Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS)

Balakrishnan, Pachamuthu; Lee, Beom‐Jin; Oh, Dong Hoon; Kim, Jong Oh; Hong, Myung Ja; Jee, Jun‐Pil; Kim, Jung Ae; Yoo, Bong Kyu; Woo, Jong Soo; Yong, Chul Soon; Choi, Han‐Gon

doi:10.1016/j.ejpb.2009.03.001

Cited by 296 publications

(144 citation statements)

References 19 publications

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“…The solid-state is commonly characterized using differential scanning calorimetry (DSC) (Balakrishnan et al, 2009;Craig, 2006;Kang et al, 2012) or XRay powder diffraction (XRPD) (Docoslis et al, 2007;Hu et al, 2012;Wei et al, 2012) or vibrational spectroscopy (Milović et al, 2012;Nazzal et al, 2002;Stillhart and Kuentz, 2012). However these techniques are costly and require a highly trained user (for XRPD) and are destructive (for DSC).…”

Section: Introductionmentioning

confidence: 99%

“…Microscopic analysis with scanning or transmission electronic microscopes (SEM or TEM) may also be used (Balakrishnan et al, 2009;Yi et al, 2008aYi et al, , 2008bZhang et al, 2012). But once again it is costly, require highly trained users and it can only be used to see very small surfaces making representativity of the sampling a very big issue.…”

Section: Introductionmentioning

confidence: 99%

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Thorough characterization of a Self-Emulsifying Drug Delivery System with Raman hyperspectral imaging: A case study

Sacré

Netchacovitch

Bleye

et al. 2015

International Journal of Pharmaceutics

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Newly developed drugs often have poor bioavailability due to their poor water solubility (BCS class 2 drugs). It is therefore necessary to develop new strategies to enhance their solubility and their activity, among which, Self-Emulsifying Drug Delivery System (SEDDS).The efficacy of the drugs contained in these preparations is mainly affected by the solid state and the particle size of the active pharmaceutical ingredient (API).However, it is quite complex, long and expensive to characterize these parameters with classical techniques such as X-Ray powder diffraction, differential scanning calorimetry or hot stage microscopy.The present article presents, through a case study, the advantages of the Raman hyperspectral imaging in the characterization of such formulations. Indeed, Raman chemical imaging may fully characterize SEDDS with single equipment and operator in a non-destructive way allowing the follow-up of the formulation during stability studies. Raman imaging is therefore a tool of choice in the PAT framework since it increases the knowledge of the formulation and the process. 2A quantitative multivariate method using Raman hyperspectral imaging to assay the API in the lipid based formulation has been developed and fully validated following the "total error" approach.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Thorough characterization of a Self-Emulsifying Drug Delivery System with Raman hyperspectral imaging: A case study

Sacré

Netchacovitch

Bleye

et al. 2015

International Journal of Pharmaceutics

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“…Several potential advantages of SNEDDS include capability of bypassing hepatic portal route and promoting the lymphatic transport of lipophilic drugs, reducing metabolism by cytochrome-P450 family of enzymes present in the gut enterocytes Balakrishnan et al, 2009;Date et al, 2010) and overcome enterohepatic recirculation (Elsheikh et al, 2012). This hypothesis was believed to be attained chiefly, by lymphatic transport via Peyer's patches along the GI tract (Balakumara et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

Trans-resveratrol self-nano-emulsifying drug delivery system (SNEDDS) with enhanced bioavailability potential: optimization, pharmacokinetics andin situsingle pass intestinal perfusion (SPIP) studies

Singh

Pai

2014

Drug Delivery

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Trans-resveratrol (t-RVT) is a potent antioxidant. By virtue of extensive pre-systemic metabolism and existence of enterohepatic recirculation, t-RVT bioavailability is almost zero. The current study aimed to develop self-nanoemulsifying drug delivery systems (SNEDDS) using long-chain triglycerides (LCTs) of t-RVT in an attempt to circumvent such obstacles. Equilibrium solubility studies indicated the choice of Lauroglycol FCC as lipid, and of Labrasol and Transcutol P as surfactants, for formulating the SNEDDS. Ternary phase diagrams were constructed to select the areas of nanoemulsions, and the amounts of lipid (X 1 ) and surfactant (X 2 ) as the critical factor variables. The SNEDDS were optimized using 3 2 central composite design (CCD) and the optimized formulation (OPT) located using overlay plot. The nanometer size range and high negative values of zeta potential depicted non-coalescent nature of the SNEDDS. Optimized formulation indicated marked improvement in drug release profile vis-à-vis pure drug. Cloud point determination and accelerated stability studies ascertained the stability of OPT. Augmentation in the values of K a (3.29-fold) and AUC (4.31-fold) indicated significant enhancement in the rate and extent of bioavailability by the OPT compared with pure drug. In situ perfusion (SPIP) studies in Wistar rats construed remarkable enhancement in the absorptivity and permeability parameters of SNEDDS vis-à-vis the pure drug. Successful establishment of level A of in vitro/in vivo correlation substantiated the judicious choice of the in vitro dissolution milieu for simulating the in vivo conditions. The present study, therefore, reports the successful development of SNEDDS with distinctly enhanced bioavailability of t-RVT. KeywordsBioavailability, central composite design, in situ single pass intestinal perfusion, pharmacokinetic study, self-nanoemulsifying drug-delivery system History

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“…Nowadays, several approaches are available to improve the bioavailability of dutasteride, such as solid dispersion , polymeric nanoparticle , Hydroxypropyl-β-cyclodextrin (HP-β-CD) nanostructures , and self-emulsifying drug delivery system (SEDDS). SEDDS is a promising method as it is anhydrous isotropic mixture of oil, surfactant, co-surfactant, and drug, which spontaneously form oil-in-water emulsion following the dilution in aqueous medium upon agitation (Abdalla et al, 2008;Balakrishnan et al, 2009;Gursoy and Benita., 2004). Lee et al, (2015), designed supersaturable Self -microemulsifying drug delivery system (S-SMEDDS) of dutasteride for oral administration.…”

Section: Introductionmentioning

confidence: 99%

Self-Nanoemulsifying Drug Delivery Systems of Poorly Soluble Drug Dutasteride: Formulation and In-Vitro characterization

2017

J App Pharma Sci

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The present study aims to prepare and evaluate the self-nanoemulsifying drug delivery system (SNEDDS) to enhance the dissolution rate of a poorly soluble drug dutasteride. The formulation was prepared using capryol PGMC, Cremophor EL, and polyethylene glycol (PEG) 400 as oil, surfactant and co-surfactant, respectively. The pseudo-ternary phase diagrams with presence and absence of drug were plotted to find out the nanoemulsification range and also to evaluate the effect of dutasteride on the emulsification behavior of the phases. Prepared SNEDDS formulations were evaluated for its particle size distribution, nanoemulsifying properties, robustness to dilution, self-emulsification time, turbidity measurement, drug content and in-vitro dissolution. Furthermore, the optimized formulations were evaluated for heating cooling cycle, centrifugation studies, freeze thaw cycling, particle size distribution and zeta potential to confirm the stability of the formed SNEDDS formulations. The particle size, zeta potential and polydispersity index of the optimized formulation was found to be 35.45 nm, -15.45 and 0.19, respectively. The in vitro results revealed that the prepared formulation enhanced the dissolution rate of dutasteride significantly compared to pure drug. In 60 minutes, the formulation showed 83.15% and 82.04 % drug release for pH 6.8 and pH 1.2 respectively. Based on the results, it was concluded that the dutasteride-loaded SNEDDS revealed better dissolution compared to the raw drug suspension and commercial drug.

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Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS)

Cited by 296 publications

References 19 publications

Thorough characterization of a Self-Emulsifying Drug Delivery System with Raman hyperspectral imaging: A case study

Thorough characterization of a Self-Emulsifying Drug Delivery System with Raman hyperspectral imaging: A case study

Trans-resveratrol self-nano-emulsifying drug delivery system (SNEDDS) with enhanced bioavailability potential: optimization, pharmacokinetics andin situsingle pass intestinal perfusion (SPIP) studies

Self-Nanoemulsifying Drug Delivery Systems of Poorly Soluble Drug Dutasteride: Formulation and In-Vitro characterization

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