Dermal and Transdermal Macromolecule Delivery Using Enhancer Molecules and Colloidal Carrier Systems – Part 2: Percutaneous Administration of Heparin

Skin Pharmacology and Physiology

Alyoussef Alkrad J.a· Almalki Y.A.a· Dahmash E.Z.a,b· Hassouneh L.K.b· Neubert R.H.H.c

Author affiliations

aFaculty of Pharmacy, Isra University, Amman, Jordan
bDepartment of Chemical and Pharmaceutical Sciences, School of Life Sciences, Pharmacy and Chemistry, Kingston University, London, UK
cInstitute of Applied Dermatopharmacy, Martin Luther University Halle-, Wittenberg, Germany

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Article / Publication Details

First-Page Preview

Abstract of Research Article

Received: April 13, 2022
Accepted: October 26, 2022
Published online: December 01, 2022

Number of Print Pages: 11
Number of Figures: 7
Number of Tables: 3

ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)

For additional information: https://www.karger.com/SPP

Abstract

Introduction: Heparin is a commonly used anti-coagulant administered either by intravenous or subcutaneous injection for a systemic effect or topically for the treatment of peripheral vascular disorders. Objective: This study aimed to formulate heparin in non-ionic colloidal carrier systems (CCSs) having enhanced percutaneous absorption for systemic and topical administration. Methods: Five CCSs were developed and characterized for their rheological properties, droplet size, and drug loading. The percutaneous absorption of heparin was evaluated in vitro using Franz diffusion cells with rats’ skin and with the aid of a developed high-pressure chromatography method. Furthermore, the efficacy of two developed heparin CCSs was tested percutaneously in rats by measuring the response against the time in comparison to subcutaneous administration. Results: The rheograms and droplet size measurements showed that the developed drug delivery systems have Newtonian properties with a droplet size between 109 and 460 nm. As much as 500 mg of heparin could be loaded in around 5 mL of CCS. Furthermore, using Franz diffusion cells, a diffusion rate of 19.216 ± 2.01 USP U/cm2.h could be achieved for heparin-loaded CCSs. Moreover, the estimated percutaneous in vivo relative bioavailability in comparison to subcutaneous administration could reflect that at least more than 50% of the drug passed through the skin. Conclusion: The developed novel non-toxic CCSs containing heparin can be good candidates for percutaneous administration as alternative delivery systems for subcutaneous and intravenous invasive administration.

© 2022 S. Karger AG, Basel

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First-Page Preview

Abstract of Research Article

Received: April 13, 2022
Accepted: October 26, 2022
Published online: December 01, 2022

Number of Print Pages: 11
Number of Figures: 7
Number of Tables: 3

ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)

For additional information: https://www.karger.com/SPP

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