeation as the critical quality attributes (CQAs). In situ single pass intestinal perfusion (SPIP) studies in Wistar rats substantiated significant augmentation in the absorption (5-to 6-fold) and permeation (4-to 5-fold) parameters from the optimized MCT and LCT-SNEDDS vis-à-vis the pure drug. In vivo pharmacodynamic studies in Plasmodium berghi infected laca mice exhibited superior reduction in the levels of percent parasitemia, SGOT, SGPT and bilirubin, followed by higher survival rate of the animals by optimized MCT-SNEDDS followed by LCT-SNEDDS vis-à-vis the pure drug, which was subsequently ratified through histopathological examination of liver tissues. Overall, the studies construed successful development of the optimized SNEDDS of artemether with distinctly improved biopharmaceutical and antimalarial potential.

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Section: In Vivo Pharmacodynamic Studiesmentioning

confidence: 88%

Section: Introductionmentioning

confidence: 99%

Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

et al. 2016

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“…As the addition of OLM might interfere to a certain extent with the self-emulsification process, an alteration in the optimal oil-surfactant ratio might occur [13]. Hence, ternary phase diagrams were constructed using mixtures of the oil, surfactants and co-surfactant in different ratios to determine the optimal concentration of excipients required [14].…”

Section: Construction Of Ternary Phase Diagrammentioning

confidence: 99%

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Sisinthy

Nalamolu

Sarah

2016

Int J Pharm Pharm Sci

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Objective: The objective of the present study was to design, optimise and characterise self nano emulsifying drug delivery systems (SNEDDS) for a poorly water soluble drug, olmesartan medoxomil (OLM) by Formulation by Design (FbD) approach with an aim to improve its solubility and dissolution. Methods:The SNEDDS were systematically optimised using three factor Box-Behnken Results: Following optimisation, the values of formulation variables were found to be 142.276 mg (Capryol P), 399.999 mg (Cremophor EL) and 598.871 mg (Transcutol P) which produced a globule size of 12.64 nm, percentage drug release of 93.34% and a turbidity of 0.02 FNU. TEM studies demonstrated spherical droplet morphology.design. Concentration of formulation variables, namely, the oil phaseX1 (Capryol 90), the surfactant X2 (Cremophor EL), and the co-surfactant X3 (Transcutol P), was optimized for its impact on mean globule size (Y1), percentage drug release in 20 min (Y2) and turbidity (Y3) of the formulation. Ternary phase diagrams were constructed to select the areas of nanoemulsion and the amounts of oil, surfactant and cosurfactants as critical formulation variables. The prepared SNEDDS were characterised for globule size, dissolution studies, turbidity, and transmission electron microscopy (TEM). Conclusion:Thus, the present studies reveal that the SNEDDS is a promising drug delivery system approach for the enhancement of solubility and dissolution rate of OLM.

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“…Determination of reasonable excipients is the primary obstacle of creating s-SEDDS. Therefore, these perspectives ought to speak to significant future working heading Gentamycine 5 folds [39] Halofantrine 6-8 folds [30] Acyclovire 3.5 folds [31] Phenytoin 2.3 folds [32] Carvedilol 3-4 folds [33] Simvastatin 1.5 folds [34] …”

Section: ) Zeta Potential Measurementsmentioning

confidence: 99%

Self-Emulsifying Drug Delivery System

Talegave¹

2017

WJPR

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Self-emulsifying drug delivery system are the unique mixture of oil, solvent surfactant, co-surfactant, co-solvents. These are the effective approach to solving the solubility of poorly soluble drug. From couple of years aqueous solubility is biggest issues to the formulator for formulation and development of novel drug delivery. SEDDSs are Good strategy for enhancement of oral absorption and bioavailability of BCS class 2 and class 4 drugs. For these system oral route is most convenient than other route. Requirement of this system is due to poor solubility and oral absorption of highly lipid soluble drug. Those drug which is formulated by SEDDS will have good pharmaceutical market. These system have ability to form emulsification with the solid as well as liquid dosage form .SEDDS are very quickly dispersed in the gastro-intestinal fluid and making micro or Nano-emulsion containing solubilized drug. These article covers formulation, Evaluation, future aspect and application part of self-emulsifying drug delivery system.

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Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

Cited by 103 publications

References 40 publications

Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Self-Emulsifying Drug Delivery System

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