Nanostructured Lipid Carriers Can Enhance Oral Absorption of Khellin, a Natural Pleiotropic Molecule

Vanti, Giulia; Muti, Lucrezia; D’Ambrosio, Mario; Grifoni, Lucia; Bergonzi, Maria Camilla; Luceri, Cristina; Bilia, Anna Rita

doi:10.3390/molecules26247657

Cited by 6 publications

(7 citation statements)

References 40 publications

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“…The samples were analyzed by dynamic and electrophoretic light scattering (DLS and ELS) to evaluate the average particle size, PdI and Z-potential of the NLCs and CBD-loaded NLCs, which resulted in them being suitable for oral administration [35] (Table 1). NLC dimensions after CBD loading increased slightly but without any significance, as reported by other studies [29]. PdI of both formulations was less than 0.3, indicating worthy sample homogeneity.…”

Section: Physical and Chemical Characterization Of Nlcs And Cbd-loade...supporting

confidence: 80%

“…Fixed amounts of Poloxamer 188, Lauroglycol 90, Tween 20 and Labrafil M 2125 were set as 0.50% or 1.05% w/v, while Compritol 888 ATO was investigated in the range between 2.5 and 3.0% w/v. NLCs were prepared using the emulsification-ultrasonication method, as previously reported [29].…”

Section: Preparation Of Nlcs and Optimization Of Cbd-loaded Nlcsmentioning

confidence: 99%

“…The stability of CBD-NLC, in terms of CBD recovery (R%), size and PdI of nanoparticles, was evaluated in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) by using 50 folds dilution [29]. Briefly, the composition of SGF was 3.2 g of pepsin, 2.0 g of NaCl and 7 mL HCl dissolved in 1 L of ultrapure water (pH adjusted to 2.0 using 1 M NaOH).…”

Section: Studies Of Cbd-nlc Stability In Gastric and Intestinal Simul...mentioning

confidence: 99%

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Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine

2023

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The purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instability in simulated physiological conditions and in the acidic media, which results in a very low bioavailability—less than 6%. NLCs containing CBD (10 mg/mL), Compritol 888 ATO, Lauroglycol 90, Labrafil 2125, Tween 20, and Poloxamer 188 were formulated. This resulted in them being suitable for oral administration because the size was less than 200 nm, polydispersity index 0.152, and ζ-potential −39.21 ± 1.89 mV. Recovery and encapsulation efficiency were 100% and 93%, respectively. After two hours of incubation in simulated gastric fluid (SGF), NLCs remained unchanged, protecting CBD from acidic medium. Indeed, CBD is also reported to be not stable in media with pH = 7.4 at 37 °C, but our studies evidenced that in the presence of the intestinal fluid, the NLC was digested and formed an emulsion, which can protect and preserve the CBD chemical structure, as confirmed by the 100% recovery found after six hours. Accordingly, CBD-loaded NLCs are a promising oral formulation that optimize bioaccessibility in the small intestine.

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Section: Physical and Chemical Characterization Of Nlcs And Cbd-loade...supporting

confidence: 80%

Section: Preparation Of Nlcs and Optimization Of Cbd-loaded Nlcsmentioning

confidence: 99%

Section: Studies Of Cbd-nlc Stability In Gastric and Intestinal Simul...mentioning

confidence: 99%

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Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine

2023

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“…Chemical characterization of escinosomes was carried out by determining the encapsulation efficiency (EE%) and total recovery (R%) of AG and ESN. In order to measure EE%, the not encapsulated drug was removed by the dialysis bag method, performed using Spectra/Por ® regenerated cellulose membranes, with 12–14 kDa molecular weight cut-off, by Repligen Europe B.V. (Breda, The Netherlands) [ 13 ]. The dialysis bag, filled with 1 mL of formulation, was immersed in 1 L of ultrapure water at 25 ± 1 °C and kept under magnetic stirring at 100 rpm for 1 h. Then, the purified formulation was diluted 20 times in methanol to break up the escinosomes and solubilize the active substances.…”

Section: Methodsmentioning

confidence: 99%

Escinosomes: Safe and Successful Nanovesicles to Deliver Andrographolide by a Subcutaneous Route in a Mice Model of Oxaliplatin-Induced Neuropathy

et al. 2022

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Andrographolide (AG) is a natural diterpene lactone endowed with considerable therapeutic potential for treating numerous diseases, including neurological disorders, but its low aqueous solubility and scarce bioavailability limit its clinical use. To overcome this problem, AG was encapsulated in escinosomes, special nanovesicles made of escin (ESN), a natural saponin, and phosphatidylcholine. Escinosomes loaded with AG had an average size of 164.7 ± 13.30 nm, optimal polydispersity index (0.190 ± 0.0890) and high ζ-potential (−35.4 ± 0.451 mV), and significantly loaded the active substance—the encapsulation efficiency of AG was about 88%. Escinosomes allowed the prolonged release of AG over time, without burst effects—about 85% AG was released after 24 h. Morphological analysis by cryo-transmission electron microscopy showed nanovesicles with a spherical shape, unilamellar and oligolamellar structures, and dimensions in agreement with those measured by dynamic light scattering. In addition, stability studies were performed on AG-loaded escinosomes stored for one month at 4 °C. The pain-relieving efficacy of these nanovesicles was tested in a rat model of oxaliplatin-induced neuropathy. AG-loaded escinosomes, subcutaneously administered, effectively reduced the thermal allodynia characteristic of chemotherapy-induced neuropathy, enhancing and prolonging the effect of the natural compound. Overall, AG-loaded escinosomes were found to be excellent for loading AG, physically and chemically stable for one-month storage, and with controlled-release properties, making the formulation an ideal pharmacological approach for persistent pain treatment.

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“…The implementation of NLC offers several advantages, including improved absorption capacity, enhanced stability, and reduced reliance on surfactant components [ 15 , 16 ]. With the utilization of NLC, a diverse range of components can be incorporated, extending beyond the mere absorption of active compounds [ 17 ]. By harnessing the advantages offered by NLC, researchers can explore novel formulations and optimize the delivery of lipophilic drugs, ultimately enhancing their therapeutic efficacy.…”

Section: Introductionmentioning

confidence: 99%

Propolis-Based Nanostructured Lipid Carriers for α-Mangostin Delivery: Formulation, Characterization, and In Vitro Antioxidant Activity Evaluation

et al. 2023

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α-Mangostin (a xanthone derivative found in the pericarp of Garcinia mangostana L.) and propolis extract (which is rich in flavonoids and phenols) are known for their antioxidant properties, making them potential supplements for the treatment of oxidative stress-related conditions. However, these two potential substances have the same primary drawback, which is low solubility in water. The low water solubility of α-mangostin and propolis can be overcome by utilizing nanotechnology approaches. In this study, a propolis-based nanostructured lipid carrier (NLC) system was formulated to enhance the delivery of α-mangostin. The aim of this study was to characterize the formulation and investigate its influence on the antioxidant activity of α-mangostin. The results showed that both unloaded propolis-based NLC (NLC-P) and α-mangostin-loaded propolis-based NLC (NLC-P-α-M) had nanoscale particle sizes (72.7 ± 1.082 nm and 80.3 ± 1.015 nm, respectively), neutral surface zeta potential (ranging between +10 mV and −10 mV), and good particle size distribution (indicated by a polydispersity index of <0.3). The NLC-P-α-M exhibited good entrapment efficiency of 87.972 ± 0.246%. Dissolution testing indicated a ~13-fold increase in the solubility of α-mangostin compared to α-mangostin powder alone. The incorporation into the propolis-based NLC system correlated well with the enhanced antioxidant activity of α-mangostin (p < 0.01) compared to NLC-P and α-mangostin alone. Therefore, the modification of the delivery system by incorporating α-mangostin into the propolis-based NLC overcomes the physicochemical challenges of α-mangostin while enhancing its antioxidant effectiveness.

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Nanostructured Lipid Carriers Can Enhance Oral Absorption of Khellin, a Natural Pleiotropic Molecule

Cited by 6 publications

References 40 publications

Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine

Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine

Escinosomes: Safe and Successful Nanovesicles to Deliver Andrographolide by a Subcutaneous Route in a Mice Model of Oxaliplatin-Induced Neuropathy

Propolis-Based Nanostructured Lipid Carriers for α-Mangostin Delivery: Formulation, Characterization, and In Vitro Antioxidant Activity Evaluation

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