Microemulsions as a Surrogate Carrier for Dermal Drug Delivery

Abstract

Microemulsions are isotropic, thermodynamically stable transparent (or translucent) systems of oil, water, and surfactant, frequently in combination with a cosurfactant with a droplet size usually in the range of 20-200 nm. Since their discovery, they have attained increasing significance both in basic research and in industry. Due to their distinct advantages such as enhanced drug solubility, thermodynamic stability, facile preparation, and low cost, uses and applications of microemulsions have been numerous. Recently, there is a surge in the exploration of microemulsion for transdermal drug delivery for their ability to incorporate both hydrophilic (5-fluorouracil, apomorphine hydrochloride, diphenhydramine hydrochloride, tetracaine hydrochloride, and methotrexate) and lipophilic drugs (estradiol, finasteride, ketoprofen, meloxicam, felodipine, and triptolide) and enhance their permeation. Very low surface tension in conjunction with enormous increase in the interfacial area due to nanosized droplets of the microemulsion influences the drug permeation across the skin. A large number of oils and surfactants are available, which can be used as components of microemulsion systems for transdermal delivery but their toxicity, irritation potential, and unclear mechanism of action limit their use. Besides surfactants, oils can also act as penetration enhancers (oleic acid, linoleic acid, isopropyl myristate, isopropyl palmitate, etc.). The transdermal drug delivery potential of microemulsions is dependent not only on the applied constituents of the vehicle but also drastically on the composition/internal structure of the phases which may promote or hamper the drug distribution in the vehicles. This article explores microemulsion as transdermal drug delivery vehicles with emphasis on components selection for enhanced drug permeation and skin tolerability of these systems and further future directions.

Transdermal Drug Delivery and Methods to Enhance It

“…Их характерной особенностью является возможность вводить в их состав как водо-, так и жирорастворимые компонен-ты, обеспечивая в дальнейшем более высокую аб-сорбцию активных компонентов неповрежденным участком кожного покрова [22][23][24][25]. Привлекатель-ными эмульсии являются также с точки зрения про-стоты производства и высокой растворяющей спо-собности [21,[24][25][26]. Помимо прочего при введении ЛВ в эмульсии в ряде случаев становится возмож-ным избежать гидролиза, разложения и окисления внесенных субстанций [21].…”

“…Эмульсии представ-ляют собой гетерогенную систему как минимум из двух несмешивающихся жидкостей, одна из ко-торых (дисперсная фаза) диспергирована в другой (дисперсная среда). В зависимости от внесенного в систему эмульгатора различают прямые эмульсии («масло в воде») и обратные («вода в масле») [21][22][23][24]26]. Возможно создание сложных эмульсий, в ко-торых капли масла диспергированы в каплях воды, которые, в свою очередь, диспергированы в масле, либо наоборот [23].…”

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

“…Microemulsion formulations can increase drug transdermal permeation, as has been demonstrated in numerous studies (Kreilgaard, Pedersen, Jaroszewski, 2000;Sintov, Sharipo, 2004;Hua et al, 2004;Sintov, Botner, 2006;Sintov, Brandys-Sitton, 2006;Heuschkel, Goebel, Neubert, 2008;Azeem et al, 2009;Neubert, 2011). Several hypotheses have been put forward for the mechanism of drug permeation enhancement.…”

Untitled

“…Vitamin C helps to facilitate recovery from fungal infection and reduces symptoms of inflammation associated with fungal and yeast infections. [6][7][8][9] With all the above aspects keeping in mind, the present work was developed to investigate the potential of microemulsion-based topical drug delivery system containing curcumin oil as active moiety and Vitamin C as an adjunct for the treatment of fungal infection with antifungal and antioxidant activity together.…”