Release study of selected terpenes from nanostructured lipid carriers

Lasoń, Elwira; Sikora, Elżbieta; Ogonowski, Jan; Tabaszewska, Małgorzata; Skoczylas, Łukasz

doi:10.1016/j.colsurfa.2016.06.021

Cited by 25 publications

(15 citation statements)

References 30 publications

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“…was found to be 59.1 ± 5.9%. Our results established that, while EE% for UA-G4K was comparable or slightly lower than those reported for UA-loaded lipid- or amphiphilic methoxypoly(ethylene glycol)–polycaprolactone (mPEG–PCL)-based NPs, its DL% was notably higher (49.7% vs. 4–13%) [ 15 , 49 , 50 ]. Also, DL% of UA-G4K was higher than that obtained by solid inclusion complexes of UA with cyclodextrin derivatives, which were obtained with stochiometric ratio of 1:1, and DL% values in the range 26.5–28.7% [ 16 ].…”

Section: Resultssupporting

confidence: 77%

“…Concerning PDI, the value observed for UA-G4K was lower than that observed for the empty dendrimer G4K. Collectively, the PDI value determined for UA-G4K established for a low polydispersity, similar or lower than those previously reported for lipid-polymer-and dendrimer-based UA-formulations[49][50][51]. Interestingly, the results proved a considerable improvement in particle size after the uploading of UA in G4K particles, thus confirming the high value of DL% obtained by HPLC analysis.…”

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confidence: 82%

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Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

2021

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Ursolic acid (UA) is a pentacyclic triterpenoid found in many medicinal plants and aromas endowed with numerous in vitro pharmacological activities, including antibacterial effects. Unfortunately, UA is poorly administered in vivo, due to its water insolubility, low bioavailability, and residual systemic toxicity, thus making urgent the development of water-soluble UA formulations. Dendrimers are nonpareil macromolecules possessing highly controlled size, shape, and architecture. In dendrimers with cationic surface, the contemporary presence of inner cavities and of hydrophilic peripheral functions, allows to encapsulate hydrophobic non-water-soluble drugs as UA, to enhance their water-solubility and stability, and to promote their protracted release, thus decreasing their systemic toxicity. In this paper, aiming at developing a new UA-based antibacterial agent administrable in vivo, we reported the physical entrapment of UA in a biodegradable not cytotoxic cationic dendrimer (G4K). UA-loaded dendrimer nanoparticles (UA-G4K) were obtained, which showed a drug loading (DL%) much higher than those previously reported, a protracted release profile governed by diffusion mechanisms, and no cytotoxicity. Also, UA-G4K was characterized by principal components analysis (PCA)-processed FTIR spectroscopy, by NMR and elemental analyses, and by dynamic light scattering experiments (DLS). The water solubility of UA-G4K was found to be 1868-fold times higher than that of pristine UA, thus making its clinical application feasible.

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Section: Resultssupporting

confidence: 77%

supporting

confidence: 82%

Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

2021

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“…However, forskolin was characterized by the highest value of this factor. Lasoń et al [30] conducted the release study of selected terpenes (geranic acid, forskolin, ursolic acid) from nanostructured lipid carriers. In this case, the highest final release of the active (nearly 70%) was achieved for ursolic acid.…”

Section: Release Of Terpenesmentioning

confidence: 99%

Influence of Terpene Type on the Release from an O/W Nanoemulsion: Experimental and Theoretical Studies

Miastkowska

Śliwa

2020

Molecules

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The interaction between a drug molecule and its carrier’s components is an important factor which influences the drug release profile. For this purpose, molecular dynamics (MD) may be the in silico tool which can help to understand the mechanism of drug loading/release. The aim of this work is to explain the effect of interactions between different types of terpenes, namely perillyl alcohol, forskolin, ursolic acid, and the nanoemulsion droplet core, on the release by means of experimental and theoretical studies. The basic nanoemulsion was composed of caprylic/capric triglyceride as the oil phase, polysorbate 80 as the emulsifier, and water. The in vitro release tests from a terpene-loaded nanoemulsion were carried out to determine the release profiles. The behavior of terpenoids in the nanoemulsion was also theoretically investigated using the molecular dynamics method. The forskolin-loaded nanoemulsion showed the highest percentage of drug release (almost 80% w/w) in contrast to ursolic acid and perillyl alcohol-loaded nanoemulsions (about 53% w/w and 19% w/w, respectively). The results confirmed that the kinetic model of release was terpene-type dependent. The zero-order model was the best to describe the ursolic acid release profile, while the forskolin and the perillyl alcohol followed a first-order and Higuchi model, respectively. Molecular dynamics simulations, especially energetical analysis, confirmed that the driving force of terpenes diffusion from nanoemulsion interior was their interaction energy with a surfactant.

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“…Relatively to the release study, overall, it was observed a burst release in the first hours and then a gradual release. Furthermore, it has been observed that terpenes with lower lipophilicity tend to remain linked to lipid nanoparticles for longer time than higher lipophilic terpenes (Lasoń, Sikora, Ogonowski, Tabaszewska, & Skoczylas, 2016).…”

Section: Nanostructured Lipid Carriers (Nlcs)mentioning

confidence: 99%

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Gonçalves

Martins

Duarte

et al. 2018

Trends in Food Science & Technology

176

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Background: Aiming at the enhancement of food products' nutritional and health value, the incorporation of nutraceuticals has attracted increasing interest in the last years. However, they often exhibit low water solubility and stability, limiting their direct incorporation into food products. Also, they show very low bioavailability due to limited bioaccessibility, poor absorption and/or chemical transformation within the gastrointestinal tract. This renders their health benefits extremely difficult to be realized by the consumers. Scope and approach: In the present review the recent innovations regarding the formulation and design of biobased micro and nano-delivery systems to encapsulate nutraceuticals is discussed; it also gives an overview of the challenges associated to their development; and highlights some strategies to enhance nutraceuticals' bioavailability. An insight about delivery systems' potential toxicity (in particular at nano-scale) is also provided. Key findings and conclusions: Recent developments in the design of bio-based delivery systems offer the possibility of stabilizing and enhancing nutraceuticals' functionality within food products. In fact, different strategies can be used to enhance nutraceuticals' bioavailability: i) nano-delivery systems, besides showing a huge potential for the protection of valuable nutraceuticals during food processing/digestion, can be used to increase their bioavailability; ii) absorption enhancement technologies have been successfully used to increase nutraceuticals' membrane permeation; and iii) excipient foods have been shown to improve nutraceuticals' biological activity. However, the application of these enabling technologies to food is hindered by very pertinent issues that can be summarized in the effective preservation/maximization of the nutraceuticals' bioactivity and safety, once inside the human body.

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Release study of selected terpenes from nanostructured lipid carriers

Cited by 25 publications

References 30 publications

Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

Influence of Terpene Type on the Release from an O/W Nanoemulsion: Experimental and Theoretical Studies

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

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