Effect of drug solubility and lipid carrier on drug release from lipid nanoparticles for dermal delivery

Zoubari, Gaith; Staufenbiel, Sven; Volz, Pierre; Alexiev, Ulrike; Bodmeier, Roland

doi:10.1016/j.ejpb.2016.10.021

Cited by 58 publications

(38 citation statements)

References 26 publications

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“…Solubility studies show higher drug solubility in GMS, either alone or combined with LEC than in individual CH or CH-LEC mixture (S1 File, S5 Table). The high affinity of the drug to the lipid could hamper the partitioning of E to the dissolution medium as stated earlier [81]. Secondly, GMS was reported to be able of packing with LEC due to hydrophobic interaction between their respective hydrophobic parts and hydrogen bonds between their hydrophilic segments resulting in higher viscosity upon contact with water [82].…”

Section: Drug Release Studymentioning

confidence: 89%

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

et al. 2020

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A platform capable of specifically delivering an antiviral drug to the liver infected with hepatitis B is a major concern in hepatology. Vaccination has had a major effect on decreasing the emerging numbers of new cases of infection. However, the total elimination of the hepatitis B virus from the body requires prolonged therapy. In this work, we aimed to target the liver macrophages with lipid polymer hybrid nanoparticles (LPH), combining the merit of polymeric nanoparticles and lipid vesicles. The hydrophilic antiviral drug, entecavir (E), loaded LPH nanoparticles were optimized and physicochemically characterized. A modulated lipidic corona, as well as, an additional coat with vitamin E were used to extend the drug release enhance the macrophage uptake. The selected vitamin E coated LPH nanoparticles enriched with lecithin-glyceryl monostearate lipid shell exhibited high entrapment for E (80.47%), a size � 200 nm for liver passive targeting, extended release over one week, proven serum stability, retained stability after refrigeration storage for 6 months. Upon macrophage uptake in vitro assessment, the presented formulation displayed promising traits, enhancing the cellular retention in J774 macrophages cells. In vivo and antiviral activity futuristic studies would help in the potential application of the ELPH in hepatitis B control.

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Section: Drug Release Studymentioning

confidence: 89%

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

et al. 2020

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“…It was supposed that the existence of liquid lipid inside the nanoparticle would inhibit highly ordered recrystallization after the preparation process leading to an increased drug loading capacity and improved release profile [10]. Therefore, nanostructured lipid carriers (NLC) have obtained an increased interest because of various advantages such as the increased drug loading capacity [11,12], controlled drug release [13], high drug stability [14], biocompatibility, and non-toxicity [15,16]. Several investigations concerning the physicochemical properties of SLN and NLC have been carried out so far.…”

Section: Introductionmentioning

confidence: 99%

Vesicle-like structure of lipid-based nanoparticles as drug delivery system revealed by molecular dynamics simulations

Khalkhali

Mohammadinejad

Khoeini

et al. 2019

International Journal of Pharmaceutics

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Lipid-based drug delivery systems are considered as promising vehicles for hydrophobic drug compounds. Lipid distribution within the droplet can affect drug loading capacity in these carriers. However, it is extremely challenging to determine the nanostructure within these carriers through the implementation of the direct experimental methods due to the ultrafine size. Therefore, coarse grained molecular dynamics (MD) simulation was utilized to model different kinds of lipid-based nanoparticles of the diameter about 12 nm including solid lipid nanoparticles (SLN), nanoemulsion (NE), and nanostructured lipid carriers (NLC), and the organization of the lipids within the carriers was explored. The aforementioned nanoparticles consisted of stearic acid, oleic acid as lipids, and sodium dodecyl sulfate (SDS) as a surfactant in water medium. Furthermore, the impact of solid to liquid mass ratio on the lipid distribution within the lipid matrix was investigated regarding the NLC simulations. In the equilibrium state, we observed the vesicle-like structure for all the investigated systems in which the hydrophilic moieties of the lipids and surfactant organized a semi-bilayer fold into the droplet and the hydrophobic tails accumulated among them. It is worth mentioning although SDS as a harsh surfactant, which is a special case, was expected to be present in the surface of the droplet, it penetrated into the lipids. Additionally, our results showed remarkable entrapped water beads inside the droplet in the form of one or more cavities along the internal layer of the head groups which was surrounded by lipid head groups. It was also reported that in the building structure of the nanoemulsion and SLN, in the central parts of the droplets, lipids were denser than the case of NLCs. Moreover, no crystallization occurred within the lipid-based carriers. Finally, the results indicated that, in the case of NLC simulations, the lipid distribution within the lipid matrix was insensitive to the mass fraction of solid to liquid lipids.

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“…Since single‐molecule high‐resolution microscopy and single‐particle tracking using TIRFM is used to detect individual fluorescent dye molecules or fluorescently labeled drug molecules , in this study TIRFM was applied to selectively detect individual as well as clusters of fluorescently tagged nanoparticles. Upon application on skin, TIRFM provided information on the localization as well as the lateral diffusion dynamics in certain skin compartments .…”

Section: Discussionmentioning

confidence: 99%

“…The data acquisition was conducted using the software package Hipic (Hamamatsu, Japan). Data analysis was performed as in References 38 and 39.…”

Section: Methodsmentioning

confidence: 99%

“…Due to the invasiveness of those methods, wide‐field 2 PM was applied for non‐invasive, in situ imaging to gain insight into rare events of deeper penetration of nanoparticles. Single‐molecule total internal reflection fluorescence microscopy (TIRFM) was applied to analyze fluorescence signals with higher sensitivity and spatial resolution .…”

Section: Introductionmentioning

confidence: 99%

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Identification of polystyrene nanoparticle penetration across intact skin barrier as rare event at sites of focal particle aggregations

Döge

Hadam

Volz

et al. 2018

Journal of Biophotonics

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The question whether nanoparticles can cross the skin barrier is highly debated. Even in intact skin rare events of deeper penetration have been reported, but technical limitations and possible artifacts require careful interpretation. In this study, horizontal scanning by 2-photon microscopy (2 PM) of full-thickness human skin samples placed in a lateral position yielded highly informative images for skin penetration studies of fluorescently tagged nanoparticles. Scanning of large fields of view allowed for detailed information on interfollicular and follicular penetration in tissue blocks without damaging the sample. Images in histomorphological correlation showed that 2P-excited fluorescence signals of fluorescently tagged 20 and 200 nm polystyrene nanoparticles preferentially accumulated in the stratum corneum (SC) and in the upper part of vellus hair follicles (HFs). Rare events of deeper penetration in the SC and in the infundibulum of vellus HFs were observed at sites of high focal particle aggregations. Wide-field 2 PM allows for imaging of nanoparticle penetration in large tissue blocks, whereas total internal reflection microscopy (TIRFM) enables selective detection of individual nanoparticles as well as clusters of nanoparticles in the SC and within the epidermal layer directly beneath the SC, thus confirming barrier crossing with high sensitivity.

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Effect of drug solubility and lipid carrier on drug release from lipid nanoparticles for dermal delivery

Cited by 58 publications

References 26 publications

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

Vesicle-like structure of lipid-based nanoparticles as drug delivery system revealed by molecular dynamics simulations

Identification of polystyrene nanoparticle penetration across intact skin barrier as rare event at sites of focal particle aggregations

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