scholarly journals Differential Scanning Calorimetry Analyses of Idebenone-Loaded Solid Lipid Nanoparticles Interactions with a Model of Bio-Membrane: A Comparison with In Vitro Skin Permeation Data

2018 ◽  
Vol 11 (4) ◽  
pp. 138 ◽  
Author(s):  
Lucia Montenegro ◽  
Francesco Castelli ◽  
Maria Sarpietro
Keyword(s):  
Differential Scanning Calorimetry ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Enthalpy Changes ◽  
In Vitro Skin Permeation ◽  
The Difference ◽  
Penetration Data

Differential scanning calorimetry (DSC) has emerged as a helpful technique both to characterize drug delivery systems and to study their interactions with bio-membranes. In this work, we compared idebenone (IDE)-loaded solid lipid nanoparticle (SLN) interactions with bio-membranes assessed by DSC with previous in vitro skin penetration data to evaluate the feasibility of predicting IDE skin penetration using DSC analyses. In vitro interactions experiments were performed using multi-lamellar liposomes as a model of bio-membrane. Enthalpy changes (ΔH) and transition temperature (Tm) were assessed during nine repeated DSC scans to evaluate IDE-loaded SLN–bio-membrane interactions over time. Analyzing ΔH and Tm values for each scan, we observed that the difference of ΔH and Tm values between the first and the last scan seemed to be related to SLN ability to locate IDE in the epidermis and in the stratum corneum, respectively. Therefore, the results of this study suggest the possibility of qualitatively predicting in vitro IDE skin penetration from IDE-loaded SLN utilizing the calorimetric parameters obtained from interaction experiments between the carriers under investigation and a model of bio-membrane.

Avobenzone encapsulated in modified dextrin for improved UV protection and reduced skin penetration

2016 ◽  
Vol 70 (6) ◽  
Author(s):  
Chia-Ching Li ◽  
Li-Huei Lin ◽  
Hsun-Tsing Lee ◽  
Jing-Ru Tsai
Keyword(s):  
Differential Scanning Calorimetry ◽  
Thermogravimetric Analysis ◽  
Inclusion Complexes ◽  
Skin Penetration ◽  
Uv Protection ◽  
Skin Damage ◽  
Protection Factor ◽  
Scanning Calorimetry ◽  
Uv Filter

AbstractThe present study used differential scanning calorimetry, thermogravimetric analysis, and UV spectrometry to examine: i) the encapsulation of an organic UV filter 1-(4-methoxyphenyl)-3-(4-tert-butylphenyl)propane-1,3-dione (avobenzone) within modified dextrin and ii) the characteristics of these inclusion complexes (MDA). The properties of avobenzone emulsions with and without encapsulation in modified dextrin, the in vitro UV protection factor, dissolution and release, and the skin penetrability of avobenzone were also examined. The presence of inclusion complexes significantly decreased the tendency of the UV filter to penetrate the skin. In addition, such inclusion complexes should effectively prevent skin damage from radiation extending from the UVA to the UVC.

scholarly journals Improved photostability, reduced skin permeation and irritation of isotretinoin by solid lipid nanoparticles / Povećana fotostabilnost, smanjena permeacija i iritacija izotretinoina iz kruto-tekućih nanočestica

2012 ◽  
Vol 62 (4) ◽  
pp. 547-562 ◽  
Author(s):  
Golmohammadzadeh Shiva ◽  
Mortezania Somaye ◽  
Jaafari Mahmoud Reza
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Skin Permeation ◽  
Mouse Skin ◽  
Morphological Characteristics ◽  
Average Diameter ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Scanning Calorimetry ◽  
Solid Lipid

The aim of this study was to develop new solid lipid nanoparticles of isotretinoin (IT-SLNs) and evaluate the ability of IT-SLNs to improve photostability, reduce skin permeation and irritating effects. IT-SLNs were prepared by the hot high pressure homogenization method. Size, zeta potential and morphological characteristics of the preparations were assessed by transmission electron microscopy (TEM) and thermotropic properties with differential scanning calorimetry (DSC). IT-SLNs had a small average diameter of 74.05 ± 8.91 nm and high encapsulation efficiency (EE) of 80.6 ± 1.2 %. The results showed that the entrapment of IT into SLNs reduced significantly its photodegradation. The in vitro permeation data showed that IT-SLNs can accumulate in the different layers of the skin and prevent systemic uptake of IT in mouse skin. IT-SLNs also significantly increased IT accumulation in the different layers of the stratum corneum of human skin. IT-SLN formulation was significantly less irritating compared to commercial IT-GEL, which shows its potential for improving skin tolerability and being a carrier for topical delivery of IT.

scholarly journals Influence of ceramide 2 on in vitro skin permeation and retention of 5-ALA and its ester derivatives, for Photodynamic Therapy

2009 ◽  
Vol 45 (1) ◽  
pp. 109-116 ◽  
Author(s):  
Maria Bernadete Riemma Pierre ◽  
Renata Fonseca Vianna Lopez ◽  
Maria Vitória Lopes Badra Bentley
Keyword(s):  
Photodynamic Therapy ◽  
Aminolevulinic Acid ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Drug Formulation ◽  
Interesting Approach ◽  
In Vitro Skin Permeation ◽  
Cutaneous Delivery ◽  
Endogenous Precursor

Photodynamic therapy (PDT) based on topical 5-aminolevulinic acid (5-ALA), an endogenous precursor of protoporphyrin, is an interesting approach for the treatment of skin cancer. However, 5-ALA is a hydrophilic molecule and such a characteristic limits its appropriate cutaneous penetration and retention. In this way, more lipophilic molecules, such as esterified 5-ALA derivatives, have been under investigation in order to improve the skin penetration of this molecule. Drug formulation can also alter 5-ALA skin penetration. Therefore, the aim of this work was to study the influence of ceramide 2 - the main lipid of the SC- on the cutaneous delivery of 5-ALA and its ester derivatives in vitro, using Franz diffusion cell. The skin permeation of all studied drugs was decreased in the presence of ceramide, representing a desirable characteristic in order to avoid the risk of systemic side effects. Nevertheless, the SC and [epidermis + dermis] retention after 16 h has also been decreased in the presence of ceramide, as compared to control. In conclusion, ceramide was not a good adjuvant, meaning that research of other vehicles could be useful to improve cutaneous delivery of 5-ALA.

Effect of Edge Activator on Characteristic and in Vitro Skin Permeation of Meloxicam Loaded in Elastic Liposomes

2011 ◽  
Vol 194-196 ◽  
pp. 537-540 ◽  
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Cetylpyridinium Chloride ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Transdermal Drug Delivery System ◽  
Scanning Calorimetry ◽  
In Vitro Skin Permeation

The aim of this study was to prepare and investigate the potential use of liposomes in the transdermal drug delivery of meloxicam (MX). The vesicles containing a constant amount of MX, phosphatidylcholine (PC), cholesterol (Chol) and cetylpyridinium chloride (CPC) (1:5:1:1 MX/PC/Chol/CPC molar ratio) to obtain liposomes. MX loaded liposomes were investigated for particle size, zeta potential, entrapment efficiency (%EE) and in vitro skin permeation. The results indicated that the liposomes were spherical in structure, 77 to 100 nm in size and charged. The %EE of MX in the vesicles ranged from 55 to 56%. The elastic liposomes consisting of MX/PC/Chol/CPC provided a significantly higher skin permeation of MX compared to the other formulations. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analysis indicated that the application of liposomes may disrupt the stratum corneum lipid. Our research suggests that MX loaded elastic liposomes can be potentially used as a transdermal drug delivery system.

scholarly journals Characterization and In Vitro Skin Permeation of Meloxicam-Loaded Liposomes versus Transfersomes

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Transdermal Drug Delivery System ◽  
Scanning Calorimetry ◽  
Stratum Corneum Lipid ◽  
In Vitro Skin Permeation ◽  
Ft Ir

The goal of this study was to develop and evaluate the potential use of liposome and transfersome vesicles in the transdermal drug delivery of meloxicam (MX). MX-loaded vesicles were prepared and evaluated for particle size, zeta potential, entrapment efficiency (%EE), loading efficiency, stability, and in vitro skin permeation. The vesicles were spherical in structure, 90 to 140 nm in size, and negatively charged ( to  mV). The %EE of MX in the vesicles ranged from 40 to 70%. Transfersomes provided a significantly higher skin permeation of MX compared to liposomes. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analysis indicated that the application of transfersomes significantly disrupted the stratum corneum lipid. Our research suggests that MX-loaded transfersomes can be potentially used as a transdermal drug delivery system.

scholarly journals In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1027
Author(s):  
Lucia Montenegro ◽  
Ludovica Maria Santagati ◽  
Maria Grazia Sarpietro ◽  
Francesco Castelli ◽  
Annamaria Panico ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Skin Penetration ◽  
Lipid Nanoparticles ◽  
Penetration Enhancers ◽  
Isopropyl Myristate ◽  
Skin Delivery ◽  
Rate Limiting Step ◽  
In Vitro Skin Permeation ◽  
Chemical Penetration Enhancers

Lipid nanoparticles (LNPs) have been proposed as carriers for drug skin delivery and targeting. As LNPs effectiveness could be increased by the addition of chemical penetration enhancers (PE), in this work, the feasibility of incorporating PE into LNPs to improve idebenone (IDE) targeting to the skin was investigated. LNPs loading IDE 0.7% w/w were prepared using hydrophilic (propylene glycol, PG, 10% w/w or N-methylpyrrolidone, NMP, 10% w/w) and/or lipophilic PE (oleic acid, OA, 1% w/w; isopropyl myristate, IPM, 3.5% w/w; a mixture of 0.5% w/w OA and 2.5% w/w IPM). All LNPs showed small sizes (<60 nm), low polydispersity index and good stability. According to the obtained results, IDE release from LNPs was not the rate-limiting step in IDE skin penetration. No IDE permeation was observed through excised pigskin from all LNPs, while the greatest increase of IDE penetration into the different skin layers was obtained using the mixture OA/IPM. The antioxidant activity of IDE-loaded LNPs, determined by the oxygen radical absorbance capacity assay, was greater than that of free IDE. These results suggest that the use of suitable PE as LNPs components could be regarded as a promising strategy to improve drug targeting to the skin.

Transdermal Delivery of Metoprolol II: In-Vitro Skin Permeation and Bioavailability in Hairless Rats

1995 ◽  
Vol 84 (2) ◽  
pp. 158-160 ◽  
Author(s):  
Tapash K. Ghosh ◽  
Joseph Adir ◽  
Si‐Ling Xiang ◽  
Samuel Onyilofur
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
In Vitro Skin Permeation

Mannosylated Solid Lipid Nanocarriers Of Chrysin To Target Gastric Cancer: Optimization and Cell line Study.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sonia S. Pandey ◽  
Farhinbanu I. Shaikh ◽  
Arti R. Gupta ◽  
Rutvi J. Vaidya
Keyword(s):  
Gastric Cancer ◽  
Particle Size ◽  
Ex Vivo ◽  
Biological Effects ◽  
Entrapment Efficiency ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Lipid Nanocarriers

Background: Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability. Objective: The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer. Methods: The Chrysin loaded SLNs (C-SLNs) were developed optimized, characterized and further mannosylated. The C-SLNs were developed with high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines. Results: DSC and XRD data predict the chrysin encapsulation in lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in dependent variable - increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs. Conclusion: These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat the gastric cancer.

In vitro skin permeation of hinokitiol loaded in vesicles composed of behenyltrimethylammonium chloride and stearic acid

2010 ◽  
Vol 36 (5) ◽  
pp. 556-562 ◽  
Author(s):  
Xia Yang ◽  
Hyeon Yong Lee ◽  
Jin-Chul Kim
Keyword(s):  
Stearic Acid ◽  
Skin Permeation ◽  
In Vitro Skin Permeation

scholarly journals In Vitro Skin Permeation of Morphine Hydrochloride during the Finite Application of Penetration-Enhancing System Containing Water, Ethanol and l-Menthol

2002 ◽  
Vol 25 (1) ◽  
pp. 134-136 ◽  
Author(s):  
Yasunori Morimoto ◽  
Yoshio Wada ◽  
Toshinobu Seki ◽  
Kenji Sugibayashi
Keyword(s):  
Skin Permeation ◽  
In Vitro Skin Permeation ◽  
Morphine Hydrochloride
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