Solid lipid nanoparticles and nanostructured lipid carriers: A review emphasizing on particle structure and drug release

Gordillo-Galeano, Aldemar; Mora-Huertas, Claudia Elizabeth

doi:10.1016/j.ejpb.2018.10.017

Cited by 352 publications

(215 citation statements)

References 274 publications

Supporting

Mentioning

200

Contrasting

Unclassified

Order By: Relevance

“…Solid lipid nanoparticles (SLNs) are nanosized spherical shaped structures composed of a solid lipid core stabilized by surfactants and eventually co-surfactants [157,199,202,236,237]. Several lipids are used in the formulation of SLNs, such as triglycerides (tricaprin, trilaurin, tripalmitin), hard fat type lipids (glycerol behenate, glycerol palmitostearate), and waxes (ethyl palmitate).…”

Section: Solid Lipid Nanoparticles and Nanostructured Lipid Carriersmentioning

confidence: 99%

Lipid Systems for the Delivery of Amphotericin B in Antifungal Therapy

2020

View full text Add to dashboard Cite

Amphotericin B (AmB), a broad-spectrum polyene antibiotic in the clinic for more than fifty years, remains the gold standard in the treatment of life-threatening invasive fungal infections and visceral leishmaniasis. Due to its poor water solubility and membrane permeability, AmB is conventionally formulated with deoxycholate as a micellar suspension for intravenous administration, but severe infusion-related side effects and nephrotoxicity hamper its therapeutic potential. Lipid-based formulations, such as liposomal AmB, have been developed which significantly reduce the toxic side effects of the drug. However, their high cost and the need for parenteral administration limit their widespread use. Therefore, delivery systems that can retain or even enhance antimicrobial efficacy while simultaneously reducing AmB adverse events are an active area of research. Among those, lipid systems have been extensively investigated due to the high affinity of AmB for binding lipids. The development of a safe and cost-effective oral formulation able to improve drug accessibility would be a major breakthrough, and several lipid systems for the oral delivery of AmB are currently under development. This review summarizes recent advances in lipid-based systems for targeted delivery of AmB focusing on non-parenteral nanoparticulate formulations mainly investigated over the last five years and highlighting those that are currently in clinical trials.

show abstract

Section: Solid Lipid Nanoparticles and Nanostructured Lipid Carriersmentioning

confidence: 99%

Lipid Systems for the Delivery of Amphotericin B in Antifungal Therapy

2020

View full text Add to dashboard Cite

show abstract

“…The possible reason for this phenomenon could be attributed to CAT3 demonstrating higher solubility in lipids after forming OA-CAT3, and due to the stable presentation in the lipid core, ensuring less precipitate during the cooling process of the OA-CAT3-SLN formulation. However, during the cooling process of the CAT3-SLN, the free drugs cannot acquire enough solubility in lipids if not conjugated to OA, indicating that the oversaturated drugs in aqueous phase will precipitate out and crystallize, getting absorbed on the lipid surface owing to the hydrophobic nature [57]. The inconsistent location of CAT3 in the lipid core of OA-CAT3-SLN and CAT3-SLN resulted in the differences in the in vitro drug release and EE.…”

Section: Discussionmentioning

confidence: 99%

Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates

Wang

Lin

et al. 2020

Pharmaceutics

View full text Add to dashboard Cite

13a-(S)-3-pivaloyloxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (CAT3) is a novel oral anti-glioma pro-drug with a potent anti-tumor effect against temozolomide-resistant glioma in vivo. However, poor lipid solubility has limited the encapsulation efficacy during formulation development. Moreover, although the active metabolite of CAT3, 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (PF403), can penetrate the blood-brain barrier and approach the brain tissue with a 1000-fold higher anti-glioma activity than CAT3 in vitro, its bioavailability and Cmax were considerably low in plasma, limiting the anti-tumor efficacy. In this study, a novel oleic acid-CAT3 conjugate (OA-CAT3) was synthesized at the first time to increase the lipid solubility of CAT3. The OA-CAT3 loaded solid lipid nanoparticles (OA-CAT3-SLN) were constructed using an ultrasonic technique to enhance the bioavailability and Cmax of PF403 in plasma. Our results demonstrated that CAT3 was amorphous in the lipid core of OA-CAT3-SLN and the in vitro release was well controlled. Furthermore, the encapsulation efficacy and the zeta potential increased to 80.65 ± 6.79% and −26.7 ± 0.46 mV, respectively, compared to the normal CAT3 loaded SLN. As indicated by the high-performance liquid chromatography-mass spectrometry (HPLC-MS/MS) quantitation, the monolayer cellular transepithelial transport rate of OA-CAT3-SLN improved by 2.42-fold relied on cholesterol compared to the CAT3 suspension. Hence, the in vitro cell viability of OA-CAT3-SLN in C6 glioma cells decreased to 29.77% ± 2.13% and 10.75% ± 3.12% at 48 and 72 h, respectively. Finally, compared to the CAT3 suspension, the in vivo pharmacokinetics in rats indicated that the plasma bioavailability and Cmax of PF403 as afforded by OA-CAT3-SLN increased by 1.7- and 5.5-fold, respectively. Overall, the results indicate that OA-CAT3-SLN could be an efficacious delivery system in the treatment of glioma.

show abstract

“…MLN were selected because their interior vacuoles would be the most suitable carriers of Lys 37 , considering their strong hydrophilic nature 54 . SLN and NLC, despite exhibiting a lower Lys loading potential, are relatively simpler to produce and thus would be easier to produce at an industrial scale 55 . Table 3 presents the different combinations of lipids and surfactants used to prepare the nanoparticles.…”

Section: Methodsmentioning

confidence: 99%

Applying nanotechnology to increase the rumen protection of amino acids in dairy cows

Albuquerque

Casal

Páscoa

et al. 2020

Sci Rep

View full text Add to dashboard Cite

the amino acid requirements of high-production dairy cows represent a challenge to ensuring that their diet is supplied with available dietary resources, and thus supplementation with protected amino acids is necessary to increase their post-ruminal supply. Lysine is often the most limiting amino acid in cornbased diets. the present study proposes the use of lipid nanoparticles as novel rumen-bypass systems and assesses their capability to carry lysine. Solid lipid nanoparticles, nanostructured lipid carriers and multiple lipid nanoparticles were considered and their resistance in a rumen inoculum collected from fistulated cows was assessed. All nanoparticles presented diameters between 200-500 nm and surface charges lower than −30 mV. Lysine encapsulation was achieved in all nanoparticles, and its efficiency ranged from 40 to 90%. Solid lipid nanoparticles composed of arachidic or stearic acids and Tween 60 resisted ruminal digestion for up to 24 h. The nanoparticles were also proven to protect their lysine content from the ruminal microbiota. Based on our findings, the proposed nanoparticles represent promising candidates for rumen-bypass approaches and should be studied further to help improve the current technologies and overcome their limitations.

show abstract

Solid lipid nanoparticles and nanostructured lipid carriers: A review emphasizing on particle structure and drug release

Cited by 352 publications

References 274 publications

Lipid Systems for the Delivery of Amphotericin B in Antifungal Therapy

Lipid Systems for the Delivery of Amphotericin B in Antifungal Therapy

Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates

Applying nanotechnology to increase the rumen protection of amino acids in dairy cows

Contact Info

Product

Resources

About