scholarly journals Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

2015 ◽  
Vol 51 (1) ◽  
pp. 85-90 ◽  
Author(s):  
Edileia Bagatin ◽  
Tais Aleriana Lucon Wagemaker ◽  
Nelson dos Reis Aguiar Júnior ◽  
Mirela Donato Gianeti ◽  
Erika Maria Berardo Gonçalves ◽  
...  
Keyword(s):  
High Performance ◽  
Standard Treatment ◽  
Skin Penetration ◽  
Aqueous Methanol ◽  
In Vitro Permeation ◽  
Receptor Compartment ◽  
Chemical Peeling ◽  
Deep Layers ◽  
Franz Diffusion Cells

Tretinoin is used in the management of acne and it is part of a gold standard treatment for photoaging. It has also been reported as an agent for superficial chemical peeling in highly concentrated formulations with few considerations about skin penetration. The aim of this study was to evaluate the influence of drug concentration and vehicles currently used on skin penetration of tretinoin. In vitro permeation tests were carried out using Franz diffusion cells fitted with porcine ear skin and 10% aqueous methanol in the receptor compartment. Formulations studied, cream or hydroalcoholic dispersion, containing 0.25%, 1% and 5% of tretinoin were placed in the donor compartment for six hours. Tretinoin concentration in skin layers was measured by high performance liquid chromatography. The largest amount of tretinoin from both vehicles was detected in stratum corneum with significant differences among the three concentrations. The hydroalcoholic dispersion was the best vehicle. Significant amounts of tretinoin were found even in deep layers of epidermis. The formulation with 0.25% tretinoin showed better results when considered the amount of tretinoin on skin in terms of percentage. Finally, skin penetration of tretinoin was influenced by vehicle and concentration of this drug used in formulation.

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.

Development and evaluation of a heparin gel for transdermal delivery via laser-generated micropores

2021 ◽  
Vol 12 (2) ◽  
pp. 133-144
Author(s):  
Deepal Vora ◽  
Yujin Kim ◽  
Ajay K Banga
Keyword(s):  
Transdermal Delivery ◽  
Continuous Intravenous Infusion ◽  
In Vitro Permeation ◽  
Assisted Delivery ◽  
Permeation Studies ◽  
Franz Diffusion Cells ◽  
Transdermal Route ◽  
Poloxamer Gel ◽  
Ablative Laser

Aim: Our study investigated the feasibility of transdermal delivery of heparin, an anticoagulant used against venous thromboembolism, as an alternative to intravenous administration. Materials & methods: Skin was pretreated using ablative laser (Precise Laser Epidermal System [P.L.E.A.S.E.®] technology) for enhanced delivery of heparin. In vitro permeation studies using static Franz diffusion cells provided a comparison between delivery from 0.3% w/v heparin-loaded poloxamer gel and solution across untreated and laser-treated dermatomed porcine ear skin. Results: No passive delivery of heparin was observed. Laser-assisted delivery from solution (26.07 ± 1.82 μg/cm2) was higher (p < 0.05) than delivery from heparin gel (11.28 ± 5.32 μg/cm2). However, gel is likely to sustain the delivery over prolonged periods like a maintenance dose via continuous intravenous infusion. Conclusion: Thus, ablative laser pretreatment successfully delivered heparin, establishing the feasibility of delivering hydrophilic macromolecules using the transdermal route.

scholarly journals Effect of Topical Liposomes Containing Paromomycin Sulfate in the Course of Leishmania major Infection in Susceptible BALB/c Mice

2009 ◽  
Vol 53 (6) ◽  
pp. 2259-2265 ◽  
Author(s):  
Mahmoud R. Jaafari ◽  
Neda Bavarsad ◽  
Bibi Sedigheh Fazly Bazzaz ◽  
Afshin Samiei ◽  
Dina Soroush ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Mouse Skin ◽  
Parasite Burden ◽  
Lesion Size ◽  
Control Group ◽  
In Vitro Permeation ◽  
Significant Difference ◽  
Pm 10 ◽  
Franz Diffusion Cells

ABSTRACT The aim of this study was to evaluate the antileishmanial effects of topical liposomal paromomycin sulfate (PM) in Leishmania major-infected BALB/c mice. Liposomes containing 10 or 15% PM (Lip-PM-10 and Lip-PM-15, respectively) were prepared by the fusion method and were characterized for their size and encapsulation efficiency. The penetration of PM from the liposomal PM formulations (LPMFs) through and into skin was evaluated in vitro with Franz diffusion cells fitted with mouse skin at 37°C for 8 h. The in vitro permeation data showed that almost 15% of the LPMFs applied penetrated the mouse skin, and the amount retained in the skin was about 60% for both formulations. The 50% effective doses of Lip-PM-10 and Lip-PM-15 against L. major promastigotes in culture were 65.32 and 59.73 μg/ml, respectively, and those against L. major amastigotes in macrophages were 24.64 and 26.44 μg/ml, respectively. Lip-PM-10 or Lip-PM-15 was used topically twice a day for 4 weeks to treat L. major lesions on BALB/c mice, and the results showed a significantly (P < 0.001) smaller lesion size in the mice in the treated groups than in the mice in the control group, which received either empty liposomes or phosphate-buffered saline (PBS). Eight weeks after the beginning of the treatment, every mouse treated with LPMFs was completely cured. The spleen parasite burden was significantly (P < 0.001) lower in mice treated with Lip-PM-10 or Lip-PM-15 than in mice treated with PBS or control liposomes, but no significant difference was seen between the two groups treated with either Lip-PM-10 or Lip-PM-15. The results suggest that topical liposomal PM may be useful for the treatment of cutaneous leishmaniasis.

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.

scholarly journals Development and Physicochemical Characterization of Desonide-Loaded Nanocapsule Suspensions

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
M. B. Antonow ◽  
R. Lorenzoni ◽  
G. M. Barbosa ◽  
A. F. Ourique ◽  
P. Gomes ◽  
...  
Keyword(s):  
Particle Size ◽  
High Performance Liquid Chromatography ◽  
High Performance ◽  
Release Kinetics ◽  
Physicochemical Characterization ◽  
Eudragit S100 ◽  
Franz Diffusion Cells ◽  
Negative Zeta Potential

Desonide is a topical corticosteroid that has been used for more than 30 years; however, its prolonged use can induce several side effects, affecting dermis and epidermis. The present work consists of development desonide-loaded nanocapsule suspensions (D-NC) using different polymers (Eudragit S100® or Eudragit L100®) and desonide-loaded lipid-core nanocapsules (D-LNC). They were formulated by interfacial deposition using the preformed polymer method and all formulations showed negative zeta potential and adequate nanotechnological characteristics (particle size 161–202 nm, polydispersity index < 0.20). Simple and sensitive methods using high-performance liquid chromatography (HPLC) were developed to quantify desonide in LNC and to study its release kinetics. The method was linear, specific, precise, and exact and therefore can be applied in quantification of D-NC and D-LNC. We evaluatedin vitromethods for drug release (dissolution, Franz diffusion cells, and dialysis sac) and we use mathematical models (monoexponential, biexponential, and Korsmeyer-Peppas) to show release kinetics from this system.

scholarly journals Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

Uniciencia ◽  
2021 ◽  
Vol 35 (2) ◽  
pp. 1-10
Author(s):  
María Inés Velloso ◽  
Héctor Alfredo Andreeta ◽  
María Fabiana Landoni
Keyword(s):  
Nasal Mucosa ◽  
Tween 80 ◽  
Ionic Surfactant ◽  
Apparent Permeability ◽  
In Vitro Permeation ◽  
Apparent Permeability Coefficient ◽  
Dose Control ◽  
Franz Diffusion Cells ◽  
Cetrimonium Bromide

The aim of the present study was to evaluate the effect of two surfactants on in vitro permeation of butorphanol through equine nasal mucosa. Franz diffusion cells and equine nasal mucosa were used. Three formulations were developed based on citric acid, sodium citrate, sodium chloride, and butorphanol tartrate and administered at a 24.4 g cm-3 dose. Control formulation lacked any penetration enhancer. Formulation 1 (F1) had a cationic surfactant (cetrimonium bromide) and formulation 2 (F2) had a non-ionic surfactant (Tween 80). Statistically comparing flux values at the steady state (Jss), apparent permeability coefficient (Kp), and lag-time from control, F1 and F2 for the respiratory region does not show statistically significant differences (α= 0.05). However, statistically significant differences were found on the Jss and Kp, values from control, F1, and F2 in olfactory mucosa. A statistical analysis on the latter showed significant differences between the Jss values of F1 and F2 and between control and F2. Based on this, Tween 80 proved to be a promising excipient in developing intranasal butorphanol formulations in equines since it increases its passage through the nasal mucosa. These results are very promising to continue with the development of intranasal butorphanol formulation in equines.

scholarly journals Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1213
Author(s):  
Raha Rahbari ◽  
Ionut Ichim ◽  
Ryan Bamsey ◽  
Jemma Burridge ◽  
Owen J. Guy ◽  
...  
Keyword(s):  
Dissociation Constants ◽  
Skin Barrier ◽  
Acid Dissociation ◽  
Acid Dissociation Constant ◽  
Molecular Weights ◽  
Patch Application ◽  
In Vitro Permeation ◽  
Franz Diffusion Cells ◽  
Topical Applications

Polymer-based solid microstructures (MSts) have the potential to significantly increase the quantity and range of drugs that can be administered across the skin. MSt arrays are used to demonstrate their capacity to bypass the skin barrier and enhance permeability by creating microchannels through the stratum corneum, in a minimally invasive manner. This study is designed to demonstrate the ability of MSts to exceed the current boundaries for transdermal delivery of compounds with different molecular weights, partition coefficients, acid dissociation constants, melting points, and water solubilities. In vitro permeation of a range of selected molecules, including acetyl salicylic acid (aspirin), galantamine, selegiline hydrochloride (Sel-HCl), insulin, caffeine, hydrocortisone (HC), hydrocortisone 21-hemisuccinate sodium salt (HC-HS) and bovine serum albumin (BSA) has been studied across excised porcine skin with and without poke and patch application of MSts. Permeation of the molecules was monitored using Franz diffusion cells over 24 h. MSts significantly increased the permeation of all selected molecules up to 40 times, compared to topical applications of the molecules without MSts. The greatest increase in permeation was observed for caffeine with 70 ± 8% permeation and the lowest enhancement was observed for HC with a 2.4 ± 1.3% increase in permeation. The highest obtained flux was BSA (8133 ± 1365 μg/cm2/h) and the lowest flux observed for HC (11 ± 4 μg/cm2/h). BSA and HC also showed the highest (16,275 ± 3078 μg) and the lowest (73 ± 47 μg) permeation amount after 24 h respectively. MSt-treated skin exhibits greatly increased permeation. The molecule parameters (size, acid dissociation constant, partition coefficient and solubility)—traditional hurdles associated with passive diffusion through intact skin—are overcome using MSt skin treatment.

scholarly journals EFECTO DE UN SURFACTANTE NO IONICO EN LA PERMEABILIDAD DE BUTORFANOL A TRAVES DE MUCOSA NASAL EQUINA

2021 ◽  
Vol 19 (suplemento) ◽  
Author(s):  
M I Velloso
Keyword(s):  
Intranasal Administration ◽  
Tween 80 ◽  
Ionic Surfactant ◽  
Apparent Permeability ◽  
In Vitro Permeation ◽  
Equine Medicine ◽  
Site Of Action ◽  
The Central Nervous System ◽  
Franz Diffusion Cells

Implementation of intranasal administration for the delivery of drugs with site of action into the central nervous system, such as butorphanol, became a potential choice in equine medicine.  In this study, using Franz-diffusion cells the in vitro permeation rate through respiratory and olfactory equine nasal mucosa of two butorphanol formulations was estimated and compared.  Both formulations had the same composition, was the exception for formulation 2, that contained 2, 5 x 10 -4 M of a non-ionic surfactant (tween 80). Butorphanol administered dose was 24, 4 mg/cm2. Plots of the cumulative amounts of butorphanol against time were constructed, where maximum flux values at the steady state (Jss), apparent permeability coefficients (Kp) and lag-time (tlag) were estimated. The Jss and Kp show that permeation of butorphanol through olfactory mucosa is different than respiratory mucosa. Moreover, Jss for formulation 2 was higher than formulation 1 in both anatomical areas, probably for the effect of the surfactant. The present results are promising to carry on with the development of formulation of butorphanol for intranasal administration.

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