scholarly journals Transdermal Nitroglycerin Delivery Using Acrylic Matrices: Design, Formulation, and In Vitro Characterization

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Houman Savoji ◽  
Amir Mehdizadeh ◽  
Ahmad Ramazani Saadat Abadi
Keyword(s):  
Skin Permeation ◽  
Peel Strength ◽  
Adhesion Properties ◽  
Pressure Sensitive Adhesives ◽  
In Vitro Characterization ◽  
Chemical Permeation Enhancers ◽  
Transdermal Drug Delivery Systems ◽  
Franz Diffusion Cells ◽  
Chemical Permeation

Nitroglycerin (TNG) transdermal drug delivery systems (TDDSs) with different acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) were prepared. The effects of PSAs and CPEs types and concentrations on skin permeation and in vitro drug release from devices were evaluated using the dissolution method as well as the modified-jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that the permeation rate or steady state flux (Jss) of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak 2516 and Duro-Tak 2054 showed the highest and Duro-Tak 2051 showed the lowest Jss. Among the various CPEs, propylene glycol and cetyl alcohol showed the highest and the lowest enhancement of the skin permeation of TNG, respectively. The adhesion properties of devices such as 180° peel strength and probe tack values were obtained. It was shown that increasing the concentration of CPE led to reduction in the adhesion property of PSA. Moreover, after optimization of the formulation, it was found that the use of 10% PG as a CPE and 25% nitroglycerin loading in Duro-Tak 2054 is an effective monolithic DIAP for the development of a transdermal therapeutic system for nitroglycerin.

Chemical Permeation Enhancers for Transdermal Delivery of Thiocolchicoside: Assessment of Ex-vivo Skin Flux and In-vivo Pharmacokinetics

2017 ◽  
Vol 10 (5) ◽  
pp. 3827-3835
Author(s):  
Y Madhusudan Rao ◽  
Gayatri P ◽  
Ajitha M ◽  
P. Pavan Kumar ◽  
Kiran kumar
Keyword(s):  
Passive Control ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vivo Studies ◽  
Permeation Enhancers ◽  
Casting Technique ◽  
Chemical Permeation Enhancers ◽  
Chemical Permeation ◽  
In Vivo Pharmacokinetics

Present investigation comprises the study of ex-vivo skin flux and in-vivo pharmacokinetics of Thiocolchicoside (THC) from transdermal films. The films were fabricated by solvent casting technique employing combination of hydrophilic and hydrophobic polymers. A flux of 18.08 µg/cm2h and 13.37µg/cm2h was achieved for optimized formulations containing 1, 8-cineole and oleic acid respectively as permeation enhancers. The observed flux values were higher when compared to passive control (8.66 µg/cm2h). Highest skin permeation was observed when 1,8-cineole was used as chemical permeation enhancer and it considerably (2-2.5 fold) improved the THC transport across the rat skin. In vivo studies were performed in rabbits and samples were analysed by LC-MS-MS. The mean area under the curve (AUC) values of transdermal film showed about 2.35 times statistically significant (p<0.05) improvement in bioavailability when compared with the oral administration of THC solution. The developed transdermal therapeutic systems using chemical permeation enhancers were suitable for drugs like THC in effective management of muscular pain.    

scholarly journals Penetration of Chlorhexidine into Human Skin

2008 ◽  
Vol 52 (10) ◽  
pp. 3633-3636 ◽  
Author(s):  
T. J. Karpanen ◽  
T. Worthington ◽  
B. R. Conway ◽  
A. C. Hilton ◽  
T. S. J. Elliott ◽  
...  
Keyword(s):  
Human Skin ◽  
High Performance ◽  
Skin Permeation ◽  
Full Thickness ◽  
Alternative Strategies ◽  
Thickness Skin ◽  
Skin Antisepsis ◽  
Permeation Studies ◽  
Franz Diffusion Cells

ABSTRACT This study evaluated a model of skin permeation to determine the depth of delivery of chlorhexidine into full-thickness excised human skin following topical application of 2% (wt/vol) aqueous chlorhexidine digluconate. Skin permeation studies were performed on full-thickness human skin using Franz diffusion cells with exposure to chlorhexidine for 2 min, 30 min, and 24 h. The concentration of chlorhexidine extracted from skin sections was determined to a depth of 1,500 μm following serial sectioning of the skin using a microtome and analysis by high-performance liquid chromatography. Poor penetration of chlorhexidine into skin following 2-min and 30-min exposures to chlorhexidine was observed (0.157 ± 0.047 and 0.077 ± 0.015 μg/mg tissue within the top 100 μm), and levels of chlorhexidine were minimal at deeper skin depths (less than 0.002 μg/mg tissue below 300 μm). After 24 h of exposure, there was more chlorhexidine within the upper 100-μm sections (7.88 ± 1.37 μg/mg tissue); however, the levels remained low (less than 1 μg/mg tissue) at depths below 300 μm. There was no detectable penetration through the full-thickness skin. The model presented in this study can be used to assess the permeation of antiseptic agents through various layers of skin in vitro. Aqueous chlorhexidine demonstrated poor permeation into the deeper layers of the skin, which may restrict the efficacy of skin antisepsis with this agent. This study lays the foundation for further research in adopting alternative strategies for enhanced skin antisepsis in clinical practice.

scholarly journals Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran
Keyword(s):  
Analgesic Activity ◽  
Skin Permeation ◽  
Tween 80 ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Topical Gel ◽  
Carbopol Gel ◽  
Franz Diffusion Cells ◽  
Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

Formulation and Evaluation of DHA Oil based Nicotinamide Nanoemulsion Gel for Treating Atopic Dermatitis

2020 ◽  
Vol 10 (6) ◽  
pp. 892-901
Author(s):  
Gayathri P. Pradeep ◽  
Vidya Viswanad
Keyword(s):  
Drug Release ◽  
Cell Line ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Nanoemulsion Gel ◽  
Permeation Studies ◽  
Franz Diffusion Cells

Background: Atopic dermatitis (or eczema) can be defined as a chronic inflammatory condition accompanied by severe pruritus. Objective: The prepared gel was evaluated for in vitro drug release, in vitro occlusion studies, transepidermal water loss studies, skin permeation studies, in vitro skin irritation studies and antiinflammatory cell line studies. Methods: In vitro drug release studies were performed using Franz diffusion cells. The in vitro occlusion studies were carried out by the procedure reported by Wissing et al. TEWL determination was done by the method proposed by Reiger. The skin permeation studies were carried out using porcine skin using Franz diffusion cells. In vitro skin irritation study was carried out using HETCAM (Hen’s Egg Test on the Chorioallantoic Membrane) method. Anti-inflammatory cell line studies were carried out using RAW 264.7 cell lines. Results: In vitro drug release studies,drug release of nicotinamide from nanoemulsion gel was found to be more than marketed gel. Kinetic modelling showed a higuchi model with non-fickian diffusion. In vitro occlusion study showed the percentage of evaporated water from prepared nanoemulsion formulation after 72 h is very less compared with the other formulations. The TEWL measurement shows the reduction in TEWL has more in prepared nanoemulsion gel than other formulations. Anti-inflammatory cell line studies proved that the nanoemulsion gel has inhibition capacity on COX activity, LOX activity, Inducibe nitric oxide synthase and cellular nitrate levels. Conclusion: DHA oil based nicotinamidenanoemulsion gel were prepared successfully and the evaluation of prepared gel showed better drug release and skin permeation with better antiinflammatory activity.

scholarly journals Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 566 ◽  
Author(s):  
Aneta Pokorna ◽  
Pavel Bobal ◽  
Michal Oravec ◽  
Lucie Rarova ◽  
Janette Bobalova ◽  
...  
Keyword(s):  
Blood Circulation ◽  
Time Range ◽  
Enhancement Ratio ◽  
Transdermal Administration ◽  
Good Patient Compliance ◽  
Model Drug ◽  
Franz Diffusion Cells ◽  
Chemical Permeation

Transdermal administration of drugs that penetrate, in this case directly into the blood circulation, has many advantages and is promising for many drugs thanks to its easy application and good patient compliance. (S)-8-Methyl-6,9-diazaspiro[4.5]decan-7,10-dione (alaptide), has been studied as a potential chemical permeation enhancer. Based on its structure, four selected piperazine-2,5-diones were synthesized by means of multi-step synthetic pathways. All the compounds were investigated on their ability to enhance the permeation of the model drug theophylline from the hydrophilic medium propylene glycol:water (1:1). In vitro experiments were performed using vertical Franz diffusion cells at constant temperature 34 ± 0.5 °C and using full-thickness pig (Sus scrofa f. domestica) ear skin. Withdrawn samples were analyzed by RP-HPLC for determination of the permeated amount of theophylline. All the compounds were applied in ratio 1:10 (w/w) relative to the amount of theophylline. One hour after application, the permeated amount of theophylline from formulations with alaptide and (3S,6S)-3,6-dimethylpiperazine-2,5-dione, was ca. 15- and 12-fold higher, respectively, than from the formulation without the tested compounds. Despite the enhancement ratio of both enhancers in a steady state was ca. 2.3, the pseudo-enhancement ratio in the time range from 1 to 3 h was 4.4. These enhancement ratios indicate that the compounds are able to enhance the permeation of agents through the skin; however, the short-term application of both compound formulations seems to be more advantageous. In addition, the screening of the cytotoxicity of all the prepared compounds was performed using three cell lines, and the compounds did not show any significant toxic effect.

scholarly journals Topical Administration of Cannabidiol: Influence of Vehicle-Related Aspects on Skin Permeation Process

2020 ◽  
Vol 13 (11) ◽  
pp. 337
Author(s):  
Antonella Casiraghi ◽  
Umberto M. Musazzi ◽  
Giorgio Centin ◽  
Silvia Franzè ◽  
Paola Minghetti
Keyword(s):  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Skin Permeation ◽  
Topical Administration ◽  
Optimal Choice ◽  
Literature Evidence ◽  
Hildebrand Solubility Parameter ◽  
Hydrophilic Gel ◽  
Franz Diffusion Cells

Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from Cannabis sativa which, given its claimed beneficial properties and therapeutic potential, has lately aroused considerable attention from the scientific community. Starting from the little literature evidence, the main purpose of this study was to investigate the topical administration of CBD, with particular focus on the influence of vehicle-related aspects on the skin permeation process. This could provide useful information for the design of suitable drug delivery systems which could be used in developing topical medicines and cosmetics. In vitro human skin permeation studies were conducted using modified Franz diffusion cells to compare the performance of four solutions and two semisolid formulations. The Hildebrand solubility parameter was used to better understand the thermodynamic aspects implied in the partitioning process of the cannabinoid compound into the skin. It was interestingly found that a hydrophilic gel, mostly consisting of propylene glycol (79%, w/w), can be an optimal choice for the topical administration of CBD. Moreover, the feasibility of the preparation of CBD-loaded (trans)dermal patches, made with new printing technology, was also demonstrated.

Studies on In Vitro Release Performance of Hydrophilic Drugs and Lipophilic Drugs in Amphiphilic SIS-Based Hot-Melt Pressure Sensitive Adhesives

2013 ◽  
Vol 395-396 ◽  
pp. 389-398
Author(s):  
Yong Nan Hu ◽  
Qing Wang ◽  
Yu Ming Sun ◽  
Xiao Hui Li ◽  
Xin Yi Che ◽  
...  
Keyword(s):  
Lipophilic Drugs ◽  
Good Thermal Stability ◽  
Hydrophilic Drugs ◽  
Pressure Sensitive Adhesives ◽  
Pressure Sensitive ◽  
Blending Method ◽  
Π Complex ◽  
Transdermal Drug Delivery Systems ◽  
Hot Melt

In order to fabricate a kind of amphiphilic hot-melt pressure sensitive adhesives (HMPSAs) suitable for transdermal drug delivery systems (TDDS) of natural medicines, SIS-based hot-melt pressure sensitive adhesives were modified by a melt-blending method, in which a kind of hydrophilic poly (ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) (RLPO) and polyethylene glycol 2000 (PEG2000) were utilized. Functional RLPO and its plasticizer PEG2000 worked as a hydrophilic skeleton of amphiphilic HMPSAs. SEM and FT-IR results indicated that RLPO and SIS were partially compatible with each other through n-π complex between the n electrons of the carbonyl group of RLPO and the π electrons of the benzene rings of SIS and their compound had a good thermal stability. The phase microscope images showed that PEG could improve the compatibility between RLPO phase and SIS phase. As the ratio of SIS/RLPO/PEG equaled to 1/2/1.6, their compounds obtained bi-continuous structures. Geniposide (logP<0) and oleanic acid (logP=9.0) were chosen as representatives of hydrophilic drugs and lipophilic drugs, respectively. It was observed that both hydrophilic drugs and lipophilic drugs had a continuous release in the optimized amphiphilic HMPSAs. In addition, the release behavior of hydrophilic geniposide could be controlled by adjusting the ratio of RLPO to PEG.

Formulation and Evaluation of Isosorbide Dinitrate Acrylic Matrix Transdermal Patches

2011 ◽  
Vol 197-198 ◽  
pp. 1217-1220
Author(s):  
Ponwanit Jarenputtakrun ◽  
Praneet Opanasopit ◽  
Suwannee Panomsuk ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Propylene Glycol ◽  
Isosorbide Dinitrate ◽  
Skin Permeation ◽  
Casting Method ◽  
Pressure Sensitive Adhesive ◽  
Transdermal Drug Delivery System ◽  
Pressure Sensitive Adhesives ◽  
Pressure Sensitive ◽  
Transdermal Patches

The aim of this study was to prepare and investigate the isosorbide dinitrate transdermal patches (IDPs) in the concentration of 40 mg/cm2. Acrylic pressure sensitive adhesives (PSA) were used to formulate IDPs. IDPs were prepared by casting method. The effect of content of PSA, and concentration of enhancer, propylene glycol, in the formulations were evaluated. IDPs were investigated for their thickness, weight/area ratio, adhesiveness and in vitro skin permeation. The higher the content of PSA in the formulation, the higher the thickness and the W/A ratio. Propylene glycol added in the formulation (2.5, 5, 10%) significantly enhanced the skin permeation of ISDN. The higher the content of PG, the higher the flux of ISDN through the skin. Our research suggests that isosorbide dinitrate loaded with 10% of propylene glycol in acrylic matrix pressure sensitive adhesive can be potentially used as a transdermal drug delivery system.

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