Development and <i>in vitro</i> characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

Zupančič, Ožbej; Rohrer, Julia; Lam, Hung Thanh; Grießinger, Julia Anita; Bernkop‐Schnürch, Andreas

doi:10.1080/03639045.2017.1338722

Cited by 29 publications

(20 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Section: Cloud Point Assessmentmentioning

confidence: 99%

“…SEDDSs are sensitive towards changes in temperature [33,141]. However, excipients can remain functional while subjected to different temperatures that do not exceed the temperature at which the dehydration of components is observed [141]. Dehydration of excipients incorporated in emulsified systems may be visually identified as a sudden change of formulation appearance, from clear to turbid, once exposed to heightened temperatures [142].…”

Section: Cloud Point Assessmentmentioning

confidence: 99%

“…Dehydration of excipients incorporated in emulsified systems may be visually identified as a sudden change of formulation appearance, from clear to turbid, once exposed to heightened temperatures [142]. This specific temperature is denoted the cloud point of SEDDSs [141,142]. Dehydration of excipients causes irreversible phase separation, which in turn risks erratic drug release, since spontaneous emulsification is destroyed by irreversible phase separation [141].…”

Section: Cloud Point Assessmentmentioning

confidence: 99%

“…This specific temperature is denoted the cloud point of SEDDSs [141,142]. Dehydration of excipients causes irreversible phase separation, which in turn risks erratic drug release, since spontaneous emulsification is destroyed by irreversible phase separation [141]. For the purpose of oral SEDDS development, formulations should own a cloud point temperature higher than 37 • C, similar to the systemic circulation temperature.…”

Section: Cloud Point Assessmentmentioning

confidence: 99%

“…For the purpose of oral SEDDS development, formulations should own a cloud point temperature higher than 37 • C, similar to the systemic circulation temperature. This is to avoid the dehydration of excipients within the gastrointestinal tract [141]. Contrary, SEDDSs projected for topical drug delivery should portray cloud points exceeding 32 • C as to avoid formulation instability at the skin surface, which is known for an approximate temperature of 32 • C. However, SEDDSs intended for transdermal drug delivery should follow the same criteria as oral SEDDSs by exhibiting the dehydration of excipients at a temperature exceeding 37 • C, as these droplets should eventually reach the blood circulation in order to establish therapeutic effects [143].…”

Section: Cloud Point Assessmentmentioning

confidence: 99%

See 4 more Smart Citations

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

View full text Add to dashboard Cite

Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing capacity lead the way forward to ground-breaking research. Contrarily, SEDDSs destined for topical/transdermal drug delivery have received limited attention. Therefore, this review is focused at utilising principles, established during development of oral SEDDSs, and tailoring them to fit evaluation strategies for an optimised topical/transdermal drug delivery vehicle. This includes a detailed discussion of how the authentic pseudo-ternary phase diagram is employed to predict phase behaviour to find the self-emulsification region most suitable for formulating topical/transdermal SEDDSs. Additionally, special attention is given to the manner of characterising oral SEDDSs compared to topical/transdermal SEDDSs, since absorption within the gastrointestinal tract and the multi-layered nature of the skin are two completely diverse drug delivery territories. Despite the advantages of the topical/transdermal drug administration route, certain challenges such as the relatively undiscovered field of skin metabolomics as well as the obstacles of choosing excipients wisely to establish skin penetration enhancement might prevail. Therefore, development of topical/transdermal SEDDSs might be more complicated than expected.

show abstract

Section: Cloud Point Assessmentmentioning

confidence: 99%

Section: Cloud Point Assessmentmentioning

confidence: 99%

Section: Cloud Point Assessmentmentioning

confidence: 99%

Section: Cloud Point Assessmentmentioning

confidence: 99%

Section: Cloud Point Assessmentmentioning

confidence: 99%

See 3 more Smart Citations

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

View full text Add to dashboard Cite

show abstract

Histidine-based ionizable cationic surfactants: novel biodegradable agents for hydrophilic macromolecular drug delivery

Polidori,

To,

Kali

et al. 2024

Drug Deliv. and Transl. Res.

View full text Add to dashboard Cite

The aim of this study was to design surfactants based on histidine (His) for hydrophobic ion-pairing and evaluate their safety and efficacy. Lauryl, palmitoyl and oleyl alcohol, as well as 2-hexyl-1-decanol were converted into surfactants with histidine as head-group via esterification. The synthesized His-surfactants were characterized regarding pKa, critical micellar concentration (CMC), biodegradability, toxicity on Caco-2 cells, and ability to provide endosomal escape. Furthermore, the suitability of these agents to be employed as counterions in hydrophobic ion pairing was evaluated. Chemical structures were confirmed by 1H-NMR, FT-IR, and MS. The synthesized surfactants showed pKa values ranging from 4.9 to 6.0 and CMC values in the range of 0.3 to 7.0 mM. Their biodegradability was proven by enzymatic cleavage within 24 h. Below the CMC, His-surfactants did not show cytotoxic effects on Caco-2 cells (cell viability > 80%). All His-surfactants showed the ability to provide endosomal escape in a pH-dependent manner in the range of 5.2 to 6.8. Complexes formed between His-surfactants and heparin or plasmid DNA (pDNA) via hydrophobic ion pairing showed at least 100-fold higher lipophilicity than the correspondent model drugs. According to these results, His-surfactants might be a promising safe tool for delivering hydrophilic macromolecular drugs and nucleic acids. Graphical abstract

show abstract

Recent trends of self-emulsifying drug delivery system for enhancing the oral bioavailability of poorly water-soluble drugs

Tran

Park

2021

J. Pharm. Investig.

View full text Add to dashboard Cite

Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

Abstract: The results of this study suggest that the developed SEDDS could be considered for oral opioid peptide delivery.

Cited by 29 publications

References 37 publications

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

Histidine-based ionizable cationic surfactants: novel biodegradable agents for hydrophilic macromolecular drug delivery

Recent trends of self-emulsifying drug delivery system for enhancing the oral bioavailability of poorly water-soluble drugs

Contact Info

Product

Resources

About