Transdermal delivery of polidocanol from sol–gel patch: ex vivo skin permeation studies using iontophoresis for the treatment of varicose veins

A biocompatible topical thermo-reversible hydrogel containing Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs) was studied as an innovative strategy for the topical treatment of skin inflammatory diseases. The PF-NLCs-F127 hydrogel was characterized physiochemically and short-time stability tests were carried out over 60 days. In vitro release and ex vivo human skin permeation studies were carried out in Franz diffusion cells. In addition, a cytotoxicity assay was studied using the HaCat cell line and in vivo tolerance study was performed in humans by evaluating the biomechanical properties. The anti-inflammatory effect of the PF-NLCs-F127 was evaluated in adult male Sprague Daw-ley® rats using a model of inflammation induced by the topical application of xylol for 1 h. The developed PF-NLCs-F127 exhibited a heterogeneous structure with spherical PF-NLCs in the hydrogel. Furthermore, a thermo-reversible behaviour was determined with a gelling temperature of 32.5 °C, being close to human cutaneous temperature and thus favouring the retention of PF. Furthermore, in the ex vivo study, the amount of PF retained and detected in human skin was high and no systemic effects were observed. The hydrogel was found to be non-cytotoxic, showing cell viability of around 95%. The PF-NLCs-F127 is shown to be well tolerated and no signs of irritancy or alterations of the skin’s biophysical properties were detected. The topical application of PF-NLCs-F127 hydrogel was shown to be efficient in an inflammatory animal model, preventing the loss of stratum corneum and reducing the presence of leukocyte infiltration. The results from this study confirm that the developed hydrogel is a suitable drug delivery carrier for the transdermal delivery of PF, improving its dermal retention, opening the possibility of using it as a promising candidate and safer alternative to topical treatment for local skin inflammation and indicating that it could be useful in the clinical environment.

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Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches

Pharmaceutics ◽

10.3390/pharmaceutics12030282 ◽

2020 ◽

Vol 12 (3) ◽

pp. 282 ◽

Cited By ~ 4

Author(s):

Julia Zhang ◽

Anna Froelich ◽

Bozena Michniak-Kohn

Keyword(s):

Transdermal Delivery ◽

Oral Delivery ◽

Ex Vivo ◽

Skin Permeation ◽

Entrapment Efficiency ◽

Topical Delivery ◽

Onset Of Action ◽

Promising Alternative ◽

Inflammatory Drugs ◽

Systemic Onset

The aim of this study is to develop, characterize and compare conventional liposome, deformable liposome (transfersome) and microemulsion formulations as potential topical delivery systems for meloxicam. Liposomes were characterized in terms of vesicle size, zeta potential and entrapment efficiency. For microemulsions, particle size, electrical conductivity and viscosity studies were performed to assess the structure of the investigated systems. An ex vivo skin permeation study has been conducted to compare these formulations. The dermal and transdermal delivery of meloxicam using these formulations can be a promising alternative to conventional oral delivery of non-steroidal anti-inflammatory drugs (NSAIDs) with enhanced local and systemic onset of action and reduced side effects.

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Emulgels Containing Carbopol 934P and Different Vegetable Oils for Topical Propolis Delivery: Bioadhesion, Drug Release Profile, and Ex Vivo Skin Permeation Studies

AAPS PharmSciTech ◽

10.1208/s12249-020-01748-3 ◽

2020 ◽

Vol 21 (6) ◽

Author(s):

Rafaela Said dos Santos ◽

Camila Félix Vecchi ◽

Hélen Cássia Rosseto ◽

Jéssica Bassi da Silva ◽

Maria Eduarda Lima Dano ◽

...

Keyword(s):

Drug Release ◽

Vegetable Oils ◽

Ex Vivo ◽

Skin Permeation ◽

Release Profile ◽

Drug Release Profile ◽

Permeation Studies ◽

Carbopol 934P

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Nanoethosomes for transdermal delivery of tropisetron HCl: multi-factorial predictive modeling, characterization, and ex vivo skin permeation

Drug Development and Industrial Pharmacy ◽

10.1080/03639045.2017.1287717 ◽

2017 ◽

Vol 43 (6) ◽

pp. 958-971 ◽

Cited By ~ 20

Author(s):

Hanaa A. Abdel Messih ◽

Rania A. H. Ishak ◽

Ahmed S. Geneidi ◽

Samar Mansour

Keyword(s):

Predictive Modeling ◽

Transdermal Delivery ◽

Ex Vivo ◽

Skin Permeation

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Association of 3-O-methylquercetin with β-cyclodextrin: complex preparation, characterization and ex vivo skin permeation studies

Journal of Inclusion Phenomena and Macrocyclic Chemistry ◽

10.1007/s10847-008-9450-4 ◽

2008 ◽

Vol 62 (1-2) ◽

pp. 149-159 ◽

Cited By ~ 13

Author(s):

Liege Schwingel ◽

Daniel Fasolo ◽

Maribete Holzschuh ◽

Ivana Lula ◽

Rubén Sinisterra ◽

...

Keyword(s):

Ex Vivo ◽

Skin Permeation ◽

Cyclodextrin Complex ◽

Complex Preparation ◽

Permeation Studies

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Ceramide-based nanostructured lipid carriers for transdermal delivery of isoliquiritigenin: Development, physicochemical characterization, and in vitro skin permeation studies

Korean Journal of Chemical Engineering ◽

10.1007/s11814-016-0267-3 ◽

2016 ◽

Vol 34 (2) ◽

pp. 400-406 ◽

Cited By ~ 10

Author(s):

Geun Young Noh ◽

Ji Young Suh ◽

Soo Nam Park

Keyword(s):

Transdermal Delivery ◽

Skin Permeation ◽

Physicochemical Characterization ◽

Nanostructured Lipid Carriers ◽

In Vitro Skin Permeation ◽

Permeation Studies

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Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Pharmaceutics ◽

10.3390/pharmaceutics13081218 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1218

Author(s):

Mohammad A. Altamimi ◽

Afzal Hussain ◽

Sultan Alshehri ◽

Syed Sarim Imam ◽

Usamah Abdulrahman Alnemer

Keyword(s):

Drug Release ◽

Zeta Potential ◽

Transdermal Delivery ◽

Ex Vivo ◽

Skin Permeation ◽

Oral Drug ◽

In Vitro Drug Release ◽

Drug Deposition ◽

Drug Content

Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

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