A novel approach for the development and optimization of self emulsifying drug delivery system using HLB and response surface methodology: Application to fenofibrate encapsulation

Bahloul, Badr; Lassoued, Mohamed Ali; Sfar, Souad

doi:10.1016/j.ijpharm.2014.03.040

Cited by 49 publications

(32 citation statements)

References 29 publications

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“…But, formulation development by the two methods is subjected to a large number of experiments. Recently a HLB coupled to response surface methodology (RSM) approach is developed by Bahloul et al (2014), which may reduce the number of trials to develop and optimize the SEDDS with desired drug release and satisfactory pharmacokinetic parameters (Bahloul et al, 2014(Bahloul et al, , 2015.…”

Section: Introductionmentioning

confidence: 99%

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

et al. 2016

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Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug. In this review, potential issues or questions on SEDDS are identified and summarized from the pharmacokinetic point of view. Primarily this review includes the conflict between the influences of droplet size, variation in correlation between in vitro lipolysis or ex-vivo intestinal permeation and pharmacokinetic parameters, variation in in vivo results of solid and liquid SEDDS, and potential challenges or limitation of pharmacokinetic studies on human volunteers with orally administered SEDDS. In the past decades, hundreds of in vivo studies on SEDDS have been published. In the present study, only the relevant article on in vivo pharmacokinetic studies with orally administered SEDDS published in past 5-6 years are analyzed for an up to date compilation. KeywordsPoor bioavailability, self-nanoemulsifying delivery system, self-microemulsifying delivery system, in vitro lipolysis, pharmacokinetic of SEDDS History

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Section: Introductionmentioning

confidence: 99%

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

et al. 2016

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“…Indeed, we can maintain sink conditions in octanol phase with a low volume of organic solvent. Finally, fenofibrate is soluble in supercritical CO 2 (Chen et al, 2010) and this API is often used in the literature as a model molecule for all processes involving the use of supercritical CO 2 (Dalvi et al, 2013;Hiendrawan et al, 2014;Sanganwar and Gupta, 2008) and for processes that attempt to increase the aqueous solubility of a compound by self-emulsification in a lipid-based formulation (Bahloul et al, 2014;Devraj et al, 2013;Griffin et al, 2014;Mu et al, 2013) or by any other techniques (Dong et al, 2014;Kalivoda et al, 2012;Niu et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

“…This concept is very useful because it reduces the number of required experiments and makes the search process fast and effective. The use of the statistical methods involved in DoE is now well established in the pharmaceutical industry and it is recommended that it be applied to the development of any process (Bahloul et al, 2014;Brion et al, 2009). In the present study, a screening design was firstly performed in order to identify the critical factors affecting the DoE response.…”

Section: Introductionmentioning

confidence: 99%

Optimization of a PGSS (particles from gas saturated solutions) process for a fenofibrate lipid-based solid dispersion formulation

Pestieau

Krier

Lebrun³

et al. 2015

International Journal of Pharmaceutics

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“…Experiments were run in random order to increase the predictability of the model. Optimisation was performed using a desirability function to obtain the levels of X1, X2 and X3, which minimised (Y1) and (Y3) and maximised (Y2) [16][17][18][19][20][21]. The quadratic model generated by design is as follows:…”

Section: Experimental Designmentioning

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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A novel approach for the development and optimization of self emulsifying drug delivery system using HLB and response surface methodology: Application to fenofibrate encapsulation

Cited by 49 publications

References 29 publications

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

Optimization of a PGSS (particles from gas saturated solutions) process for a fenofibrate lipid-based solid dispersion formulation

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

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