Influence of chemical and structural features of low molecular weight heparins (LMWHs) on skin penetration

Franzè, Silvia; Gennari, C.; Minghetti, Paola; Cilurzo, Francesco

doi:10.1016/j.ijpharm.2015.02.001

Cited by 17 publications

(23 citation statements)

References 22 publications

(24 reference statements)

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“…34 Franze et al proposed that the low molecular weight heparins exhibit different skin permeability properties. 35 However, the previous study showed that ceftriaxone is undetectable in the in vitro model. We suggested that ceftriaxone was delivered from blood to the tissues by passive diffusion.…”

Section: Resultsmentioning

confidence: 99%

In vitro Penetration and in vivo Distribution of Honokiol into the Intervertebral Disc in Rat

Chen

Chiang

et al. 2015

ANAL. SCI.

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Honokiol is a potential candidate for the treatment of intervertebral disc (IVD) degeneration. In this study, we develop in vitro and in vivo methods to detect the distribution of honokiol in intervertebral discs using high-performance liquid chromatography. A rat tail disc was used for both experimental models. For the in vivo animal experiment, blood samples and tail discs were collected at 15, 30, 60, 120 and 240 min after honokiol administration (30 mg/kg, i.v.). The analyte was separated by a mobile phase of methanol and 10 mM NaH2PO4 buffer at pH 2.8 (78:22, v/v) and pumped through a reversed-phase analytical column (250 × 4.6 mm, particle size 5 μm) at room temperature. The in vitro experimental results demonstrated that honokiol diffused into the intervertebral disc and was concentration-dependent. The active concentration is obtained for the therapeutic level at 15 and 30 min after honokiol administration in the in vivo model.

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Section: Resultsmentioning

confidence: 99%

In vitro Penetration and in vivo Distribution of Honokiol into the Intervertebral Disc in Rat

Chen

Chiang

et al. 2015

ANAL. SCI.

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“…Epidermis sheets were obtained through mechanical separation from the remaining tissue with forceps after skin immersion in water at 60 ± 1 °C for 1 min. Prior to the experiment, the integrity of the epidermis samples was assessed by measuring the electrical impedance using a voltage of 100 mV and a frequency of 100 Hz (Agilent 4263B LCR Meter, Microlease, Italy) …”

Section: Methodsmentioning

confidence: 99%

Rationalizing the Design of Hyaluronic Acid-Decorated Liposomes for Targeting Epidermal Layers: A Combination of Molecular Dynamics and Experimental Evidence

et al. 2021

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This work provides information on the features of low molecular weight hyaluronic acid (HA)-decorated liposomes to target resveratrol (RSV) in the skin. Deformable liposomes were made of soy-phosphatidylcholine with Tween 80 as the fluidizing agent. For HA conjugation, three different phosphoethanolamines were tested: 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE), 1,2-dimyristoyl-sn-glycero-3-phosphoethanolamine (DMPE), and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE). The different phosphoethanolamine-HA conjugates were inserted into the liposome bilayer by hydration (HA on both faces of the bilayer) or by the postinsertion method (HA only on the external face of the bilayer). The effect of these variables on deformability was experimentally assessed by an in-house method (K value, the lower the value, the higher the deformability) and molecular dynamics (MD) simulations. The results showed that the K values of HA-liposomes obtained by hydration were higher than the K values of HA-liposomes prepared by postinsertion, and both were at least 10-fold higher than the K values of the corresponding plain liposomes. The nature of the lipid anchor played a key role in deformability (DMPE > DOPE > DPPE) with high variability in the case of DOPE formulations. These data were justified by the trends found in silico for the bilayer bending modulus and the HA end-to-end distance. In addition to liposome flexibility, the HA extent seems to be the key factor governing the skin penetration of RSV. When the extent is higher, the amount of the drug retained in the skin is larger. Regarding skin permeation, a parabolic trend was recorded, and the optimal amount to favor skin permeation was an approximately 30 HA/phospholipid (μg/ mmol) ratio. This study reports the first piece of evidence that it is possible to control drug delivery in the skin by tuning the amount of HA on the vesicle surface.

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“…Human stratum corneum isolation -The permeation studies were performed using the abdominal 95 skin from female donors, who underwent cosmetic surgery and signed an informed consent for the use of the biological sample for research purposes (Franzè et al, 2015). After removing the subcutaneous fatty tissue, the skin was kept frozen until further use.…”

Section: Mechanical Testingmentioning

confidence: 99%

A glimpse in critical attributes to design cutaneous film forming systems based on ammonium methacrylate

Gennari

Selmin

Franzè

et al. 2017

Journal of Drug Delivery Science and Technology

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A film forming system based on Eudragit ® RL (EuRL) was designed aiming to evidence the relevance of formulative variables on the following critical attributes: film forming rate, outward stickiness, Young modulus (Y) and in vitro drug skin permeation. Different solvent mixtures (acetone and isopropanol in the range from 10:90 to 40:60 v/v), polymer concentrations (10-30 % w/w), and plasticizer types and concentrations (triacetin or tributyl citrate, up to 50% of EuRL) 15 were evaluated. EuRL dissolved in 80/20 or 70/30 v/v isopropanol/acetone mixtures at the concentration of 20% and plasticized with tributyl citrate (20 or 30% with respect to polymer) gave films with negligible stickiness and Y lower than 3 MPa. This value should assure an intimate and prolonged contact with the skin since it was significantly lower than Y of human stratum corneum (55 MPa). The optimized formulations were able to sustain the skin permeation of ibubrofen, 20 25 30 Keywords:Eudragit RL, film forming system, skin elasticity, skin permeation, supersaturation 30 RL (EuRL) when it was compared to another widely used film forming material, namely hydroxyethyl cellulose. As an example, the skin permeability of estradiol from EuRL based films resulted significantly lower than that obtained with the cellulose ether (Zurdo Schroeder et al., 2006). Nevertheless, the use of EuRL allowed to overcome the mechanical issues associated to 65 polymer in the solvent blend.FP, or IB, or KP were dissolved in the FFS at a concentration of 4 % w/w. 265FP3, namely the formulation with the highest plasticizer content, and FP2, namely the formulation prepared with the highest acetone content. Therefore, this feature might be explained taking into account the solubilizing effect of the plasticizer, which reduced the drug thermodynamic activity in the film and, consequently, decreased its flux through the skin (Tukey test, p=0.048).In the case of IB loaded FFS, the drug permeation was positively influenced by the plasticizer 270 concentration (IB3) and the drug permeation profiles followed the rank order: IB3>IB2>IB1 (Tukey test, p<0.01). Since IB is freely mixable with EuRL (Wu and McGinity, 2001), the key factor

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Influence of chemical and structural features of low molecular weight heparins (LMWHs) on skin penetration

Cited by 17 publications

References 22 publications

In vitro Penetration and in vivo Distribution of Honokiol into the Intervertebral Disc in Rat

In vitro Penetration and in vivo Distribution of Honokiol into the Intervertebral Disc in Rat

Rationalizing the Design of Hyaluronic Acid-Decorated Liposomes for Targeting Epidermal Layers: A Combination of Molecular Dynamics and Experimental Evidence

A glimpse in critical attributes to design cutaneous film forming systems based on ammonium methacrylate

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