Influence of lipid matrix composition on biopharmaceutical properties of lipid nanoparticles

Keck, Cornelia M.; Specht, David; Brüßler, Jana

doi:10.1016/j.jconrel.2021.08.016

Cited by 23 publications

(10 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…6A). The decrease in corneometer values for the NLC confirms the formation of the invisible patch, that was previously reported for various other NLC formulations [1,2,39,40]. Six hour after application, no significant differences in skin hydration were found between oil, ME, and NE.…”

Section: Skin Hydrationsupporting

confidence: 87%

“…Dry skin will therefore result in poor penetration. Therefore, only long-lasting, durable films can provide an effective and long-lasting dermal penetration [37,[39][40][41]. Data of this study show that after dermal application of the different formulations, the NLC provided the best protection from chemical degradation for the AI surrogate and resulted in the most effective and durable film on top of the skin.…”

Section: Synopsis Of Biopharmaceutical Propertiesmentioning

confidence: 79%

See 1 more Smart Citation

Are lipid nanoparticles really superior? A holistic proof of concept study

Wiemann

Keck

2021

Drug Deliv. and Transl. Res.

Self Cite

View full text Add to dashboard Cite

Lipid nanoparticles are a successful carrier system for dermal drug delivery. They possess various beneficial properties, i.e., increased chemical stability for chemically labile compounds, increased dermal penetration of active compounds, or skin carrying properties after dermal application due to the formation of a so-called “invisible patch.” Despite manifold studies showing these properties individually, a study that investigates if one lipid nanoparticle formulation can really combine all the above-mentioned benefits at once is not yet available. In the present study, lipid nanoparticles (NLC) were produced and characterized regarding their physico-chemical properties. The chemical stability of the incorporated active ingredient (AI) was determined, as well as the dermal penetration efficacy of the AI, and the skin carrying properties of the NLC after dermal penetration. The properties of the NLC were compared to classical formulations, i.e., AI dissolved in pure oil, an o/w cream base and a nanoemulsion. All formulations contained similar lipids and emulsifiers, which allowed for a direct comparison of the different properties. NLC were shown to provide most efficient chemical stabilization and most efficient dermal penetration for the AI. The formation of the invisible patch was shown for the NLC but not for the other formulations. Skin hydration and skin carrying properties were also most pronounced for the NLC. Results provide evidence that NLC can combine all beneficial effects that were previously described in one formulation. Thus, providing evidence that NLC are a holistically superior formulation principle when compared to other formulation principles. Graphical abstract

show abstract

Section: Skin Hydrationsupporting

confidence: 87%

Section: Synopsis Of Biopharmaceutical Propertiesmentioning

confidence: 79%

Are lipid nanoparticles really superior? A holistic proof of concept study

Wiemann

Keck

2021

Drug Deliv. and Transl. Res.

Self Cite

View full text Add to dashboard Cite

show abstract

“…Most liposomes/LNPs are undoubtedly used in medical science, but academics who usually use these nanoparticles for drug delivery prefer conventional bulk methods, such as ethanol dilution, solvent injection or homogenization to prepare liposomes. 19 , 175 , 176 They concentrate on designing and optimizing the nanocarrier itself instead of novel techniques for nanocarrier preparation. Since the production techniques cannot resolve the critical clinical problems in liposomal applications, such as delivery efficacy, organ-specific and cell-specific delivery and toxicity, to mention a few, it was not surprising that these bulk methods were chosen due to simplicity, cost-saving and safety.…”

Section: Discussionmentioning

confidence: 99%

Lipid in Chips: A Brief Review of Liposomes Formation by Microfluidics

Guo¹,

Sun²

2021

IJN

View full text Add to dashboard Cite

“…The NLC are a well-known drug delivery system with superior properties on skin [ 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 ]. In this study, they were produced after a previously established production protocol [ 25 ].…”

Section: Methodsmentioning

confidence: 99%

Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy

Wiemann

Keck

2022

Pharmaceutics

Self Cite

View full text Add to dashboard Cite

(1) Background: The study systematically investigated the influence of dispersed particles within a topical formulation on the dermal penetration efficacy of active compounds that are dissolved in the water phase of this formulation. The aim was to prove or disprove if particle-assisted dermal penetration can be used for improved dermal drug delivery. (2) Methods: Fluorescein was used as a surrogate for a hydrophilic active ingredient (AI). It was dissolved in the water phase of different formulations with and without particles. Two different types of particles (titanium dioxide and nanostructured lipid carriers (NLC)) were used. The influence of particle size and number of particles and the influence of skin hydrating excipients was also investigated. (3) Results demonstrate that the addition of particles can strongly increase the dermal penetration efficacy of AI. The effect depends on the size of the particles and the number of particles in the formulation, where smaller sizes and higher numbers resulted in higher penetration parameters. Formulations with NLC that contained 20% w/w or 40% w/w particles resulted in an about 2-fold higher amount of penetrated AI and increased the penetration depth about 2.5-fold. The penetration-enhancing effect was highly significant (p < 0.001) and allowed for an efficient delivery of the AI in the viable dermis. In contrast, the penetration-enhancing effect of excipients that increase the skin hydration was found to be very limited and not significant (≤5%, p > 0.05). (4) Conclusions: Based on the results, it can be concluded that particle-assisted dermal penetration can be considered to be a simple but highly efficient and industrially feasible formulation principle for improved and tailor-made dermal drug delivery of active compounds.

show abstract

Influence of lipid matrix composition on biopharmaceutical properties of lipid nanoparticles

Cited by 23 publications

References 32 publications

Are lipid nanoparticles really superior? A holistic proof of concept study

Are lipid nanoparticles really superior? A holistic proof of concept study

Lipid in Chips: A Brief Review of Liposomes Formation by Microfluidics

Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy

Contact Info

Product

Resources

About