Development and in vitro characterisation of an oral self-emulsifying delivery system for daptomycin

Zupančič, Ožbej; Partenhauser, Alexandra; Lam, Hung Thanh; Rohrer, Julia; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ejps.2015.10.005

Cited by 65 publications

(28 citation statements)

References 28 publications

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“…SEDDS composed of oil, surfactants and cosurfactants that are spontaneously emulsified in gastric fluid are not only used to incorporate poor water-soluble drugs but their protection against enzymatic degradation is also shown (Friedl et al, 2013;Rohrer et al, 2016;Zupančič et al, 2016). In addition, SEDDS can rapidly diffuse through mucus due to their small average droplet size and their shape deformation ability and exhibit high affinity to phospholipid bilayer of intestinal cells.…”

Section: Introductionmentioning

confidence: 98%

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Suchaoin

Sousa

Netsomboon

et al. 2016

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 98%

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Suchaoin

Sousa

Netsomboon

et al. 2016

International Journal of Pharmaceutics

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“…Via hydrophobic ion pairing with cationic surfactants, however, even hydrophilic macromolecular drugs such as peptides, heparins and DNA/RNA‐based drugs can be incorporated in SEDDS. Daptomycin and enoxaparin, for example, were ion‐paired with dodecylamine hydrochloride, cetrimonium bromide and benzalkonium chloride and then successfully incorporated into SEDDS for oral delivery . DNA/RNA‐based drugs are similar to peptide drugs regarding their hydrophilicity and sensibility to enzymatic degradation.…”

Section: Introductionmentioning

confidence: 99%

“…Daptomycin and enoxaparin, for example, were ion-paired with dodecylamine hydrochloride, cetrimonium bromide and benzalkonium chloride and then successfully incorporated into SEDDS for oral delivery. [3,4] DNA/RNA-based drugs are similar to peptide drugs regarding their hydrophilicity and sensibility to enzymatic degradation. Therefore, hydrophobically ion-paired complexes of pDNA were also studied for oral delivery via SEDDS.…”

Section: Introductionmentioning

confidence: 99%

Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?

Lam

Le‐Vinh

Phan³

et al. 2018

Journal of Pharmacy and Pharmacology

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Objectives The aim of this study was to evaluate the cytotoxicity of self‐emulsifying drug delivery systems (SEDDS) containing five different cationic surfactants. Methods Cationic surfactants were added in a concentration of 1% and 5% (m/m) to SEDDS comprising 30% Capmul MCM, 30% Captex 355, 30% Cremophor EL and 10% propylene glycol. The resulting formulations were characterized in terms of size, zeta potential, in‐vitro haemolytic activity and toxicity on Caco‐2 via MTT assay and lactate dehydrogenase release assay. Key findings The evaluated surfactants had in both concentrations a minor impact on the size of SEDDS ranging from 30.2 ± 0.6 to 55.4 ± 1.1 nm, whereas zeta potential changed significantly from −9.0 ± 0.3 to +28.8 ± 1.6 mV. The overall cytotoxicity of cationic surfactants followed the rank order: hexadecylpyridinium chloride > benzalkonium chloride > alkyltrimethylammonium bromide > octylamine > 1‐decyl‐3‐methylimidazolium. The haemolytic activity of the combination of cationic surfactants and SEDDS on human red blood cells was synergistic. Furthermore, cationic SEDDS exhibited higher cytotoxicity of Caco‐2 cells compared to SEDDS without cationic surfactants. Conclusions According to these results, SEDDS and cationic surfactants seem to bear an additive up to synergistic toxic risk.

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“…However, digestion for both the formulations was observed to be quite fast at early time points. Maisine-35-1 and Capmul MCM, both being the lipase substrates[47], exhibited similar lipolysis rates as indicated by insignificant difference (P>0.01) in NaOH consumption of LCG-and MCG-SNELS (…”

mentioning

confidence: 93%

Enhancing biopharmaceutical performance of an anticancer drug by long chain PUFA based self-nanoemulsifying lipidic nanomicellar systems

Khurana

Beg

Burrow

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

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The aim of this study was to develop polyunsaturated fatty acid (PUFA) long chain glyceride (LCG) enriched self-nanoemulsifying lipidic nanomicelles systems (SNELS) for augmenting lymphatic uptake and enhancing oral bioavailability of docetaxel and compare its biopharmaceutical performance with a medium-chain fatty acid glyceride (MCG) SNELS. Equilibrium solubility and pseudo ternary phase studies facilitated the selection of suitable LCG and MCG. The critical material attributes (CMAs) and critical process parameters (CPPs) were earmarked using Placket-Burman Design (PBD) and Fractional Factorial Design (FFD) for LCG- and MCG-SNELS respectively, and nano micelles were subsequently optimized using I- and D-optimal designs. Desirability function unearthed the optimized SNELS with T <5min, D <100nm, Rel >85% and Perm >75%. The SNELS demonstrated efficient biocompatibility and energy dependent cellular uptake, reduced P-gp efflux and increased permeability using bi-directional Caco-2 model. Optimal PUFA enriched LCG-SNELS exhibited distinctly superior permeability and absorption parameters during ex vivo permeation, in situ single pass intestinal perfusion, lymphatic uptake and in vivo pharmacokinetic studies over MCG-SNELS.

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Development and in vitro characterisation of an oral self-emulsifying delivery system for daptomycin

Cited by 65 publications

References 28 publications

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?

Enhancing biopharmaceutical performance of an anticancer drug by long chain PUFA based self-nanoemulsifying lipidic nanomicellar systems

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