Skin Pharmacology and Physiology
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Article / Publication Details
Abstract
Introduction: Heparin is a commonly used anticoagulant 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 HPLC method. Furthermore, the efficacy of two developed heparin CCSs were tested percutaneously in rats by measuring the response against the time in comparison to subcutaneous administration.
Results: The rheograms and droplets’ 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 CCS. Furthermore, using Franz diffusion cells, a diffusion rate of 19.216 ± 2.01 USP U/cm2.hr 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 a good candidate for percutaneous administration as alternative delivery systems for subcutaneous and intravenous invasive administration.
S. Karger AG, Basel
Article / Publication Details
Copyright / Drug Dosage / Disclaimer
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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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