scholarly journals Nanostructured Lipid Carriers as Promising Delivery Systems for Plant Extracts: The Case of Silymarin

2018 ◽  
Vol 8 (7) ◽  
pp. 1163 ◽  
Author(s):  
Vieri Piazzini ◽  
Beatrice Lemmi ◽  
Mario D’Ambrosio ◽  
Lorenzo Cinci ◽  
Cristina Luceri ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Physical Stability ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Water Soluble ◽  
Fluorescent Nanoparticles ◽  
Uptake Mechanism ◽  
Water Soluble Drug ◽  
Uptake Studies

Background: Silymarin is the extract from seeds of Silybum marianum L. Gaertn. and it has been used for decades as hepatoprotectant. Recently, it has been proposed to be beneficial in type 2 diabetes patients. However, silymarin is a poorly water soluble drug with limited oral bioavailability. In this study, nanostructured lipid carriers were proposed to enhance its solubility and intestinal absorption. Methods: Nanostructured lipid carriers were made of Stearic acid:Capryol 90 as lipid mixtures and Brij S20 as surfactant. Formulations were physically and chemically characterized. Stability and in vitro release studies were also assessed. In vitro permeability and Caco-2 cellular uptake mechanism were investigated. Results: Obtained results were based on size, homogeneity, ζ-potential and EE%. Nanostructured lipid carriers could be orally administered. No degradation phenomena were observed in simulated gastrointestinal fluids. Storage stability of suspensions and lyophilized products was also tested. Glucose was selected as best cryoprotectant agent. About 60% of silymarin was released in 24 h in phosphate buffered saline. In vitro parallel artificial membrane permeability assay experiments revealed that the nanocarrier enhanced the permeation of Silymarin. Caco-2 study performed with fluorescent nanoparticles revealed the ability of carrier to enhance the permeation of a lipophilic probe. Cellular uptake studies indicated that active process is involved in the internalization of the formulation. Conclusions: The optimized nanostructured lipid carriers showed excellent chemical and physical stability and enhanced the absorption of silymarin.

scholarly journals Study on the influence of technological factors on drug loading of poorly water-soluble drug on MCM-41 mesoporous carrier

Pharmacia ◽  
2020 ◽  
Vol 67 (4) ◽  
pp. 351-356
Author(s):  
Teodora Popova ◽  
Christina Voycheva ◽  
Borislav Tzankov
Keyword(s):  
Loading Rate ◽  
Drug Loading ◽  
In Vitro Release ◽  
Water Soluble ◽  
Technological Factors ◽  
Loading Process ◽  
Water Soluble Drug ◽  
Vitro Release ◽  
Mcm 41

The present study explored solvent impregnation drug loading process of the poorly soluble non-steroid anti-inflammatory drug indomethacin on MCM-41 type mesoporous silica carrier. Different technological factors that can influence drug-loading process as time of reaction, temperature, use of non-solvent as well as different ratios between drug and MCM-41 were studied. TEM and DLS were used to characterize physicochemical properties of obtained particles. The influence of drug-loading rate on dissolution process were studied using in-vitro release tests. Our results established that changes in explored technological factors could lead to different indomethacin loading. Moreover, the in-vitro release tests proved that drug loading rate had a direct influence on indomethacin release from MCM-41 particles. Our finding suggested that by tuning the main technological factors it would be possible different drug delivery systems with different drug loading rate to be obtained.

Nanostructured-lipid carriers-Chitosan hydrogel beads carrier system for loading of resveratrol: A new method of topical application

2022 ◽  
pp. 088532822110539
Author(s):  
Bi Wu ◽  
Yang Li ◽  
Yuan Y Li ◽  
Zhi H Shi ◽  
Xiao H Bian ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Physical Stability ◽  
In Vitro Release ◽  
In Vitro Cytotoxicity ◽  
Nanostructured Lipid Carriers ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Chitosan Hydrogel ◽  
Hydrogel Beads

The aim of this study was to develop nanostructured-lipid carriers (NLC) encapsulated by Chitosan hydrogel beads for the efficient topical carrier. Dynamic light scattering (DLS), X-ray diffraction (XRD), Differential scanning calorimetry (DSC), and attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) were conducted to study the influence of the encapsulation on the characteristic of resveratrol-loaded NLC, and the results showed that there was no impact on resveratrol-loaded NLC. Chitosan hydrogel beads could significantly improve the physical stability of resveratrol-loaded NLC. In vitro release study revealed that resveratrol-loaded NLC-Chitosan hydrogel beads had a more significant sustained-release effect on resveratrol. In vitro transdermal studies suggested that the skin permeation of resveratrol was promoted by the effect of Chitosan hydrogel beads and increased resveratrol distribution in the skin. In vitro cytotoxicity showed that resveratrol-loaded NLC-Chitosan hydrogel beads did not exert a hazardous effect on L929 cells. Hence, NLC-Chitosan hydrogel beads might be a promising method for topical applications of resveratrol.

Inclusion Complex Formation of Water- Soluble Drug, Captopril, and Peracetylated-β-Cyclodextrin in Supercritical CO2 for Controlled Release Applications

2007 ◽  
Vol 342-343 ◽  
pp. 489-492 ◽  
Author(s):  
Hullathy Subban Ganapathy ◽  
Min Hee Woo ◽  
Yeong Soon Gal ◽  
Kwon Taek Lim
Keyword(s):  
Carbon Dioxide ◽  
Inclusion Complex ◽  
In Vitro Release ◽  
Water Soluble ◽  
Inclusion Complex Formation ◽  
Hydrophobic Properties ◽  
Water Soluble Drug ◽  
Xrd Studies ◽  
Vitro Release

The inclusion complex of CO2-soluble peracetylated-β-cyclodextrin (PAc-β- CD), heptakis(2,3,6-tri-O-acetyl)-β-cyclodextrin, and highly water-soluble drug captopril, was prepared by a chemical solvent-free method using supercritical carbon dioxide. The captopril-PAc-β-CD inclusion complex was further confirmed by DSC and XRD studies. In- vitro release of captopril from an oily suspension confirmed that the dissolution rate of captopril was much retarded from the inclusion complex as a result of the hydrophobic properties of PAc-β-CD.

Hydrophobically Modified Amphiphilic Cylodextrins as Novel Carriers for Controlled Delivery of Water-Soluble Drugs

2007 ◽  
Vol 342-343 ◽  
pp. 493-496 ◽  
Author(s):  
Hullathy Subban Ganapathy ◽  
Min Young Lee ◽  
Min Hee Woo ◽  
Yeong Tae Jeong ◽  
Kwon Taek Lim
Keyword(s):  
In Vitro Release ◽  
Ester Group ◽  
Water Soluble ◽  
Controlled Delivery ◽  
Hydrophobically Modified ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Vitro Release ◽  
Potential Use

Hydrophobically modified derivative of a γ-cyclodextrin, functionalized with perfluoro alkyl ester group, was prepared and investigated for its potential use as a sustained release carrier for water-soluble drug molsidomine, a peripheral nitrovasodilator used in the treatment of angina pectoris. The molecular encapsulation of molsidomine by the amphiphilic cyclodextrin, octakis(6-O-perfluorobutanoyl)-γ-cyclodextrin (γ-CyD-F), was confirmed by DSC and XRD studies. The in-vitro release of molsidomine from peanut oil suspensions into aqueous phase was found to be significantly retarded by the complexation with γ-CyD-F, mainly due to the hydrophobic properties of the γ-CyD-F.

scholarly journals Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release

Polymers ◽  
2021 ◽  
Vol 13 (18) ◽  
pp. 3158
Author(s):  
Raissa Lohanna Gomes Quintino Corrêa ◽  
Renan dos Santos ◽  
Lindomar José Calumby Albuquerque ◽  
Gabriel Lima Barros de Araujo ◽  
Charlotte Jennifer Chante Edwards-Gayle ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Polymeric Nanoparticles ◽  
Substantial Reduction ◽  
In Vitro Release ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Pluronic P123 ◽  
Water Soluble Drug ◽  
Vis Spectroscopy

Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties lacking. In parallel, recent studies have led to the improvement of drug administration, including encapsulation in polymeric nanoparticles (NPs). Here, we present CIP’s crystal structure determined by PDRX data. We also propose an encapsulation method for CIP in micelles produced from Pluronic P123/F127 and PEO-b-PCL, aiming to improve its solubility, hydrophilicity, and delivery. We determined the NPs’ physicochemical properties by DLS, SLS, ELS, and SAXS and the loaded drug amount by UV-Vis spectroscopy. Micelles showed sizes around 10–20 nm for Pluronic and 35–45 nm for the PEO-b-PCL NPs with slightly negative surface charge and successful CIP loading, especially for the latter; a substantial reduction in ζ-potential may be evidenced. For Pluronic nanoparticles, we scanned different conditions for the CIP loading, and its encapsulation efficiency was reduced while the drug content increased in the nanoprecipitation protocol. We also performed in vitro release experiments; results demonstrate that probe release is driven by Fickian diffusion for the Pluronic NPs and a zero-order model for PEO-b-PCL NPs.

Multiple Unit Asymmetric Membrane Capsule: A Means for Delivery of Highly Water Soluble Drug

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Harmeet Singh ◽  
Anil Philip ◽  
Kamla Pathak
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Asymmetric Membrane ◽  
Porous Region ◽  
Water Soluble Drug ◽  
Multiple Unit ◽  
Coating Formulation

A multiple unit, non-disintegrating asymmetric polymeric capsular system was used to deliver highly water-soluble drug in a controlled manner. A highly water-soluble drug, metformin hydrochloride (MHCl), was selected as a model drug to demonstrate how the controlled release could be generated in vitro by changes in the core as well as the coating formulation. Formation of asymmetric capsule wall membrane involved wet phase inversion process, in which the asymmetric membrane (AM) was precipitated on glass mold pins by dipping the mold pins into a coating solution containing the good and bad solvents for the polymer followed by quenching in an aqueous quench bath. The study optimized by 23 factorial design evaluates the influence of coating formulation namely concentration of ethylcellulose and pore former (glycerol) and core component namely controlled release potassium chloride crystals. Scanning Electron Microscopy (SEM) showed the presence of outer dense non porous region and inner, thick, porous region for the prepared AM. Statistical test were applied at P > 0.05 on all the formulations undergoing in vitro release studies. Results showed the solubility of MHCl to have been modulated (reduced) over an extended period of time with pH independent, and osmotic pressure dependant drug release. The release kinetics was found to be zero order.

Solid Lipid Nanoparticles and Chitosan-coated Solid Lipid Nanoparticles as Promising Tool for Silybin Delivery: Formulation, Characterization, and In vitro Evaluation

2018 ◽  
Vol 16 (2) ◽  
pp. 142-152 ◽  
Author(s):  
Vieri Piazzini ◽  
Lorenzo Cinci ◽  
Mario D'Ambrosio ◽  
Cristina Luceri ◽  
Anna Rita Bilia ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Solid Lipid Nanoparticles ◽  
Cell Monolayer ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Burst Release ◽  
Solid Lipid ◽  
Vitro Release

Background: Silybin (Sb) is the major flavolignan of the extract of Silybum marianum. It is used for the treatment of various acute and chronic liver toxicities, inflammation, fibrosis and oxidative stress. Many studies indicate that Sb is also active against different carcinomas and it has been very recently proposed to be beneficial in type 2 diabetes patients. However, Sb is a low water soluble and low permeable compound. Objective: In this study, Solid Lipid Nanoparticles (SLNs) were proposed to enhance the solubility and the intestinal absorption of Sb. </P><P> Methods: SLNs were made of stearic acid and Brij 78 and subsequently coated with chitosan. Formulations were physically and chemically characterized. Stability studies were also assessed. Sb in vitro release was evaluated in different pH media. In vitro permeability test with artificial membranes and Caco-2 cells were performed. Cellular uptake and mucoadhesion studies were conducted. Results: Both nanoparticles were found to be stable. In vitro release indicated that SLNs may prevent burst release and gastric degradation of Sb. Higher extent of Sb permeation was observed for both nanoparticles in PAMPA and Caco-2 cell monolayer models. The results of the cellular uptake study suggested the involvement of active endocytic processes. Chitosan significantly improves mucoadhesion properties of nanoparticles. </P><P> Conclusions: Together with the excellent stability, strong mucoadhesive property, and slow release, chitosan coated SLNs demonstrated promising potential to enhance absorption of hydrophobic Sb after oral administration.

scholarly journals Freeze-Dried Lopinavir-Loaded Nanostructured Lipid Carriers for Enhanced Cellular Uptake and Bioavailability: Statistical Optimization, in Vitro and in Vivo Evaluations

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 97 ◽  
Author(s):  
Arshad Khan ◽  
Jahanzeb Mudassir ◽  
Safia Akhtar ◽  
Vikneswaran Murugaiyah ◽  
Yusrida Darwis
Keyword(s):  
Cellular Uptake ◽  
Chemical Interaction ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Simulated Gastric Fluid ◽  
Burst Release ◽  
Simulated Intestinal Fluid ◽  
Differential Scanning Calorimetry Study ◽  
Freeze Dried

Nanostructured lipid carriers (NLCs) loaded with lopinavir (LPV) were prepared by the high-shear homogenization method. The LPV-NLCs formulations were freeze-dried using trehalose as a cryoprotectant. In vitro release studies in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8) showed a burst release. The optimized freeze-dried formulation (LPV-NLC-7-Tres) had a particle size (PS), polydispersity index (PdI), zeta potential (ZP) and % entrapment efficiency (%EE) of 286.8 ± 1.3 nm, 0.413 ± 0.017, −48.6 ± 0.89 mV and 88.31 ± 2.04%, respectively. The optimized formulation observed by transmission and scanning electron microscopes showed a spherical shape. Differential scanning calorimetry study revealed the absence of chemical interaction between the drug and lipids. In vitro cellular uptake study using Caco-2 cell line showed a higher LPV uptake from LPV-NLC-7-Tres formulation compared to the free LPV-suspension. The 6-month stability study showed a minimum rise of ~40 nm in PS, while no significant changes in PdI, ZP and drug content of the LPV-NLC-7-Tres formulation stored at 5 °C ± 3 °C. The bioavailability of LPV following oral administration of LPV-NLC-7-Tres in male Wistar rats was found 6.98-fold higher than the LPV-suspension. In conclusion, the nanostructure lipid carriers are potential carriers for improving the oral bioavailability of lopinavir.

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