scholarly journals Performance of Oleic Acid and Soybean Oil in the Preparation of Oil-in-Water Microemulsions for Encapsulating a Highly Hydrophobic Molecule

2021 ◽  
Vol 5 (4) ◽  
pp. 50
Author(s):  
Laura Fernández-Peña ◽  
Boutaina Z. El Mojahid ◽  
Eduardo Guzmán ◽  
Francisco Ortega ◽  
Ramón G. Rubio
Keyword(s):  
Oleic Acid ◽  
Carboxylic Acid ◽  
Soybean Oil ◽  
Size Range ◽  
Pharmaceutical Formulations ◽  
Oil In Water ◽  
Hydrophobic Molecule ◽  
The Stability ◽  
Highly Hydrophobic ◽  
Nanometric Size

This work analyzes the dispersion of a highly hydrophobic molecule, (9Z)-N-(1,3-dihydroxyoctadecan-2-yl)octadec-9-enamide (ceramide-like molecule), with cosmetic and pharmaceutical interest, by exploiting oil-in-water microemulsions. Two different oils, oleic acid and soybean oil, were tested as an oil phase while mixtures of laureth-5-carboxylic acid (Akypo) and 2-propanol were used for the stabilization of the dispersions. This allowed us to obtain stable aqueous-based formulations with a relatively reduced content of oily phase (around 3% w/w), that may enhance the bioavailability of this molecule by its solubilization in nanometric oil droplets (with a size range of 30–80 nm), that allow the incorporation of a ceramide-like molecule of up to 3% w/w, to remain stable for more than a year. The nanometric size of the droplet containing the active ingredient and the stability of the formulations provide the basis for evaluating the efficiency of microemulsions in preparing formulations to enhance the distribution and availability of ceramide-like molecules, helping to reach targets in cosmetic and pharmaceutical formulations.

scholarly journals Engineered Dutasteride-Lipid Based Nanoparticle (DST-LNP) System Using Oleic and Stearic Acid for Topical Delivery

2022 ◽  
Vol 9 (1) ◽  
pp. 11
Author(s):  
Norhayati Mohamed Noor ◽  
Sana Umar ◽  
Azila Abdul-Aziz ◽  
Khalid Sheikh ◽  
Satyanarayana Somavarapu
Keyword(s):  
Oleic Acid ◽  
Size Range ◽  
Negative Impact ◽  
X Ray ◽  
Acid Formulation ◽  
Permeation Studies ◽  
Nanoparticle System ◽  
Dermal Delivery ◽  
Nanometric Size

Male pattern baldness (MPB) is a common condition that has a negative impact on the psycho-social health of many men. This study aims to engineer an alcohol-free formulation to cater for individuals who may have had allergic reactions to alcohol-based preparations. A lipid-based nanoparticle system composed of stearic and oleic acid (solid and liquid lipid) was used to deliver dutasteride (DST) for topical application. Two compositions, with oleic acid (Formulation A) and without (Formulation B), were compared to analyse the role of oleic acid as a potential active ingredient in addition to DST. DST-loaded LNP were prepared using the emulsification–ultrasonication method. All of the prepared formulations were spherical in shape in the nanometric size range (150–300 nm), with entrapment efficiencies of >75%. X-ray diffractograms revealed that DST exists in an amorphous form within the NLP matrices. The drug release behaviour from both LNP preparations displayed slow release of DST. Permeation studies through pig ear skin demonstrated that DST-LNP with oleic acid produced significantly lower permeation into the dermis compared to the formulation without oleic acid. These results suggest that the proposed formulation presents several characteristics which are novel, indicating its suitability for the dermal delivery of anti-androgenic molecules.

scholarly journals Influence of Whey Protein Micro-Gel Particles and Whey Protein Micro-Gel Particles-Xanthan Gum Complexes on the Stability of O/W Emulsions

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2301
Author(s):  
Man Zhang ◽  
Bin Liang ◽  
Hongjun He ◽  
Changjian Ji ◽  
Tingting Cui ◽  
...  
Keyword(s):  
Oxidative Stability ◽  
Whey Protein ◽  
High Speed ◽  
Xanthan Gum ◽  
Physical Stability ◽  
Theoretical Support ◽  
Gel Particles ◽  
Oil In Water ◽  
The Stability ◽  
The Impact

Appropriate pretreatment of proteins and addition of xanthan gum (XG) has the potential to improve the stability of oil-in-water (O/W) emulsions. However, the factors that regulate the enhancement and the mechanism are still not clear, which restricts the realization of improving the emulsion stability by directional design of its structure. Therefore, the effects of whey protein micro-gel particles (WPMPs) and WPMPs-XG complexes on the stability of O/W emulsion were investigated in this article to provide theoretical support. WPMPs with different structures were prepared by pretreatment (controlled high-speed shear treatment of heat-set WPC gels) at pH 3.5–8.5. The impact of initial WPC structure and XG addition on Turbiscan Indexes, mean droplet size and the peroxide values of O/W emulsions was investigated. The results indicate that WPMPs and XG can respectively inhibit droplet coalescence and gravitational separation to improve the physical stability of WPC-stabilized O/W emulsions. The pretreatment significantly enhanced the oxidative stability of WPC-stabilized O/W emulsions. The addition of XG did not necessarily enhance the oxidative stability of O/W emulsions. Whether the oxidative stability of the O/W emulsion with XG is increased or decreased depends on the interface structure of the protein-XG complex. This study has significant implications for the development of novel structures containing lipid phases that are susceptible to oxidation.

scholarly journals Polymeric Micelles for the Enhanced Deposition of Hydrophobic Drugs into Ocular Tissues, without Plasma Exposure

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 744
Author(s):  
Ijeoma F. Uchegbu ◽  
Jan Breznikar ◽  
Alessandra Zaffalon ◽  
Uche Odunze ◽  
Andreas G. Schätzlein
Keyword(s):  
Polymeric Micelles ◽  
Rabbit Model ◽  
Penetration Enhancer ◽  
Hydrophobic Drugs ◽  
Ocular Tissues ◽  
Ocular Penetration ◽  
Self Assembling ◽  
Similar Dose ◽  
Oil In Water ◽  
The Stability

Commercial topical ocular formulations for hydrophobic actives rely on the use of suspensions or oil in water emulsions and neither of these formulation modalities adequately promote drug penetration into ocular tissues. Using the ocular relevant hydrophobic drug, cyclosporine A (CsA), a non-irritant ocular penetration enhancer is showcased, which may be used for the formulation of hydrophobic actives. The activity of this penetration enhancer is demonstrated in a healthy rabbit model. The Molecular Envelope Technology (MET) polymer (N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan), a self-assembling, micelle-forming polymer, was used to formulate CsA into sterile filtered nanoparticulate eye drop formulations and the stability of the formulation tested. Healthy rabbits were dosed with a single dose of a MET–CsA (NM133) 0.05% formulation and ocular tissues analyzed. Optically clear NM133 formulations were prepared containing between 0.01–0.1% w/v CsA and 0.375–0.75% w/v MET polymer. NM133 0.01%, NM133 0.02% and NM133 0.05% were stable for 28 days when stored at refrigeration temperature (5–6 °C) and room temperature (16–23 °C), but there was evidence of evaporation of the formulation at 40 °C. There was no change in drug content when NM133 0.05% was stored for 387 days at 4 °C. On topical dosing to rabbits, corneal, conjunctival and scleral AUC0–24 levels were 25,780 ng.h g−1, 12,046 ng.h g−1 and 5879 ng.h g−1, respectively, with NM133 0.05%. Meanwhile, a similar dose of Restasis 0.05% yielded lower values of 4726 ng.h/g, 4813 ng.h/g and 1729 ng.h/g for the drug corneal, conjunctival and scleral levels, respectively. NM133 thus delivered up to five times more CsA to the ocular surface tissues when compared to Restasis. The MET polymer was non-irritant up to a concentration of 4% w/v. The MET polymer is a non-irritant ocular penetration enhancer that may be used to deliver hydrophobic drugs in optically clear topical ocular formulations.

scholarly journals Nanoemulsions for the Encapsulation of Hydrophobic Actives

Cosmetics ◽  
2021 ◽  
Vol 8 (2) ◽  
pp. 45
Author(s):  
Eduardo Guzmán ◽  
Laura Fernández-Peña ◽  
Lorenzo Rossi ◽  
Mathieu Bouvier ◽  
Francisco Ortega ◽  
...  
Keyword(s):  
Surface Charge ◽  
Long Term Stability ◽  
Promising Tool ◽  
Oil In Water ◽  
Nanometric Range ◽  
Negative Surface ◽  
Negative Surface Charge ◽  
Highly Hydrophobic ◽  
Technological Interest

This work analyzes the dispersion of two highly hydrophobic actives, (9Z)-N-(1,3-dihydroxyoctadecan-2-yl)octadec-9-enamide (ceramidelike molecule) and 2,6-diamino-4-(piperidin-1-yl)pyrimidine 1-oxide (minoxidil), using oil-in-water nanoemulsions with the aim of preparing stable and safe aqueous-based formulations that can be exploited for enhancing the penetration of active compounds through cosmetic substrates. Stable nanoemulsions with a droplet size in the nanometric range (around 200 nm) and a negative surface charge were prepared. It was possible to prepare formulations containing up to 2 w/w% of ceramide-like molecules and more than 10 w/w% of minoxidil incorporated within the oil droplets. This emulsions evidenced a good long-term stability, without any apparent modification for several weeks. Despite the fact that this work is limited to optimize the incorporation of the actives within the nanoemulsion-like formulations, it demonstrated that nanoemulsions should be considered as a very promising tool for enhancing the distribution and availability of hydrophobic molecules with technological interest.

scholarly journals Photoluminescent Coordination Polymers Based on Group 12 Metals and 1H-Indazole-6-Carboxylic Acid

Inorganics ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 20
Author(s):  
Antonio A. García-Valdivia ◽  
Estitxu Echenique-Errandonea ◽  
Gloria B. Ramírez-Rodríguez ◽  
José M. Delgado-López ◽  
Belén Fernández ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Coordination Polymers ◽  
Density Functional ◽  
Free Ligand ◽  
Emission Spectra ◽  
Point Of View ◽  
Theoretical Point ◽  
Fourier Transformed Infrared Spectroscopy ◽  
3D Network ◽  
The Stability

Two new coordination polymers (CPs) based on Zn(II) and Cd(II) and 1H-indazole-6-carboxylic acid (H2L) of general formulae [Zn(L)(H2O)]n (1) and [Cd2(HL)4]n (2) have been synthesized and fully characterized by elemental analyses, Fourier transformed infrared spectroscopy and single crystal X-ray diffraction. The results indicate that compound 1 possesses double chains in its structure whereas 2 exhibits a 3D network. The intermolecular interactions, including hydrogen bonds, C–H···π and π···π stacking interactions, stabilize both crystal structures. Photoluminescence (PL) properties have shown that compounds 1 and 2 present similar emission spectra compared to the free-ligand. The emission spectra are also studied from the theoretical point of view by means of time-dependent density-functional theory (TD-DFT) calculations to confirm that ligand-centred π-π* electronic transitions govern emission of compound 1 and 2. Finally, the PL properties are also studied in aqueous solution to explore the stability and emission capacity of the compounds.

scholarly journals Assessment of Fennel Oil Microfluidized Nanoemulsions Stabilization by Advanced Performance Xanthan Gum

Foods ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 693
Author(s):  
Rubén Llinares ◽  
Pablo Ramírez ◽  
José Antonio Carmona ◽  
Luis Alfonso Trujillo-Cayado ◽  
José Muñoz
Keyword(s):  
Essential Oil ◽  
Rheological Properties ◽  
Xanthan Gum ◽  
Mechanical Energy ◽  
Physical Stability ◽  
Processing Condition ◽  
Oil In Water ◽  
Mechanical Spectra ◽  
The Stability ◽  
Fennel Oil

In this work, nanoemulsion-based delivery system was developed by encapsulation of fennel essential oil. A response surface methodology was used to study the influence of the processing conditions in order to obtain monomodal nanoemulsions of fennel essential oil using the microchannel homogenization technique. Results showed that it was possible to obtain nanoemulsions with very narrow monomodal distributions that were homogeneous over the whole observation period (three months) when the appropriate mechanical energy was supplied by microfluidization at 14 MPa and 12 passes. Once the optimal processing condition was established, nanoemulsions were formulated with advanced performance xanthan gum, which was used as both viscosity modifier and emulsion stabilizer. As a result, more desirable results with enhanced physical stability and rheological properties were obtained. From the study of mechanical spectra as a function of aging time, the stability of the nanoemulsions weak gels was confirmed. The mechanical spectra as a function of hydrocolloid concentration revealed that the rheological properties are marked by the biopolymer network and could be modulated depending on the amount of added gum. Therefore, this research supports the role of advanced performance xanthan gum as a stabilizer of microfluidized fennel oil-in-water nanoemulsions. In addition, the results of this research could be useful to design and formulate functional oil-in-water nanoemulsions with potential application in the food industry for the delivery of nutraceuticals and antimicrobials.

The effect of oleic acid on the stability of magnetite ferrofluid

1995 ◽  
Vol 31 (6) ◽  
pp. 4178-4180 ◽  
Author(s):  
M.S. Dababneh ◽  
N.Y. Ayoub
Keyword(s):  
Oleic Acid ◽  
The Stability
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