Influence of the formulation type (o/w, w/o/w emulsions and ointment) on the topical delivery of paromomycin

Abstract

Ointments containing paromomycin (PA) have been used for topical treatment of cutaneous leishmaniasis. Although influence of the vehicle on skin permeation is crucial for optimization of formulations containing PA, this aspect has not been investigated experimentally. In this study, we have evaluated the influence of the formulation type [oil-in-water (o/w), water-in-oil-in-water (w/o/w) emulsions and ointment] on in vitro release and skin permeation of PA and experiments were carried out on cellulose acetate membrane and skin biopsies from hairless mice, respectively. PA release from o/w emulsion (51.7% ± 0.9 of dose applied) was faster than that observed for w/o/w emulsion (3.0% ± 0.5). PA absorption from o/w emulsion (87.1% ± 3.9) through stripped skin was 5 to 6 times higher than that observed for w/o/w multiple emulsion (14.7% ± 0.5) and ointment (16.6% ± 0.1). PA permeation through intact (normal) skin was negligible for all tested formulations. Skin uptake from o/w emulsion (0.9% ± 0.1) was greater than that observed for w/o/w multiple emulsion (0.3% ± 0.1) and ointment (0.1% ± 0.1). These results suggest that a hydrophilic vehicle (o/w emulsion) could be an interesting alternative to improve topical delivery of PA.

A review of current treatments strategies based on paromomycin for leishmaniasis

“…Another investigation related to PM topical delivery was related to the formulation vehicle (emulsion or ointment). The authors prepared three different formulations [127]: 1% PM water/oil/water (W/O/W) emulsion, 1% PM oil/water (O/W) emulsion and 1% PM ointment. The in vitro release profile and skin permeation of these formulations were evaluated.…”

“…However, PM absorption from O/W emulsion (around 87%) through stripped (without stratum corneum barrier) skin was 5-6 times higher than that observed for the other two formulations. Therefore, the authors proposed O/W emulsion containing PM as the best alternative to improve the topical delivery of this drug [127].…”

Dermal and Transdermal Delivery of Active Substances from Semisolid Bases

“…Emulsions may be two-phase systems (o/w or w/o) or multi-phase systems (w/o/w or o/w/o) [20][21][22]42] . Among emulsion bases, creams, emulgels, bigels, microemulsion gels can be distinguished [20][21][22]42] . The cream is a conventional semisolid preparation.…”

Optimization of Rheological Behaviour and Skin Penetration of Thermogelling Emulsions with Enhanced Substantivity for Potential Application in Treatment of Chronic Skin Diseases

“…The vehicle of a topical formulation plays an important role with respect to disease control and therapeutic outcome. It controls the penetration profile of the preparation [1,2,3,4,5] and has an effect on the skin barrier function [6,7]. This can improve or worsen the healing process of diseased skin.…”