Preparation and characterization of 12-HSA-based organogels as injectable implants for the controlled delivery of hydrophilic and lipophilic therapeutic agents
“…However, the shift was more accentuated for the 12HSA organogels. The melting temperature (Tmelt) for the 12HSA organogels without VE was close to 79 °C, as reported by Esposito and coworkers [ 38 ] at the same concentration, but higher than 37 °C for the gelation temperature (Tgel). Besides the different rheometer geometries and oily phases, the authors used strategies that could impact the crystallization pattern, such as a slower cooling rate compared to in our experiment (1 °C/min), a surfactant, and a co-solvent [ 3 , 37 ].…”
Candelilla wax (CW) and 12-hydroxystearic acid (12HSA) are classic solid-fiber-matrix organogelators. Despite the high number of studies using those ingredients in oily systems, there is scarce literature using a mixture of oil and antioxidants. Vitamin E (VE) is an important candidate for its lipophilicity and several applications on pharmaceutical, cosmetics, and food industries. In this work, we investigated the influences of mixtures between vegetable oil (VO) and VE on the microstructures and rheological properties of CW and 12HSA organogels. A weak gel (G′′/G′ > 0.1) with a shear-thinning behavior was observed for all samples. The presence of VE impacted the gel strength and the phase transition temperatures in a dose-dependent pattern. Larger and denser packed crystals were seen for 12HSA samples, while smaller and more dispersed structures were obtained for CW organogels. The results obtained in this work allowed the correlation of the structural and mechanical properties of the organogels, which plays an important role in the physical-chemical characteristics of these materials.
“…However, the shift was more accentuated for the 12HSA organogels. The melting temperature (Tmelt) for the 12HSA organogels without VE was close to 79 °C, as reported by Esposito and coworkers [ 38 ] at the same concentration, but higher than 37 °C for the gelation temperature (Tgel). Besides the different rheometer geometries and oily phases, the authors used strategies that could impact the crystallization pattern, such as a slower cooling rate compared to in our experiment (1 °C/min), a surfactant, and a co-solvent [ 3 , 37 ].…”
Candelilla wax (CW) and 12-hydroxystearic acid (12HSA) are classic solid-fiber-matrix organogelators. Despite the high number of studies using those ingredients in oily systems, there is scarce literature using a mixture of oil and antioxidants. Vitamin E (VE) is an important candidate for its lipophilicity and several applications on pharmaceutical, cosmetics, and food industries. In this work, we investigated the influences of mixtures between vegetable oil (VO) and VE on the microstructures and rheological properties of CW and 12HSA organogels. A weak gel (G′′/G′ > 0.1) with a shear-thinning behavior was observed for all samples. The presence of VE impacted the gel strength and the phase transition temperatures in a dose-dependent pattern. Larger and denser packed crystals were seen for 12HSA samples, while smaller and more dispersed structures were obtained for CW organogels. The results obtained in this work allowed the correlation of the structural and mechanical properties of the organogels, which plays an important role in the physical-chemical characteristics of these materials.
“…Nevertheless, it was shown that 12‐HSA oleogels could be a promising tool for the controlled release of neutraceuticals in tablets [ 104 ] or even injectable implants. [ 105 ]…”
Oleogels offer the possibility to replace conventional saturated fatty acid (SAFA)-based lipids with a healthier alternative by immobilizing liquid edible oils in a 3D-network which is provided by an oleogelator. Numerous molecules which can structure oils rich in (poly)unsaturated fatty acids have been identified. These differ greatly in their chemical composition, network formation, and interactions and thus macroscopic properties of the respective oleogels. Oleogels have been a focal point of food research for over 20 years, yet product applications are lacking. Hence, the question arises whether the application of oleogels is unfeasible or if science lost sight of its objective. This review aims to assess different structuring systems concerning their availability, their potential for the utilization in food products and, if possible, their prices. Moreover, recent studies comprising the application of oleogels in food products are reviewed with special emphasis on the state and the function of the lipid phase during processing and in the final product. Therefore, the physical properties and preparation methods of different oleogels need to be considered in connection with the respective food application. Finally, it is discussed whether the application of oleogels is justified in these products and advantageous in comparison to liquid oil. Practical Applications: A diet rich in mono-and polyunsaturated fatty acids which make up the majority of liquid edible oils lowers the risk to suffer from cardiovascular diseases. Unfortunately, these oils cannot provide texture to food products in their native state. Oleogelation has the potential to deliver the solid structure necessary for numerous food products by transferring an oil rich in essential fatty acids into a solid-like structure. Besides, the nutritional value of these oils remains practically unchanged. Although oleogelation has been the objective of various research groups for more than 20 years, product applications are scarce. This review aims to stimulate the mindfulness of research concerning the successful application of oleogels in food products. This hopefully enables a better connection between science and industry.
“…However, the disadvantages of these polymers include their degradation to highly acidic monomers, which might trigger autocatalytic processes [ 13 , 14 , 15 ], drug degradation [ 16 ], or drug precipitation [ 17 ] prior to release due to the formation of highly acidic microenvironments [ 13 ] inside the polymer matrix. Solid lipids [ 18 , 19 ], organogels [ 20 , 21 , 22 ], and phospholipids [ 23 , 24 ] are biodegradable and biocompatible alternatives to PLGA and PLA, which deserve further investigation.…”
PLGA-based in situ forming implants (ISFI) often require a high amount of potentially toxic solvents such as N methyl-Pyrrolidone (NMP). The aim of the present study was to develop lipid in-situ-forming oleogels (ISFOs) as alternative delivery systems. 12-Hydroxystearic acid (12-HSA) was selected as the oleogelling agent and three different oleoformulations were investigated: (a) 12-HSA, peanut oil (PO), NMP; (b) 12-HSA, medium-chain triglycerides (MCT), ethanol; (c) 12-HSA, isopropyl myristate (IPM), ethanol. The effects of the 12-HSA concentration, preparation method, and composition on the mechanical stability were examined using a texture analysis and oscillating rheology. The texture analysis was used to obtain information on the compression strength. The amplitude sweeps were analyzed to provide information on the gel strength and the risk of brittle fractures. The frequency sweeps allowed insights into the long-term stability and risk of syneresis. The syringeability of the ISFOs was tested, along with their acute and long-term cytotoxicity in vitro. The developed ISFOs have the following advantages: (1) the avoidance of highly acidic degradation products; (2) low amounts of organic solvents required; (3) low toxicity; (4) low injection forces, even with small needle sizes. Therefore, ISFOs are promising alternatives to the existing polymer/NMP-based ISFIs.
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