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Topical Retinoid Drug Treatment for Acne

Analyzing the medical history of the patients to be treated of acne vulgaris will help the therapist or doctor to decide which treatment will work best for the patient while simultaneously minimizing any likelihood of complications.

Different Groups of Retinoids

Non-inflammatory acne is characterized by the presence of comedones. The best method of treatment for this type of acne is the topical retinoid preparation. Using topical retinoids along with systemic drugs can treat severe forms of acne.

The effect of retinoids on acne was first observed in the 1970s. The retinoids were derived from Vitamin A and have 3 known generations as of this writing; the third generation retinoids are known to have anti-inflammatory properties. These 3 generations of retinoids are classified into non-aromatic retinoids, mono-aromatic retinoids, and poly-aromatic retinoids. Non-aromatic retinoids include retinol, tretinoin, and isotretinoin. Poly-aromatic retinoids include arotinoid, adapalene, and tazatorene. Among the topical retinoids that popular in treating acne are trenetoin, isotrenetoin, adapalene, tazarotene, and retinaldehyde.

The Function of Topical Retinoids

Acme therapy is aimed to decrease the incidences and minimize the severity of the basic clinical lesion known as microcomedo. A microcomedo has the tendency to grow into full-blown severe cases of acne. When retinoids are introduced in the system, it binds and activates the retinoid receptor cells. When retinoids exert their influence on these receptors, it normalizes the cell differentiation in the follicles of the epithelial layer, thus eliminates the formation of comedones. Because of this unique binding and activation properties of retinoids, they are considered as vitamins as well as hormones. Treating acne with retinoid is not restricted to the application on the visible lesions but targeting the entire area prone to acne helps prevent future spots.


Tretinoin is the generic name of the first-generation non-aromatic topical retinoid Vitamin A acid, which has a high affinity in binding nuclear hormone retinoic acid receptors and cellular retinoic acid binding receptor.

Tretinoin is available in the market in cream, gel, and solution forms. Using tretinoin in the treatment prevents the formation of new comedones, increases the formation of follicular epithelial cells, and initiates the elimination of corneocytes that enables the normalization of keratinazation and drainage of comedones. As a result, the follicles became clearer and more aerobic, allowing the antimicrobial agents to reach them. This inhibits the proliferation the P. acne bacteria and stops any pro-inflammatory activity on the follicles.

It is advisable to inform the patient of the epidermal irritation, pustular flare side effects, and the delayed and erratic improvements that could occur after application of tretinoin treatment. Application of tretinoin may cause photosensitization, advising a night-time application starting with a lower potency of tretinoin. Those patients that have sensitive skins can consider any other types of retinoid that causes less discomfort. However, two new formulations of tretinoin – polyolpolymer-2 and microsponge delivery system are now being used for lower accompanying irritation.


Isotretinoin is a first generation retinoid that has the capacity to bind CBRAR and RAR receptors and possesses comedolytic properties that change the turnover of epithelial cells in hair follicles. Topical isotretinoin is available in gel formula at 0.05% potency but does not suppress sebum unlike oral isotretinoin. It is almost equal to tretinoin in the reduction of comedolytic and inflammatory acne, and the adverse irritation effects that can be experienced when using tretinoin is not as frequently and as intensely experienced with isotretinoin.


Adapalene is a third-generation poly-aromatic retinoid that exhibits some characteristics of tretinoin despite their physiolochemical difference. Adapalene is extremely comedolytic and anti-inflammatory due to its ability to normalize keratinization and inflammation. Although it is as effective as tretinoin, topical application of adapalene is much better tolerated and produces less skin irritation and erythma. There is no risk of photosensitization when applying adapalene during the daytime as it is stable with oxygen and light and can be combined with benzoyl peroxide. It also goes directly to the targeted area once it gets past through the corneum strat, enclosing itself in the epidermis and hair follicles. This is due to the fact that the absorption rate of adapalene is negligible. Researchers are currently looking at the enormous potential of adapalene in acne therapy.


Application of tazarotene once a day showed greater success in treating non-inflammatory acne and reduction of the acne’s severity compared to the results on tretinoin. Tarazotene gel 0.05% is more effective than tretinoin gel with the same potency in lessening the number of open comedones and papules, and reduces pustules faster. However, the side effects that come along with it are as intolerable as tretinoin. These side effects include moderate skin irritation accompanied by burning or itching sensations, erythema, and peeling and dryness of the skin. Thus, to lower irritation levels, application of tazarotene for short periods of time (30 seconds to five minutes) is highly recommended.


0.05% potency of retinaldehyde has similar effects to that of tretinoin at 0.025% potency. It also has comedolytic effects and directly prevents the proliferation of P. acne. Retinaldehyde is a better option among retinoids because it has much better tolerability.