23 Antiperspirants

E. Holzle

Introduction

Antiperspirants are agents that suppress eccrine sweating. They are widely
used to curb cosmetically disturbing underarm wetness. Antiperspirants act
selectively at the eccrine sweat glands and do not affect apocrine glands. The
latter are responsible for the characteristic axillary body odour. The most
frequently used type of antiperspirants are metal salt solutions [21]. They
also act as antimicrobials and, thus, against the body odour. They abolish the
growth of bacteria flourishing in the humid and warm microenvironment of
the axillae [24] and prevent the formation of odoriferous substances gener-
ated from apocrine sweat by the action of bacteria [30, 31, 47, 50]. The effi-
cacy of deodorants is, however, not the subject of the present article and will
be dealt with only parenthetically.
Axillary sweating is mainly emotionally triggered and has its onset at pu-
berty. It is mainly cosmetically disturbing and comprises rarely any health
hazard. In some instances problems arise from microbial invasion, resulting
in bacterial or mycotic infections of the axillary skin. Excessive moisture fa-
cilitates maceration with consequent inflammation leading to intertrigo.
Antiperspirants have been known for many years and their use is very
common, especially in industrialised countries. They comprise a huge market
[10, 12]. Nevertheless, proprietary products are still to be optimised. With in-
creasing efficacy, their irritating potential also rises and adverse effects may
become unacceptable for consumers.
Different classes of chemicals are used as antiperspirants; these include as-
tringent agents, local anaesthetics, acids and aldehydes, metal salt solutions
and anticholinergics. All antiperspirants also act, directly or indirectly, as
deodorants. Some, such as metal salt solutions, are disinfectants or astrin-
gents which reduce bacterial colonisation of the skin. Finally, all of them dry
the skin surface and, thus, interfere indirectly with the growth conditions of
bacteria.

B. Gabard et al. (eds.), Dermatopharmacology of Topical Preparations

© Springer-Verlag Berlin Heidelberg 2000
402 E. Holzle

Pharmacology and Mechanism of Action

Acids and Aldehydes

The astringent agents formaldehyde, glutaraldehyde, tannic acid, and tri-

chloracetic acid denature proteins and, upon topical application to the skin,
can generate a superficial closure of the sweat pore by denaturing the keratin
of the uppermost layers of corneocytes [11, 26, 43]. Since only the very
superficial cell layers are affected, the closure will be repaired by desquama-
tion within few days. Treatment would be necessary almost daily.
A severe adverse effect of formaldehyde is its high potential of sensitisa-
tion leading to allergic contact dermatitis. About 15-20% of treated patients
have been shown to become affected. Hexamethylene tetramine, from which
formaldehyde is released by the acid eccrine sweat, is thought to possess a
week sensitising potential and is used in some preparations. Glutaraldehyde
is not so effective in the axillae and, when applied in higher concentration,
leads to disturbing discoloration of the horny layer. Tannic acid, sometimes
derived from chestnut or oak extracts, exerts little antiperspirant activity.

Local Anaesthetics

Blockade of peripheral nerves by local anaesthetics also affects the sympa-

thetic nervous fibres supplying the eccrine sweat glands. In an experimental
approach, a mixture from 5% lido cain and 5% prilocain was tested for its
antihidrotic features [27]. There was sufficient penetration through the stra-
tum corneum and also a measurable suppression of secretory activity. In
practice, however, these preparations are insufficient. In addition, local
anaesthetics have at least a moderate potential to induce contact hypersensi-
tivity.
In a recent experimental approach, botulinum toxin A has been applied by
subcutaneous injections with very promising results [14]. Since injections are
required, this substance cannot be used in commercial topical products.

Anticholinergics

Anticholinergics can effectively block the secretory activity of eccrine sweat

glands [46]. They would be the ideal antiperspirant if they penetrated the
horny layer and acted only locally. There are, however, two main problems:
(1) percutaneous absorption of anticholinergics is not always sufficient to
achieve a long lasting anhidrosis and (2) if larger amounts of anticholiner-
gics are absorbed via the skin, systemic adverse effects will occur. A further
draw back is the potential of anticholinergics to induce contact hypersensi-
tivity [1, 36]. In experimental settings, scopolamine hydrochloride and its es-
ters [32], poldine methosulfate [13], propantheline bromide, and hexapyrro-