Pharmacology of Therapeutic Agents in Photomedicine
Henry W. Lim, Nicholas A. Soter in Clinical Photomedicine, 2018
Tretinoin (all-trans retinoic acid) is a natural metabolite of retinol (vitamin A). Tretinoin is not used orally due to side effects resembling hypervitaminosis A (56). Isotretinoin (13-cis retinoic acid), the other naturally occurring retinol metabolite, achieves maximum blood levels after 2–4 hr and reaches a steady-state concentration in 5–7 days. The elimination half-life ranges from 10.4 to 29.5 hr (57). The absorption of the drug is enhanced by food. The drug is primarily bound to albumin. It can be found in metabolized and unmetabolized forms in the bile and urine. When this teratogenic drug is used in women of childbearing potential, an adequate means of contraception is recommended during therapy, and for at least one menstrual cycle after. This provides a window of safety, since the elimination half-life of isotretinoin is 24 hr, and all the drug should be eliminated in 7 days.
Medical therapy
Dimitris Rigopoulos, Alexander C. Katoulis in Hyperpigmentation, 2017
The most common side effects of tretinoin include a retinoid dermatitis characterized by burning or stinging, erythema, scaling, and dry skin.41,42 Given that tretinoin can be irritating, the dose must be adjusted to prevent inflammation. This inflammation may cause hyperpigmentation, especially in those with dark skin. Fortunately, most adverse effects are reversible on discontinuation of therapy, although the hyperpigmentation/hypopigmentation may persist for many months. Cutaneous reactions are predominantly moderate and only few have been reported to be severe. They are mostly limited to erythema, peeling, or both of the area of application. Generally, side effects are characterized as mild and result in no patient withdrawals.41–43 Special care should be taken when topical tretinoin is administered in patients with possible hypersensitivity to retinoids. In addition, patients should be warned that tretinoin may have a photosensitizing effect. The drug is categorized as class X and should not be administered during pregnancy.
Dermatoses of Pregnancy
Vincenzo Berghella in Maternal-Fetal Evidence Based Guidelines, 2022
Once SG have formed, there are treatment options. Topical tretinoin 0.1% cream has been shown to reduce the appearance of SG/SD when used on early lesions (striae rubra) [14]. It is important to note that once striae have become white and atrophic, topical tretinoin was shown to have no benefit in a double-blind, placebo-controlled study [15]. Topical tretinoin (Retin-A) works by binding to cytoplasmic proteins and nuclear receptors of keratinocytes and altering downstream gene transcription. The end biologic effect is to regulate the growth and differentiation of keratinocytes [16]. In addition to regulating keratinocyte proliferation, topical retinoids have been shown to decrease fine wrinkling, increase dermal collagen, and repair elastin fiber formation [17]. Improvement in the appearance of SD/SG is most likely the result of this particular biologic effect. Tretinoin is pregnancy category C, so use during pregnancy is not recommended. Its use is contraindicated during breastfeeding, which makes it difficult to use during the early stages of SG. The side effects of tretinoin therapy are erythema, desquamation, and photosensitivity limited to the application site.
Nanocrystal: a novel approach to overcome skin barriers for improved topical drug delivery
Published in Expert Opinion on Drug Delivery, 2018
Viral Patel, Om Prakash Sharma, Tejal Mehta
In the present scenario, cosmetic industry has also adopted nanotechnology with the introduction of various products, including sunscreen lotions, moisturizers, and creams. The first nanocrystal-based cosmetic product was launched in 2007 by Juvena, which explored rutin nanocrystals for the photoprotection of the skin. In this study, it was observed that the rutin nanocrystal-based formulation possessed 500-fold higher bioactivity as compared with rutin glucoside solution. The comparison was made between 5%w/v suspension of rutin nanocrystals (nondissolved) and 5%w/v solution of rutin glucoside, which was water soluble. It was concluded that despite 500-fold lower concentration of rutin dissolved in the aqueous phase of nanocrystal suspension, the nanosuspension was about two times more photoprotective for the skin, i.e. the activity of rutin was increased by 1000 times [110,146]. Tretinoin is widely used for the treatment of various dermatological disease/infections. However, photodegradation of tretinoin limits it bioavailability. Lai et al. [147] developed tretinoin nanosuspension by precipitation method, having a particle size and polydispersity index of 330 nm and 0.25, respectively. They concluded that the tretinoin nanocrystals were able to retain the drug in the dermal layers during 8 h of percutaneous study. Tretinoin was found to be more stable after ultraviolet irradiation on the tretinoin nanocrystal-based nanosuspension. Thereby, nanocrystal-based formulation can ameliorate dermal delivery with enhanced stability.
Adverse events related to topical drug treatments for acne vulgaris
Published in Expert Opinion on Drug Safety, 2020
Agnieszka Otlewska, Wojciech Baran, Aleksandra Batycka-Baran
The available topical formulations of tretinoin used for acne are 0.025–0.1% cream, 0.01–0.025% in standard gel, and 0.025–0.1% in vehicles designed to control drug release, increase drug retention in the stratum corneum and inhibit deeper penetration [12]. It is usually administered once daily [12]. There are also formulations containing prepolyolprepolymer-2 which helps to preserve drug particles on the skin surface and in the upper layers of the skin. It has been shown that tretinoin 0.025% gel and 0.025% cream significantly reduces noninflammatory and inflammatory acne lesions in a once daily application manner compared with vehicle by week 12 [22]. The first results of treatment may be seen after 2–3 weeks, but improvement is usually gradual and the majority of the patients need 2–4 months to achieve positive results [12]. The systemic toxicity has not been linked with topical tretinoin [12].
Liposome-based combination therapy for acne treatment
Published in Journal of Liposome Research, 2020
İpek Eroğlu, Minela Aslan, Ümran Yaman, Merve Gultekinoglu, Semih Çalamak, Didem Kart, Kezban Ulubayram
In combination therapy options, retinoids are commonly used due to their comedolytic and anti-inflammatory effects. These agents bind to retinoic acid receptors and thus lead to the resolving of microcomedone lesions and that is what makes them ideal for comedonal acne (Geng et al.2009, Zaenglein et al.2016). On the other hand, use of retinoids is limited by their side effects such as local irritation, elevated sensitivity to sunlight and stability problems of the active ingredients (Elbaum 1988, Brisaert et al.2001). A member of retinoids, tretinoin is the most commonly used retinoid for acne, but on the other hand, its irritative potential on the applied area and the barrier of the stratum corneum limit its usage. Also, it is affected by the exposure to oxygen, light, and acids; therefore, effectiveness of topical commercial formulations of tretinoin is mainly limited by the barrier properties of the skin, exposure to oxygen, and easy removal from the site of action (Varani et al.2000, Shin et al.2005). For this purpose, Rahman et al. have formulated liposomal formulations of tretinoin to overcome fore-mentioned problems in patients with AV. Their results indicated that liposomal tretinoin formulations provided improved skin tolerability and patients compliance when compared to the commercial gel product with enhanced activity (Rahman et al.2016).
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