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Follicles play an important role in percutaneous absorption
B Illel1, H Schaefer, J Wepierre
1Centre International de Recherches Dermatologiques (C.I.R.D.), Valbonne, France.
Journal of Pharmaceutical Sciences
|May 1, 1991
Summary
Hair follicles play a crucial role in percutaneous absorption, significantly impacting drug diffusion across the skin. Follicle-free skin shows substantially reduced absorption, highlighting the transappendageal route's importance.
Area of Science:
- Dermatology
- Pharmacokinetics
- Skin Physiology
Background:
- The stratum corneum and follicular pathways' relative contributions to percutaneous absorption remain unclear.
- Understanding these routes is vital for optimizing topical drug delivery and efficacy.
Purpose of the Study:
- To quantitatively assess the significance of the transappendageal route in percutaneous absorption.
- To investigate the role of hair follicles in the in vitro diffusion of various compounds through rat skin.
Main Methods:
- Utilized a hairless rat model with surgically created appendage-free skin.
- Compared in vitro percutaneous absorption of [3H]hydrocortisone, niflumic acid, caffeine, and p-aminobenzoic acid using diffusion cells.
- Examined diffusion in early postnatal (follicle-devoid) versus later postnatal (follicle-developed) rat skin samples.
Main Results:
- Follicles were identified as the predominant pathway for in vitro diffusion of tested compounds in hairless rat skin.
- Steady-state flux and diffusion amounts were 2-4 times lower in appendage-free skin compared to normal skin.
- Follicle-free skin exhibited a fivefold reduction in steady-state flux and total 24-hour diffusion of [3H]hydrocortisone.
Conclusions:
- Appendageal diffusion, primarily through hair follicles, is the major route for percutaneous absorption in hairless rat skin.
- Hair follicles play a more significant role in percutaneous absorption than commonly acknowledged.
- These findings have implications for drug formulation and delivery strategies targeting skin.