Dermal and Transdermal Macromolecule Delivery Using Enhancer Molecules and Colloidal Carrier Systems - Part 2:...

Area of Science:

• Pharmacology and Drug Delivery
• Materials Science

Background:

• Heparin is a widely used anticoagulant administered via injection or topical application.
• Current administration methods can be invasive and limit topical efficacy.

Purpose of the Study:

• To formulate heparin into non-ionic colloidal carrier systems (CCSs).
• To enhance percutaneous absorption of heparin for systemic and topical administration.
• To develop a non-invasive alternative to traditional heparin delivery methods.

Main Methods:

• Development and characterization of five heparin-loaded CCSs (rheology, droplet size, drug loading).
• In vitro percutaneous absorption studies using Franz diffusion cells and rat skin.
• In vivo efficacy and bioavailability assessment in rats compared to subcutaneous administration.

Main Results:

• Developed CCSs exhibited Newtonian properties with droplet sizes ranging from 109-460 nm.
• High drug loading capacity achieved (500 mg heparin in ~5 mL CCS).
• Significant in vitro heparin diffusion rate (19.216 ± 2.01 USP U/cm2.h) and >50% in vivo percutaneous bioavailability.

Conclusions:

• Novel, non-toxic heparin-loaded CCSs demonstrate potential for percutaneous delivery.
• These CCSs offer a viable alternative to invasive subcutaneous and intravenous heparin administration.
• The developed systems enhance heparin's transdermal penetration for improved therapeutic outcomes.