Ethyl oleate-containing nanostructured lipid carriers improve oral bioavailability of trans -ferulic acid ascompared with conventional solid lipid nanoparticles

2016 ◽  
Vol 511 (1) ◽  
pp. 57-64 ◽  
Author(s):  
Yongtai Zhang ◽  
Zhe Li ◽  
Kai Zhang ◽  
Gang Yang ◽  
Zhi Wang ◽  
...  
Planta Medica ◽  
2020 ◽  
Vol 86 (05) ◽  
pp. 364-372 ◽  
Author(s):  
Jidapa Musika ◽  
Nuannoi Chudapongse

AbstractLupinifolin, a plant flavonoid, has been reported to possess various pharmacological effects. It most likely exerts low oral bioavailability because of poor water solubility. The objective of this study was to develop lipid nanocarriers as drug delivery systems to increase the gastrointestinal absorption of lupinifolin extracted from Albizia myriophylla. Three types of nanocarriers, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were prepared by an emulsification-sonication technique. All three types of nanocarriers loaded with lupinifolin, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were successfully synthesized. The lipid components chosen to formulate nanocarriers were tripalmitin and/or medium chain triglyceride. Physicochemical characterizations along with releasing profiles of lupinifolin-loaded lipid nanocarriers were compared. It was found that the best lipid nanocarrier for lupinifolin was lupinifolin-loaded nanostructured lipid carriers, which demonstrated the particle size of 151.5 ± 0.1 nm, monodispersity distribution with a polydispersity index of 0.24, negative surface charge at − 41.2 ± 0.7 mV, high encapsulation (99.3%), and high loading capacity (5.0%). The obtained lupinifolin-loaded nanostructured lipid carriers exhibited prolonged release in a simulated circulatory system but produced a low release in gastrointestinal conditions (3.7%). Intestinal permeability of the nanocarriers was further evaluated in everted intestinal sacs. The results from the ex vivo study indicated that lupinifolin-loaded nanostructured lipid carriers significantly increased the absorption of lupinifolin compared to the native form. In conclusion, lupinifolin-loaded lipid nanocarriers were successfully formulated as delivery systems to enhance its oral bioavailability. Further in vivo experiments are needed to validate the results from this study.


Author(s):  
Neslihan Üstündağ Okur ◽  
Panoraia I. Siafaka ◽  
Evren Homan Gökçe

Background: The oral application of drugs is the most popular route through which the systemic effect can be achieved. Nevertheless, oral administration is limited by difficulties related to physicochemical properties of the drug molecule, including low aqueous solubility, instability, low permeability, and rapid metabolism, all of which result in low and irregular oral bioavailability. Objective: The enhancement of oral bioavailability of drug molecules with such properties could lead to extreme complications in drug preparations. Oral lipid based nanoparticles seems to possess extensive advantages due to their ability to increase the solubility, simplifying intestinal absorption and decrease or eradicate the effect of food on the absorption of low soluble, lipophilic drugs and therefore improving the oral bioavailability. Method: The present review provides a summary of the general theory of lipid based nanoparticles, their preparation methods as well as their oral applications. Moreover, the oral drug delivery challenges are discussed. Results: According to this review, the most frequent types of lipid-based nanoparticle, the solid lipid nanoparticles and nanostructured lipid carriers are potent oral carriers due to their ability to penetrate the oral drug adsorption barriers. Moreover, such lipid nanoparticles can be beneficial drug carriers against cardiovascular risk disorders as diabetes, hypertension etc. Conclusion: In this review, the most current and promising studies involving Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as oral drug carriers are reported aiming to assist researchers who focus their research on lipid based nanoparticles.


2009 ◽  
Vol 00 (00) ◽  
pp. 090820062440031-9 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Mohsen Minayian ◽  
Elaheh Moazen

2011 ◽  
Vol 6 (4) ◽  
pp. 240-250 ◽  
Author(s):  
Rajashree Hirlekar ◽  
Harshal Garse ◽  
Vilasrao Kadam

2021 ◽  
Vol 14 (8) ◽  
pp. 711
Author(s):  
Cláudia Pina Costa ◽  
Sandra Barreiro ◽  
João Nuno Moreira ◽  
Renata Silva ◽  
Hugo Almeida ◽  
...  

The nasal route has been used for many years for the local treatment of nasal diseases. More recently, this route has been gaining momentum, due to the possibility of targeting the central nervous system (CNS) from the nasal cavity, avoiding the blood−brain barrier (BBB). In this area, the use of lipid nanoparticles, such as nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN), in nasal formulations has shown promising outcomes on a wide array of indications such as brain diseases, including epilepsy, multiple sclerosis, Alzheimer’s disease, Parkinson’s disease and gliomas. Herein, the state of the art of the most recent literature available on in vitro studies with nasal formulations of lipid nanoparticles is discussed. Specific in vitro cell culture models are needed to assess the cytotoxicity of nasal formulations and to explore the underlying mechanism(s) of drug transport and absorption across the nasal mucosa. In addition, different studies with 3D nasal casts are reported, showing their ability to predict the drug deposition in the nasal cavity and evaluating the factors that interfere in this process, such as nasal cavity area, type of administration device and angle of application, inspiratory flow, presence of mucoadhesive agents, among others. Notwithstanding, they do not preclude the use of confirmatory in vivo studies, a significant impact on the 3R (replacement, reduction and refinement) principle within the scope of animal experiments is expected. The use of 3D nasal casts to test nasal formulations of lipid nanoparticles is still totally unexplored, to the authors best knowledge, thus constituting a wide open field of research.


2021 ◽  
Author(s):  
Burcu Üner ◽  
Samet Özdemir ◽  
Çetin Taş ◽  
Yıldız Özsoy ◽  
Melike Üner

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.


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