Self-nano-emulsifying drug delivery systems: an update of the biopharmaceutical aspects

Cherniakov, Irina; Domb, Abraham J.

doi:10.1517/17425247.2015.999038

Cited by 133 publications

(78 citation statements)

References 92 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…By this way drugs delivered by SEDDS may bypass first pass metabolism. All these abovementioned mechanisms are well-depicted in the review published by Cherniakov et al (2015).…”

Section: Lipidsmentioning

confidence: 82%

“…However, outcomes of these pharmacokinetic studies have been rarely summarized and addressed in recent times. In a nice scientific description, Cherniakov et al (2015) discussed the biopharmaceutical points of SEDDS after its oral administration. The review was primarily focused on the absorption, bioavailability and disposition of drugs delivered by oral SMEDDS/SNEDDS (Cherniakov et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

“…In a nice scientific description, Cherniakov et al (2015) discussed the biopharmaceutical points of SEDDS after its oral administration. The review was primarily focused on the absorption, bioavailability and disposition of drugs delivered by oral SMEDDS/SNEDDS (Cherniakov et al, 2015). Apart from this there is no compilation of reported pharmacokinetic results of this delivery system in recent times.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

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

et al. 2016

View full text Add to dashboard Cite

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

show abstract

“…By this way drugs delivered by SEDDS may bypass first pass metabolism. All these abovementioned mechanisms are well-depicted in the review published by Cherniakov et al (2015).…”

Section: Lipidsmentioning

confidence: 82%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

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

et al. 2016

View full text Add to dashboard Cite

show abstract

“…However, the charge on tiny globules definitely affects the extent of absorption from the negatively charged mucosal surface. [33] Zeta potential values suggested that microemulsions were stable and less likely to pose any problem in the short span of processing in GI tract (GIT). As the drug is already in dissolved form within the formulation, the onset of absorption will be faster.…”

Section: Zeta Potential Measurementmentioning

confidence: 99%

Untitled

Butani

2016

AJP

View full text Add to dashboard Cite

Aims: The aim of this study was to formulate a self-microemulsifying drug delivery system (SMEDDS) of Lercanidipine HCl (LCH) using medium chain (MC) and short chain (SC) glycerides as oil phase and to compare the dissolution efficiency of both formulations. Materials and Methods: Different oils and surfactants containing MC and SC fatty acid as basic molecule were screened using quantitative solubility study and constructing pseudoternary phase diagrams. Cosolvents were used as cosurfactants. The preconcentrates were tested for a self-microemulsifying time, % transmittance, cloud point, globule size, zeta potential, and in-vitro drug release. Selected formulations were compared by calculating dissolution efficiencies in different pH media. Results: Capmul MCM, Cremophor ® RH 40, and polyethylene glycol 400 were chosen as oil, surfactant, and cosurfactant, respectively, for MC glyceride and triacetin and Tween 80 were selected as oil and surfactant for SC triglyceride category, respectively. All the formulations spontaneously resulted into transparent microemulsion with globule sizes range from 50 to 90 nm for MC-SMEDDS and 200-317 nm for SC-SMEDDS. The formed microemulsions were stable as shown by zeta potential and cloud point determination. However, in-vitro drug release in 0.1 N HCl showed quite a similar dissolution of all the formulation batches, a study in the different pH media showed that LCH being weak base, possess pH dependent solubility. Conclusions: The MC-SMEDDS were able to resist the effect of pH on dissolution to some extent as compared to pure untreated LCH and simple mixture of oil and surfactant. This piece of research strongly established the need for biorelevant dissolution interphase to differentiate between the formulations.

show abstract

“…In a study by Patel et al (2011), SNEDDS system was able to induce in vivo absorption by 7.5 folds 7 . Moreover, the oil based system will escape pHrelated influence of the GI tract thus ideal as a formulation for oral adminitration 8 . In spite of the beneficial effects of the nanocarriers on living cells, undesirable effects may occur.…”

Section: Introductionmentioning

confidence: 99%

Acute Toxicity of Self Nano-emulsifying Formulation of Curcumin Analogue Gamavuton-0, A New Candidate for Rheumatoid Arthritis Treatment

Chabib¹,

Ikawati²,

Martien³

et al. 2017

IJPTR

View full text Add to dashboard Cite

: Gamavuton-0 (GVT-0), a newly developed compound synthesized by a carbonyl group and a methylene reduction of Curcumin, has been proven to have several anti arthritic activities. The compound has been further proven to have no short-term toxicity in rat in vivo. However, GVT-0 still burdens low water solubility therefore poorly absorbed in oral administration. Currently, a self-nano-emulsifying system has been developed to formulate GVT-0 into a more effective oral anti RA candidate using various oils and surfactants (SNE GVT-0). To study whether this formulation would not alter the safety of the compound in oral administration, an in vivo acute toxicity testing was conducted. A 14 day-study was performed by using four groups of wistar strain Rattus norvegicus, three rats per group, with 300 mg/kg BW GVT-0 as preliminary dose and 2000 mg/kg BW as oral treatment dose, along with naïve GVT-0 and solvent as controls. The protocols and toxic parameters were all conducted following OECD 423. The study showed that all the treatments on both 300 and 2000 mg/kg BW of SNE GVT-0 did not compromise rats' body weight, and toxicity clinical behaviours were observed on the 2000 mg/kgBW of administration, but there is no significance observed for 300 mg/kg BW administration. Microscopic observation under haematoxylin and eosin staining confirmed the clinical findings by showing degeneration and destruction for the most of organs on the 2000 mg/kg BW of administration. The results suggest SNE GVT-0 as in category four in OECD 423 globally harmonized classification system (GHS) with estimated LD50 cut-off as 2000 mg/kg BW.

show abstract

Self-nano-emulsifying drug delivery systems: an update of the biopharmaceutical aspects

Cited by 133 publications

References 92 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

Untitled

Acute Toxicity of Self Nano-emulsifying Formulation of Curcumin Analogue Gamavuton-0, A New Candidate for Rheumatoid Arthritis Treatment

Contact Info

Product

Resources

About