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 Resistivity Technique for the Evaluation of the Integrity of Buccal and Esophageal Epithelium Mucosa for In Vitro Permeation Studies: Swine Buccal and Esophageal Mucosa Barrier Models

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 643
Author(s):  
Jaiza Samara Macena de Araújo ◽  
Maria Cristina Volpato ◽  
Bruno Vilela Muniz ◽  
Gabriela Gama Augusto Xavier ◽  
Claudia Cristina Maia Martinelli ◽  
...  
Keyword(s):  
Cost Effective ◽  
Esophageal Mucosa ◽  
Buccal Epithelium ◽  
Esophageal Epithelium ◽  
Hydrophilic Drugs ◽  
In Vitro Permeation ◽  
Cost Effective Method ◽  
Permeation Studies ◽  
Franz Diffusion Cells

Permeation assays are important for the development of topical formulations applied on buccal mucosa. Swine buccal and esophageal epithelia are usually used as barriers for these assays, while frozen epithelia have been used to optimize the experimental setup. However, there is no consensus on these methods. In transdermal studies, barrier integrity has been evaluated by measuring electrical resistance (ER) across the skin, which has been demonstrated to be a simple, fast, safe, and cost-effective method. Therefore, the aims here were to investigate whether ER might also be an effective method to evaluate buccal and esophageal epithelium mucosa integrity for in vitro permeation studies, and to establish a cut-off ER value for each epithelium mucosa model. We further investigated whether buccal epithelium could be substituted by esophageal epithelium in transbuccal permeation studies, and whether their permeability and integrity were affected by freezing at −20 °C for 3 weeks. Fresh and frozen swine buccal and esophageal epithelia were mounted in Franz diffusion cells and were then submitted to ER measurement. Permeation assays were performed using lidocaine hydrochloride as a hydrophilic drug model. ER was shown to be a reliable method for evaluating esophageal and buccal epithelia. The esophageal epithelium presented higher permeability compared to the buccal epithelium. For both epithelia, freezing and storage led to decreased electrical resistivity and increased permeability. We conclude that ER may be safely used to confirm tissue integrity when it is equal to or above 3 kΩ for fresh esophageal mucosa, but not for buccal epithelium mucosa. However, the use of esophageal epithelium in in vitro transmucosal studies could overestimate the absorption of hydrophilic drugs. In addition, fresh samples are recommended for these experiments, especially when hydrophilic drugs are involved.

Deformable Surfactant Vesicles Loading Ammonium Glycyrrhizinate: Characterization and In Vitro Permeation Studies

2012 ◽  
Vol 9 (5) ◽  
pp. 494-499 ◽  
Author(s):  
Luisa Di Marzio ◽  
Carlotta Marianecci ◽  
Federica Rinaldi ◽  
Sara Esposito ◽  
Maria Carafa
Keyword(s):  
Surfactant Vesicles ◽  
In Vitro Permeation ◽  
Permeation Studies

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 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 Determination of Diclofenac Sodium in Eagle's Minimum Essential Medium with Earle's Balanced Salt Solution

2003 ◽  
Vol 86 (4) ◽  
pp. 681-684
Author(s):  
Patrícia S Lopes ◽  
Telma M Kaneko ◽  
Carolina Y Takano ◽  
Aurea C L Lacerda ◽  
Leandro R Latorre ◽  
...  
Keyword(s):  
Salt Solution ◽  
Diclofenac Sodium ◽  
Reversed Phase ◽  
Minimum Essential Medium ◽  
In Vitro Permeation ◽  
Hydrophilic Drug ◽  
Permeation Studies ◽  
The Mean

Abstract A validated method was developed for determination of diclofenac sodium, considered a model hydrophilic drug for in vitro permeation studies, in Eagle's Minimum Essential Medium (MEM) with Earle's balanced salt solution. Liquid chromatography was used to determine diclofenac sodium. This method was developed with a reversed-phase column Supercosil LC 18, DB 25 cm × 4.5 mm; the mobile phase was methanol with 3% (v/v) acetic acid–Milli-Q water (74 + 26), and detection was at 283 nm. The detection and quantitation limits were 2.41 × 10–8 and 3.31 × 10–5 μg/μL, respectively. The accuracy within-day (n = 3) and day-to-day (n = 7) was 98.83%; the mean variation coefficient for inter- (n = 7) and intraday precision (n = 3) was 12.20%, thus, not exceeding 15%. This method can be used as an analytical procedure for the determination of diclofenac sodium in MEM for in vitro permeation studies.

scholarly journals Novel Design Approaches in the Fabrication of Polymeric Microarray Patches via Micromoulding

Micromachines ◽  
2020 ◽  
Vol 11 (6) ◽  
pp. 554 ◽  
Author(s):  
Inken Ramöller ◽  
Emma McAlister ◽  
Abigail Bogan ◽  
Ana Cordeiro ◽  
Ryan Donnelly
Keyword(s):  
Skin Barrier ◽  
Systemic Delivery ◽  
Porcine Skin ◽  
Density Maps ◽  
In Vitro Permeation ◽  
Wide Range ◽  
Significant Difference ◽  
Permeation Studies ◽  
Novel Design

The focus on novel systems for transdermal delivery of therapeutic agents has increased considerably over recent years, as this administration route comes with many advantages. Polymeric microarray patches (MAPs) are minimally invasive devices that enable systemic delivery of a wide range of drugs by overcoming the outer skin barrier. Conventionally, MAPs fabricated by micromoulding have a low needle density. In this study, the performance of hydrogel-forming MAPs cast using novel industrially manufactured micromoulds with a high needle density (600 needles/0.75 cm2) was compared to that of MAPs obtained using conventional moulds with a lower density (196 needles/0.89 cm2). Surrounding holders for micromoulds were designed for time-efficient fabrication of MAPs. The influence of needle densities on mechanical strength, insertion efficiency and in vitro permeation of ibuprofen sodium (IBU) was analysed. Insertion of both MAPs into an artificial skin model and neonatal porcine skin was comparable. No significant difference was observed in permeation studies of IBU (p > 0.05), with a delivery of 8.7 ± 1.7 mg for low-density and 9.5 ± 0.1 mg for high-density MAPs within 24 h. This highlights the potential of these novel micromoulds for manufacturing polymeric MAPs with a higher needle density for future applications.

Bacterial cellulose membranes as transdermal delivery systems for diclofenac: In vitro dissolution and permeation studies

2014 ◽  
Vol 106 ◽  
pp. 264-269 ◽  
Author(s):  
Nuno H.C.S. Silva ◽  
Artur Filipe Rodrigues ◽  
Isabel F. Almeida ◽  
Paulo C. Costa ◽  
Catarina Rosado ◽  
...  
Keyword(s):  
Bacterial Cellulose ◽  
Transdermal Delivery ◽  
Delivery Systems ◽  
In Vitro Dissolution ◽  
Permeation Studies ◽  
Cellulose Membranes
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